Sacubitril: A Promising Option for Patients with Chronic Heart Failure

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Sacubitril: A Promising Option for Patients with Chronic Heart Failure

What is Sacubitril

Sacubitril is a drug used to treat heart failure with a low ejection fraction. It functions by preventing the Neprilysin enzyme from functioning. It aids in raising the concentrations of peptides, which encourages vasodilation and lessen sodium retention in the kidneys. It also improves the cardiac function. 

Valsartan, an angiotensin receptor blocker that aids in blood vessel relaxation and blood pressure lowering, it is used along with sacubitril API. These two medications are collectively known as LCZ696. 

Sacubitril is known as a standard medication in several nations after clinical trials showed that it reduce the likelihood of heart failure hospitalizations and improved symptoms.  It is important to remember Sacubitril is not suitable for everyone.

Use of Sacubitril

It is the medication used to treat heart failure along with reduced ejection fraction. This works by inhibiting the activity called neprilysin, which involves the breakdown of several hormones and peptides which is involved in the breakdown of the several hormones and peptides which can affect blood pressure and fluid balance.

With the combination of angiotensin receptor blockers valsartan, it is used for reducing the risk of cardiovascular death and hospitalization with HFrEF. 

Pharmaceutical raw materials used in the making of Sacubitril have been shown to be more effective than the standard treatment of ACE inhibitors in reducing the risk of death and hospitalization. However, it is important to note this kind of medication is not appropriate for all patients who have been diagnosed with heart disease. They should not use it without the guidance of the healthcare provider. 

Side Effects of Sacubitril

Sacubitril is used for treating heart failure with reduced ejection fraction. Like all other medications, it also has side effects. Here are some of the most common side effects of Sacubitril, that includes:

  • Dizziness
  • Hypotension
  • Hyperkalemia
  • Cough
  • Diarrhoea
  • Elevated serum creatinine

Some of the rare side effects of Sacubitril include:

  • Angioedema (swelling of the lips, face, tongue, or throat)
  • Rash
  • Liver function abnormalities
  • Neutropenia (low levels of white blood cells)
  • Increased uric acid levels
  • Hypersensitivity reactions

It is high time that you should talk to your healthcare provider if you experience any of these side effects while taking Sacubitril.

Precautions of Sacubitril

Sacubitril is the medication used to treat heart failure with a reduced ejection fraction. It is crucial to take the following precautions while using Sacubitril:

  • Inform the healthcare expert about the medical conditions you have or any medication you are taking before using Sacubitril. 
  • Do not take Sacubitril in case you are allergic to it or any of its specific ingredients.
  • Use Sacubitril with caution in case you have a history of angioedema.
  • It may cause hypertension, especially during the first week of the treatment. The healthcare expert may need to adjust your dose and monitor your blood pressure accordingly. 
  • It increases the risk of hyperkalemia. The healthcare provider may need to monitor the potassium level when you start taking Sacubitril. 
  • It may interact with other medications, such as nonsteroidal anti-inflammatory drugs, diuretics, and potassium supplements. Inform the healthcare provider about the other medications you are taking before using Sacubitril. 
  • During pregnancy or breastfeeding, Sacubitril is not recommended. Consult the healthcare provider before taking medicine.

Always follow the advice of the healthcare provider’s instructions while using Sacubitril and inform them immediately if you experience any kind of side effects or have any concerns. 

Chemical composition 

Sacubitril api structure

Sacubitril is the neprilysin inhibitor prodrug with natriuretic activity. It comes with the combination of valsartan in order to reduce the risk of cardiovascular events in any patient. The active metabolite present in Sacubitril, LBQ657 inhibits neprilysin, which is a neutral endopeptidase and cleaves natriuretic peptides such as atrial natriuretic endopeptidase. API manufacturers are trying their best to develop the efficacy of these drugs. 

The molecular formula of Sacubitril is C24H29NO5. 

The molecular weight of Sacubitril is 411.5 g/mol.

The IUPAC name of Sacubitril is 4-{[(2S,4R)-1-(4-Biphenylyl)-5-ethoxy-4-methyl-5-oxo-2-pentanyl]amino}-4-oxobutanoic acid

Conclusion

Sacubitril is the neprilysin inhibitor used in combination with Valsartan as the adjunct to reduce the potential risk of cardiovascular death or hospitalization for heart failure in patients. It is an effective medication for chronic heart failure and reduced ejection fraction. If you have any queries regarding the ingredients, pharmaceutical raw materials,  and chemical compositions, you can always reach out to Bulat Pharmaceutical. Our crew members are here to resolve all your queries. 

Osimertinib: The Miracle Drug for Advanced Lung Cancer Patients

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Osimertinib: The Miracle Drug for Advanced Lung Cancer Patients

Osimertinib is the medication used for the treatment of a certain type of non-small cell lung cancer, which has specific mutations in the epidermal growth factor receptor gene. For a deeper analysis of these drugs, if you are wondering how Osimertinib works or what is the mechanism of the drugs, then this blog is for you. Go through the article to learn more. 

It works by blocking the activity of the mutated EGFR protein, which is solely responsible for driving the spread or growth of cancer cells. By inhibiting the protein, Osimertinib can help to slow down or completely stop the growth of the cancer cells. Eventually, it will lead to a reduction in the size of the tumor and will improve the survival rates in patients with NSCLC. 

This drug is typically prescribed to patients with advanced NSCLC who had previously been treated with other EGFR inhibitors. Osimertinib can also be used as the first-line treatment for patients with NSCLC who have the specific EGFR mutations for which the drug is approved. It is taken orally as a tablet, and usually, it is well tolerated by most patients. However, like any other medication, it may cause side effects, including nausea, diarrhea, skin rash, and fatigue. 

Use of Osimertinib

  • It is used to treat non-small cell lung cancer, which has specific mutations in the epidermal growth factor gene. All these mutations are found in about ten percent of NSCLC cases.
  • It works by blocking the activity of the EGFR protein that is involved in the growth of cancer cells. By blocking the protein, Osimertinib can slow down or shrink the tumors in many patients.
  • Osimertinib is usually taken orally as a tablet once a day. It is necessary to talk to a doctor about the potential advantages and risks of using Osimertinib for NSCLC. 

Side Effects of Osimertinib

Like any other medication, it has many side effects. Some of the common side effects of Osimertinib include:

  • Diarrhea
  • Rash
  • Dry skin
  • Nausea
  • Loss of appetite
  • Fatigue
  • Vomiting
  • Shortness of breath
  • Tightness or chest pain
  • Eye redness, pain, or irritation
  • Headache
  • Swollen or painful glands
  • Unusual bruising or bleeding. 
  • Joint and muscle pain
  • Itching
  • Ulcers. White spot in the mouth or on the tips.
  • Unusual weakness or tiredness
  • Red skin lesions, often with the purple center
  • Skin rash or dryness of the skin
  • Swelling or inflammation of the mouth
  • Decreased appetite
  • Changes in the fingernails or toenails. 
  • Inability to speak
  • Thickening of the bronchial secretions

When all these side effects are usually mild, some of the patients may experience more severe side effects. For instance, Osimertinib can cause lung problems, such as pneumonitis, that can lead to shortness of breath and other respiratory symptoms. This can also cause heart problems such as QT prolongation, and that can cause an irregular heartbeat. 

In many cases, Osimertinib can cause serious allergic reactions that can include difficulty in breathing and swelling of the face, lips, hives, or tongue. 

It is necessary to discuss the potential side effects with the doctor before starting Osimertinib. Patients should also inform the doctor about pre-existing conditions or any other medications which they have taken to reduce the risk of side effects. 

Read Also: Cetilistat: Uses, Side Effects, and Precautions

Who Should Not Take Osimertinib?

Osimertinib is the medication prescribed by doctors to reduce the specific mutations in the epidermal growth factor receptor gene. Here are some of the people who should not take Osimertinib:

  • Pregnant and breastfeeding woman. 
  • People with a history of allergic reactions.
  • People who are currently taking any other medications. 
  • People with any severe kidney or liver disease. 
  • People who have a history of lung or breathing problems. 

It is important to inform the doctor about the medical conditions you have or the medication you are taking before starting the treatment with Osimertinib. The doctor will determine in your case whether Osimertinib is safe and suitable for you or not. 

Chemical composition of Osimertinib

Osimertinib structure

It is a small molecule tyrosine kinase receptor and the antineoplastic agent which is used in the therapy of the selected forms of advanced non-small cell lung cancer. This drug is associated with a moderate rate of serum aminotransferase elevations during the therapy and rare instances of clinically apparent acute liver injuries. 

Osimertinib is a member of the class aminopyrimidins, which is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is substituted by  2-methoxy-4-[2-(dimethylamino)ethyl](methyl)amino-5-acrylamidophenyl group. It is a member of indoles, a secondary amino compound, a biaryl, and a tertiary amino compound. It is the conjugate base of Osimertinib. 

Conclusion

Call your healthcare provider for medical advice and tell them about all the side effects. In case you have any queries related to the chemical compositions of the drugs, then you can reach out to us. The team of Bulat Pharmaceuticals is here to solve all your queries. 

Cetilistat: Uses, Side Effects, and Precautions

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Cetilistat: Uses, Side Effects, and Precautions

Cetilistat belongs to the class of medications, which are called anti-obesity drugs. Obesity is a common condition associated with excessive body fat. 

It increases the risk of many health problems, such as high blood pressure and diabetes, and in some instances, the person may get diagnosed with cancer or heart disease. 

Consumption of more calories than you burn by exercise or daily activities can cause Obesity.  

Use of Cetilistat

Cetilistat is used to treat Obesity and the diseases associated with diabetes. This is administered along with exercise and a healthy low-fat diet plan. 

Cetilistat is a lipase inhibitor that works by binding and blocking the action of the enzyme. It prevents the fat, which means triglycerides in food, from being metabolized and turning into free fatty acids your body can absorb. 

Usually, it is taken with food or after one hour of food. If by any chance, you skipped the meals or the food does not contain any fat, then you can skip taking cetilistat for that specific meal. 

Pharmacology of Cetilistat

Synonym : 

 2-Hexadecyloxy-6-methyl-4H-3,1-benzoxazin-4-one;ATL-962;ATL962;2-(hexadecyloxy)-6-methyl-4H-benzo[d][1,3]oxazin-4-one

Specifications & Purity : >98.0%(HPLC)

Molecular Weight: 401.59

Melting point: 72.0 ~76.0 °C

Side Effects of Cetilistat

Cetilistat may have some major or minor side effects on your body. Such as:

  • Headache
  • Vomiting or Nausea
  • Unusual weakness or tiredness
  • Itching or rash on the skin
  • Yellow-colored skin or eyes
  • Abdominal pain or discomfort
  • Difficulty in breathing
  • Dark color urine
  • Loss of appetite

One of the common cetilistat side effects is an oily stool, increased bowel movements, excessive gas, diarrhea, and abdominal cramps. This may interfere with the absorption of fat-soluble vitamins like A, D, E, and K. 

Precautions of Cetilistat

  • It is advised to take Cetilistat as per a doctor’s prescription and based on the medical condition.
  • Some people may experience sudden bowel motions, flatulence, soft tools, stool incontinence, and runny or liquid stools. 
  • Most of the side effects of Cetilistat do not require any medical attention and gradually resolve over time. If the side effects persist, then please make sure to consult a doctor. 
  • If you have any history of allergy to Cetilistat or other medicine, ensure that you have informed the doctor about it. 
  • It is advised if you are planning for pregnancy or pregnant, avoid taking Cetilistat. It is not recommended for children below 18 years of age, as the safety and effectiveness were not established.
  • Ceitilistat may have adverse effects on the gastrointestinal system. If the patient consumes a meal with a high amount of fat, then the risk will be higher.
  • Cetilistat use is not recommended for those patients who have had an organ transplant. 
  • Due to the high risk of severe adverse effects, it is recommended that people with a history of kidney disease must not consume cetilistat.

Drug Interaction

  • Drug-Drug Interaction:

Cetilistat API may interact with blood thinner, an antidiabetic drug, thyroid medicine ( levothyroxine), medicine for heart rhythm problems( Amiodarone), anticonvulsants(lamotrigine) or HIV drug ( atazanavir)

  • Drug-food Interaction:

When taking Ceitilistat, avoid high-fat meals, including butter, meat, dark chocolate, nuts, and olive oil. Otherwise, it can increase the risk of adverse effects on the intestine and stomach. 

  • Drug-Disease Interaction:

If you have cholestasis, chronic malabsorption or thyroid disorder, kidneys or diabetes, or liver problems, ensure that you have consulted a doctor before taking Cetilistat, along with checking  API manufacturing ingredients. 

Conclusion

Active Pharma Ingredient manufacturers commonly use Cetilistat for the treatment of Obesity. Read all the precautions and usage of the medicines carefully. Make sure to consult your doctor before the consumption of Cetilistat.

FAQs

  • Is Cetilistat safe for diabetic patients?

It should be used with caution in the case of diabetic patients, as it can increase the risk of low blood sugar levels. Please inform your doctor about diabetes before taking Cetilistat so that they prescribe you some antidiabetic medicine to adjust the reaction. 

  • Can I consume Ceitilistat along with cyclosporine?

It is advised not to take Ceitilistat along with , as that can reduce the effectiveness of cyclosporine. 

  • How long should I take Cetilistat?

It is recommended to use Ceitilistat as long as your doctor has prescribed you. However, avoid taking it for more than six months. 

  • How does Ceitilisat work?

Ceitilistat inhibits the action of enzymes that break down the fat absorbed by the body. It decreases the fat from the food you eat. 

Everything You Need to Know About Ibrutinib

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Everything You Need to Know About Ibrutinib

What is Ibrutinib?

Ibrutinib is a medication that belongs to a class of drugs known as Bruton’s tyrosine kinase (BTK) inhibitors. It is used to treat specific types of cancer, such as chronic lymphocytic leukemia (CLL), Waldenström’s macroglobulinemia (WM), and mantle cell lymphoma (MCL).

Ibrutinib works by inhibiting the activity of the BTK enzyme, which is found in cancer cells and plays a role in their growth and survival. By blocking the activity of this enzyme, ibrutinib can slow or stop the growth of cancer cells. It is an FDA-approved drug and one of the most widely used BTK inhibitors in treating B-cell malignancies.

Ibrutinib API is the active pharmaceutical ingredient (API) in the medication Ibrutinib. It is a small molecule inhibitor of Bruton’s tyrosine kinase (BTK) enzyme. Ibrutinib API works by blocking the activity of the BTK enzyme, which is found in cancer cells and plays a role in their growth and survival. By inhibiting the activity of this enzyme, Ibrutinib API can slow or stop the growth of cancer cells.

Chemical structure of Ibrutinib:

The chemical structure of Ibrutinib is a small molecule that can be represented by the following chemical formula: C25H24N6O2. 

Ibrutinib API structure

 Ibrutinib class of drugs- Kinase Inhibitors

The chemical structure of Ibrutinib is composed of a nitrogen-containing ring, a quinoline group, and a pyridine group. The molecule contains two chiral centers, which can exist as a pair of enantiomers. The specific enantiomer of ibrutinib that is used in the medication is the (R)-enantiomer.

It works by binding to the active site of Bruton’s tyrosine kinase (BTK) enzyme, inhibiting its activity. This prevents the activation of the B-cell receptor signaling pathway, which is important for the survival and proliferation of B-cell cancer cells.

What are the Major Uses of Ibrutinib?

It is important to note that Ibrutinib is often blended with other medications, such as chemotherapy or immunotherapy, to maximize its effectiveness and improve patient outcomes. It is primarily used to treat certain types of blood cancer; some of the major Ibrutinib uses are:

  • Chronic lymphocytic leukemia (CLL): Ibrutinib is used as a first-line treatment for patients with CLL who have specific genetic mutations (17p deletion or TP53 mutation) and for patients with CLL who have failed previous therapy.
  • Waldenström’s macroglobulinemia (WM): Ibrutinib is used as a first-line treatment for patients with WM, a rare form of non-Hodgkin lymphoma.
  • Mantle cell lymphoma (MCL): Ibrutinib is used as a first-line treatment for patients with MCL, a type of non-Hodgkin lymphoma.
  • Marginal zone lymphoma (MZL): Ibrutinib is used to treat patients with MZL who have received at least one prior therapy.

Additionally, Ibrutinib is being studied in combination with other medications for treating other types of cancer, such as solid tumors like lung, breast, and prostate cancer. It is also being evaluated for its potential use in autoimmune disorders such as rheumatoid arthritis and systemic lupus erythematosus.

What are the Side Effects of Ibrutinib?

There are a variety of side effects of Ibrutinib, some of which can be serious. The most common Ibrutinib side effects include:

  • Fatigue: Many people experience feelings of tiredness or weakness while taking ibrutinib.
  • Diarrhea: This is a common side effect of ibrutinib and can range from mild to severe.
  • Nausea: Some people experience feelings of sickness or discomfort in the stomach while taking ibrutinib.
  • High blood pressure: Some people may develop high blood pressure while taking ibrutinib, so it’s important to check your blood pressure regularly.
  • Tumor lysis syndrome (TLS): This is a rare but serious side effect that can occur in people with large amounts of cancer cells in their bodies.
  • Heart problems: Ibrutinib can cause heart problems such as atrial fibrillation, so it’s important to let your healthcare provider know if you have any symptoms of heart problems.

It is significant to remember that everyone reacts differently to medication, and not everyone will experience these side effects. It is important to work closely with a healthcare provider to manage any side effects and monitor for any signs of serious side effects.

What are the Precautions that One Should Take While Using Ibrutinib?

Ibrutinib is a powerful medication, and it’s important to be aware of some precautions while taking it:

  • Blood clotting: Ibrutinib can increase the risk of blood clots, so it’s important to let your healthcare provider know if you have a history of blood clots.
  • Infections: Ibrutinib may increase the risk of infections, so it’s important to tell your healthcare provider if you have any symptoms of infection, such as fever, chills, or sore throat.
  • High blood pressure: Ibrutinib can cause high blood pressure, so it’s important to check your blood pressure regularly.
  • Pregnancy and breastfeeding: Women should avoid getting pregnant while taking ibrutinib, and pregnant women should not take it.
  • Interactions: Ibrutinib can interact with other medications, so it’s important to let your healthcare provider learn about all the medications you are consuming, including supplements and herbal remedies.

Who Should Not Take Ibrutinib?

Ibrutinib is not suitable for everyone, and certain groups of people should not take it:

  • Pregnant women: Ibrutinib is unsafe to take during pregnancy, and women should avoid getting pregnant.
  • Breastfeeding women: Ibrutinib is unsafe to take while breastfeeding, and women should not breastfeed.
  • People with severe kidney problems: Ibrutinib is not recommended for people with severe kidney problems as it may cause further damage.
  • People with a history of blood clots: Ibrutinib can increase the risk of blood clots, so it’s important to let your healthcare provider know if you have any medical condition of blood clots.
  • People with large amounts of cancer cells: Ibrutinib may raise the risk of tumor lysis syndrome (TLS), a serious side effect that can occur in people with large amounts of cancer cells in their bodies.

Conclusion

Ibrutinib API is typically formulated with excipients and inactive substances added to a drug to improve its stability, shelf-life, or ease of use. Once formulated, the Ibrutinib API is mixed with excipients to form the final drug product, which is then packaged and labeled for distribution and sale. There are several companies known as the best Ibrutinib active pharma ingredient manufacturers. It is important to note that this is a highly potent drug and should only be handled and used under the guidance of a qualified healthcare professional.

API’s Impact on the Cost Price of Generic Medicine

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API’s Impact on the Cost Price of Generic Medicine

Countries worldwide have various pharmaceutical pricing policies implemented to cope with the increasing drug prices. Active pharmaceutical ingredient manufacturers must follow these policies and plan their procedures further. The countries often choose the combination mechanism as it helps them determine and regulate generic medicines’ prices. Here through this blog, we will learn about API’s impact on the pricing of pharmaceutical products.

What is Pharmaceutical API?

Pharmaceutical API, or active pharmaceutical ingredient, is the active substance in a medication that is responsible for its therapeutic effect. It is the part of the drug that makes it medically active and is responsible for its intended therapeutic effect. APIs are used in both brand-name and generic medications. Still, they are generally more important in producing generic drugs because they are the key ingredient that makes the generic drug equivalent to the brand-name product.

API can be produced by chemical synthesis or can be extracted from natural sources. They can be in the form of a small molecule, a biological one, or a combination of both. The API is mixed with other inactive ingredients, such as fillers and binders, to form the finished medication. The API is usually mixed with excipients to form a final drug product. These excipients are added to improve the stability, shelf life, and ease of use of the final product.

Pharmaceutical API is a critical component of the drug development process, and its quality and purity are essential to ensure that the drug is safe and effective.

How does API impact the cost price of a generic medicine?

API, or Active Pharmaceutical Ingredient, is a key component in the production of generic drugs. The cost of the API is often a major factor in determining the overall cost of a generic medication. If the API is readily available and inexpensive, the cost of the generic drug will also be low. However, if the API is in short supply or in high demand, the generic drug cost will be higher. Additionally, if the pharmaceutical API manufacturers use expensive processes or are subject to tariffs or import restrictions, this can also increase the cost of the generic drug.

Factors Impacting the cost price of generic medicines

It is true that active pharma ingredients also play a role in determining the cost of the final product. But not alone can it alter the cost of generic medicines. There are several other factors involved that can impact the cost price of generic medicines. Here we have listed some of the major ones for your knowledge, and they are:

  • API costs: As mentioned earlier, the cost of the active pharmaceutical ingredient is a key factor in determining the cost of generic medicine.
  • Production costs: The cost of producing generic medicine, including labor, materials, and equipment, can also affect the price.
  • Competition: The level of competition in the market for a particular generic medicine can also affect the price.
  • Patent expiration: The expiration of patents on brand-name drugs can open the door for generic manufacturers to produce and sell the drug, leading to increased competition and lower prices.
  • Government regulations: Government regulations and policies can also impact the cost of generic medicines. For example, some countries have price controls in place that can affect the cost of drugs. Or The cost of taxes and tariffs that may be imposed on medicine by the government in certain regions.
  • Research and Development (R&D) Costs: This includes the cost of researching and developing new drugs, including conducting clinical trials and obtaining regulatory approvals.
  • Marketing and Distribution costs: The cost of promoting and distributing the medicine, including advertising, sales and promotion, and logistics.
  • Profit Margin: The profit that the company expects to make from the sale of the medicine.
  • Quality and compliance cost: The cost of meeting the quality standards and compliance with international regulations for the production of the medicine.
  • Price negotiations with payers: The cost of negotiation with the insurance companies, pharmacy benefit managers (PBMs), and other payers that determine the final price of the drug.

Import and export tariffs can also affect the cost of the API and the final product. The final cost of a medicine is influenced by all these factors and can vary widely depending on the specific drug and the market conditions. 

Conclusion

The pharmaceutical industry is huge, and so there are many other parameters that can affect the price of generic medicines. The API manufacturers do not generally disclose their research and development costs. Instead, they choose to cite the hypothetical average costs for drug development based on self-reported data. Before the consumers have it in their hands, the medicine has to cross multiple stages. Advanced technologies are also being used within the production process, and it also impacts the cost of generic medicines. 

Niraparib: Everything You Need to Know About The Drug

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Niraparib: Everything You Need to Know About The Drug

What is Niraparib?

Niraparib is a medication used to treat certain types of ovarian, fallopian tube, and primary peritoneal cancer. PARP inhibitors are the class of drugs for Niraparib. It works by blocking an enzyme called PARP, which repairs DNA damage. By blocking PARP, Niraparib causes cancer cells to die. 

It’s important to mention that the production of Niraparib API must comply with the regulations of each country, the WHO, and the FDA, among others, to guarantee the API’s quality, efficacy, and safety.

Niraparib API is then formulated into a finished dosage form, such as tablets or capsules, for patient distribution and use. The finished dosage form may include other ingredients such as fillers, binders, and coatings.

Niraparib is chemically known as:-

(S)-N-(3-((3-aminopyridine-2-carbonyl)amino)phenyl)-3-((4-(4-chloro-3-(trifluoromethyl)phenyl)-1,2,4-triazol-1-yl)methyl)benzamide. It can be recognized as a white to off-white powder, which is soluble in methanol and ethanol, and slightly soluble in water.

Niraparib formula

Formula: C19H20N4O

ChEMBL Id: 1094636

ChemSpider ID: 24531930

Pronunciation: /nɪˈræpərɪb/; nih-RAP-uh-rib

Protein binding: 83%

Other names: MK-4827

Metabolism: Carboxylesterases

Some Significant Niraparib Uses

Niraparib API is approved as a maintenance treatment for adult patients suffering from epithelial ovarian, fallopian tube, or primary peritoneal cancer. Patients with an incomplete or partial response to platinum-based chemotherapy are also prescribed this drug. Some other major uses of Niraparib are:

  • Maintenance treatment of adult patients who are suffering from deleterious or suspected deleterious germline BRCA-mutated (gBRCAm) recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who have been treated with three or more prior lines of chemotherapy.
  • It can be used to treat adult patients with relapsed small cell carcinoma of the ovary, hypercalcemic type (SCCOHT), who have received at least two prior lines of therapy.

What are the Major Niraparib Side Effects?

It is important to note that Niraparib treatment should always be taken under the supervision of a qualified oncologist. The physician will evaluate the benefits and risks of the treatment for each patient and will monitor the patient’s response to the treatment, and adjust the dosage accordingly. But, like all medications, it can cause side effects. Some common side effects of Niraparib include:

  • Nausea
  • Fatigue
  • Anemia
  • Thrombocytopenia (low platelet count)
  • Vomiting
  • Diarrhea
  • Constipation
  • Loss of appetite
  • Headache

More serious side effects of Niraparib include:

  • Blood clots
  • Severe bleeding
  • Myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML)
  • Tumor lysis syndrome (TLS)
  • Embryo-fetal toxicity

 If you experience any kind of side effects while taking Niraparib, it is crucial to inform your healthcare provider. They might adjust your dosage or recommend ways to manage the side effects.

Precautions of Niraparib that You Should be Aware Of

Niraparib is a medication used to treat certain types of ovarian, fallopian tube, and primary peritoneal cancer. It is important to take certain precautions when using Niraparib. Some precautions to be aware of include the following:

  • Blood clotting: Niraparib may increase the risk of blood clots. Your healthcare provider may monitor your blood clotting function more frequently while taking Niraparib.
  • Bleeding: Niraparib may increase the risk of bleeding. Your healthcare provider may monitor your blood clotting function more frequently while taking Niraparib and may recommend measures to reduce the risk of bleeding.
  • Myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML): Niraparib can cause MDS and AML. Your healthcare provider will monitor your blood counts while taking Niraparib, and you may discontinue the medication if these conditions develop.
  • Tumor lysis syndrome (TLS): Niraparib can cause TLS. Your healthcare provider will monitor you for the signs and symptoms of TLS and may take measures to prevent or treat the condition.
  • Pregnancy and breastfeeding: Niraparib can cause harm to a developing fetus. Women who have reproductive potential should use effective contraception during their treatment and should continue for at least six months after the last dose of Niraparib. Women should not breastfeed while taking Niraparib.
  • Interactions with other medications: Certain medications may interact with Niraparib, so it is significant to give information about all medications, vitamins, and supplements you are currently taking before starting Niraparib treatment with your healthcare provider of 

Who Should Not Take Niraparib?

There are certain individuals who should not take Niraparib or who should use it with caution. These include:

  • Individuals who are pregnant or planning to become pregnant, Niraparib can cause harm to a developing fetus.
  • Individuals who are breastfeeding, such as Niraparib, may pass into breast milk and may cause harm to a nursing infant.
  • Individuals with a history of blood clots or bleeding disorders, such as Niraparib, may increase the risk of blood clots and bleeding.
  • Individuals taking other medications may have a higher risk of bleeding, such as warfarin or aspirin.
  • Individuals who have or had bone marrow disorders such as Niraparib can cause Myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML)
  • Individuals who have or had tumor lysis syndrome (TLS)
  • Individuals who are allergic to Niraparib or any of its ingredients.

How does Niraparib work to Treat Different Types of Cancer?

Niraparib works by inhibiting the activity of an enzyme called poly(ADP-ribose) polymerase (PARP), which is involved in repairing DNA damage in cells. When PARP is inhibited, the cancer cells are unable to repair their DNA and eventually die. This mechanism of action is particularly effective in cancer cells with mutations in genes involved in DNA repair, such as BRCA1 and BRCA2.

DNA of Cancer cells often has, which makes them more dependent on PARP for survival. By inhibiting PARP, Niraparib causes cancer cells to die, while leaving normal cells relatively unharmed.

In the case of BRCA-mutated cancer, the BRCA1 and BRCA2 genes are responsible for the repair of DNA double-strand breaks. When these genes are mutated, the cells are unable to repair the DNA damage properly, so the PARP inhibitors like Niraparib can take advantage of this vulnerability and cause cancer cell death.

Conclusion

Niraparib active pharma ingredient typically use synthetic chemical processes. The raw materials used in the synthesis of Niraparib include various chemicals such as amino acids, organic acids, and solvents. These raw materials are combined and reacted in a series of steps to produce the final API.

Talking to your healthcare provider is vital before starting Niraparib treatment, especially if you have a history of blood clots or bleeding disorders or in case you are on any other medications that may increase the risk of bleeding.

Linagliptin: Uses, Side Effects, and Precautions

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Linagliptin: Uses, Side Effects, and Precautions

What is Linagliptin?

Linagliptin is an active pharmaceutical ingredient (API), and it is a medication that lowers blood sugar levels and helps in treating type 2 diabetes. Dipeptidyl peptidase-4 (DPP-4) inhibitors are the class of drugs that Linagliptin belongs to. The API is the substance in a medication that is responsible for its therapeutic effects.

Linagliptin is chemically known as:-

(S)-3-[(3S)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6-dihydro-2H-pyridazin-3-one. It can be recognized as a white to off-white powder, which is soluble in methanol and ethanol and slightly soluble in water.

Molar mass: 472.54 g/mol

Formula: C25H26N8O2

Boiling point: 661.2 °C

ChEMBL Id: 237500

ChemSpider ID: 8271879

IUPHAR ID: 6318

Other names: BI-1356

What are Major Linagliptin Uses?

Linagliptin is used to improve blood sugar control in adults with type 2 diabetes, either alone or in combination with other diabetes medications such as metformin, sulfonylureas, or thiazolidinediones. Usually, it is prescribed to be taken once daily with or without food. It works by inhibiting the activity of an enzyme called dipeptidyl peptidase-4 (DPP-4), which results in an increase in the levels of incretin hormones. These hormones help regulate the amount of insulin released by the pancreas in response to blood sugar levels.

Linagliptin is not recommended for use in people with type 1 diabetes or in those with diabetic ketoacidosis, a serious condition in which Ketones are formed. These are high levels of blood acids that the body produces. It is also not advised for use in people with severe kidney or liver impairment.

The safety and effectiveness of linagliptin have been established in clinical trials, and it is considered an effective treatment for type 2 diabetes. However, as with all medications, it is important to discuss the potential risks and benefits with a healthcare provider before starting treatment.

Some Major Linagliptin Side Effects

Linagliptin is generally well-tolerated, but like all medications, few side effects can be cited in some people. Common side effects of linagliptin include:

  • Upper respiratory tract infections such as the common cold, sinusitis, and pharyngitis
  • Nasopharyngitis (inflammation of the nose and throat)
  • Stuffy or runny nose
  • Sore throat
  • Headache
  • Back pain
  • Diarrhea
  • Nausea

In rare cases, more serious side effects can occur, such as:

  • Allergic reactions (itchiness, rash, hives, swelling of the face, lips, tongue, or throat, difficulty breathing)
  • Pancreatitis (severe pain in the upper abdomen, nausea, vomiting)
  • Liver problems (yellowing of the skin or eyes, dark urine, abdominal pain)
  • Hypoglycemia (low blood sugar)
  • Urinary tract infection

It is crucial to talk to your healthcare provider about any side effects you experience and report to your doctor if you have any history of liver or pancreatic disease before taking linagliptin.

Precautions One Should Take Before Consuming Linagliptin

Linagliptin is a medication that should be used with caution in certain individuals and under certain conditions. Some precautions to be aware of before taking linagliptin include:

  • Any history of pancreatitis must be discussed with your healthcare provider, as there is a risk of it being triggered by the use of linagliptin.
  • If you have liver problems, then you need to inform your healthcare provider. As they may need to monitor your liver function more frequently while you are taking linagliptin.
  • If you have kidney problems, then you need to inform your healthcare provider. As they may need to adjust your dosage of linagliptin or may recommend a different medication.
  • If you are pregnant or planning to have a baby, it is important to discuss the potential risks and benefits of taking linagliptin with your healthcare provider.
  • If you are breastfeeding, it is not known if linagliptin passes into breast milk. So, it is important to discuss with your healthcare provider about the potential risks and benefits of taking linagliptin while breastfeeding.

It is important to provide your healthcare provider with a list of all medications, vitamins, and supplements you are currently taking, so they can determine if linagliptin is safe and appropriate for you to take.

Who Should Not Take Linagliptin?

There are certain individuals who should not take linagliptin or who should use it with caution. These include:

  • For individuals with type 1 diabetes, linagliptin is not indicated for this condition.
  • For individuals with diabetic ketoacidosis, linagliptin is not indicated for this condition.
  • Individuals with a history of pancreatitis, as linagliptin may increase the risk of pancreatitis.
  • Individuals with severe renal impairment, as the safety and efficacy of linagliptin have not been established in this population.
  • Individuals who are allergic to linagliptin or any of its ingredients.
  • Individuals who are taking medications that interact with linagliptin, such as gemfibrozil, may increase the risk of side effects.

It is significant to inform your healthcare provider before taking linagliptin if you have any of these conditions or are taking any of these medications. Your healthcare provider may need to adjust your dosage or recommend a different medication if you are unable to take linagliptin.

How does Linagliptin work as Medicine to Treat Type 2 Diabetes?

Linagliptin works by inhibiting the activity of the enzyme dipeptidyl peptidase-4 (DPP-4). DPP-4 is an enzyme that breaks down incretin hormones, such as GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic peptide), which are produced by the gut and play a key role in regulating glucose metabolism.

By inhibiting DPP-4, linagliptin increases the levels of incretin hormones in the body, which leads to an increase in insulin secretion and a decrease in glucagon secretion. It helps to improve glucose metabolism in people with type 2 diabetes and also lowers their blood sugar levels.

Linagliptin also has another mechanism of action which is to slow down the absorption of glucose in the gut by inhibiting the SGLT1 transporter.

Linagliptin is usually taken once daily, and the dosage may be adjusted based on the individual’s response to treatment and blood sugar levels. It is typically used in combination with diet and exercise and can be used alone or in combination with other diabetes medications such as metformin or sulfonylurea.

Conclusion

Linagliptin is typically manufactured using synthetic chemical processes. The raw materials used in the synthesis of linagliptin include various chemicals such as amino acids, organic acids, and solvents. These raw materials are combined and reacted in a series of steps to produce the final API. There are various Linagliptin active pharma ingredient manufacturers.

It’s important to mention that the production of linagliptin API must comply with the regulations of each country, the WHO, and the FDA, among others, to guarantee the quality, efficacy, and safety of the API.

Viral Hepatitis: Everything You Need to Know

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Viral Hepatitis: Everything You Need to Know

What is Viral Hepatitis?

Several viruses are known to cause Hepatitis, which refers to liver inflammation. You can lower the risk of getting Hepatitis by avoiding risky behaviors like unprotected sex, frequently drinking alcohol, and sharing needles.

Hepatitis refers to the inflammation of the liver. It is a tissue reaction to irritation or any injury that generally results in swelling and can also cause pain. 

There are many reasons for Hepatitis. The virus causes viral Hepatitis, which can be either chronic or acute. Viral Hepatitis may spread through sexual contact as well. 

There are five known Hepatitis that are categorized. Several viruses are now known to cause Hepatitis. The common form of viral Hepatitis include; 

Hepatitis A

According to the Centers for Disease Control and Prevention, there were about 2007 acute hepatitis A infections in the U.S. This form of Hepatitis has no complications and does not lead to any chronic infection. The liver generally heals from Hepatitis A within several months. However, you may observe occasional fatality from hepatitis A, which has occurred due to liver failure, and some people have required a liver transplant for the acute 

Hepatitis B

In 2017, around 22,000 new hepatitis B occurred, and around 90,0000 people are living with this disease in the U.S. The earlier hepatitis B is contracted, the more likely to become chronic. People may carry the virus without feeling sick, but still, the virus can spread. Hepatitis B can be prevented by getting vaccinated. 

Hepatitis C

About 85% of patients with hepatitis C develop chronic liver infections. About 2.4 million people in the U.S. are estimated to have this infection. This is one of the most common reasons behind liver disease in the U.S. and the number one reason behind liver transplants. 

Hepatitis D

Hepatitis D only happens to those infected by the hepatitis B virus. If you have been vaccinated against hepatitis B, you will be protected against hepatitis D. 

Hepatitis E

Healthcare providers may be unable to identify virus-causing Hepatitis as one of these. Other viruses like EBV, CMV, and HSV can also cause Hepatitis. 

Most people recover from Hepatitis, and the disease is often preventable as well. However, this is still considered a serious health risk because that can:

  • Destroy the tissue of the liver
  • Spread easily from one person to another
  • Weaken the immune system of the body
  • Cause liver failure
  • Cause liver cancer
  • Cause death. 

How Does Hepatitis Spread?

  • There can be many factors through which you can become infected with Hepatitis. It can happen through exposure to blood and body fluids like the semen of an infected person. 
  • Hepatitis can also spread by having unprotected sex, sharing or use of dirty needles for piercing, tattoos, and drug use. 
  • Being born to a pregnant woman with the infection, being bitten by someone with the infection, being treated medically who does not use sterile instruments, and sharing everyday items that include razors, toothbrushes, and piercing jewelry can all be the reason behind the Hepatitis infection. 
  • You may only get hepatitis D, in case you have hepatitis B.
  • In many cases, hepatitis E can be dangerous and even fatal in pregnant people. 

Apart from all these, there are a lot of myths regarding the spreading of Hepatitis. It does not spread by breastfeeding, coughing and sneezing, eating food that someone with the infection has prepared, kissing on the cheek or lips, hugging, shaking hands, or holding hands.

Symptoms of Viral Hepatitis

Symptoms of Hepatitis B can be intense or minor. There are cases where people are affected, but they never feel sick. Symptoms of Viral Hepatitis B may include:

  • Loose stool.
  • Loss of appetite.
  • Stomach pain.
  • Constipation.
  • Having yellow skin.
  • Mild fever or eyes.
  • Being sick to your stomach.

More than 90% of the people who get hepatitis B in their adult stage recover from their symptoms. 

  • Healthcare providers and first responders, people on dialysis, people living in close quarters with a person with chronic hepatitis B, and children’s mothers who have been infected with hepatitis B.
  • People who have unprotected sex or have been diagnosed with a sexually transmitted disease are likely to get infected by this virus.
  • People living with or working in an institutional setting such as group homes or prisons carry a high risk of getting hepatitis B.

Diagnosis

There are various ways to diagnose HBV infection, including abdominal ultrasound, liver biopsy, and blood tests. An ultrasound uses sound waves to show the size and shape of your liver and blood circulation through it. A small tissue sample is removed through a tiny incision in a liver biopsy and sent to the lab for analysis. Tests of blood plasma or serum show the response of your immunity to the virus. Tenofovir Alafenamide by leading API manufacturers fumarate is used to treat chronic Hepatitis B infection. 

Treatment of Viral Hepatitis

  • There is no such infallible treatment to cure hepatitis A, apart from carefully monitoring the liver function. If you know you have Hepatitis A earlier, you may e able to stop the infection if you get the dose of the Hepatitis A vaccine called Hepatitis A immune globulin. 
  • Hepatitis B can be treated successfully, and generally used drugs by active pharmaceutical ingredient manufacturers for the treatment of chronic hepatitis B are:
  1. Entecavir
  2. Tenofovir alafenamide
  3. Interferon alfa-2b
  4. Peginterferon alfa-2a
  • For Hepatitis C, the following drugs can be used:
  1. Daclatasvir dihydrochloride
  2. Simeprevir
  3. Sofosbuvir
  4. Elbasvir
  5. Piberntasvir

All these drugs are sometimes given with older drugs like peginterferon alfa-2a, peginterferon-2b, and ribavirin. You may have to take all these medicines for some time, even as long as six months.

If you have chronic hepatitis D, the doctor may prescribe drugs or active pharma ingredients with the interferons and add medicines for hepatitis B. 

Conclusion

The severity of Hepatitis can cause serious illness and lead to the person’s death. So you need to go for a check-up and take medicines accordingly. Active pharma ingredients manufacturers take care of that.

Can Psoriasis be Cured?

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Can Psoriasis be Cured?

It is said that the condition of Psoriasis cannot be cured but can be treated by managing the symptoms to reduce its effect on your life. No need to be afraid, as there are treatments that can help manage this disease. This blog will let you explore every vital aspect that Psoriasis holds and should be known to you. We will also discuss Apremilast API, which can help limit the spread of Psoriasis in the patient’s body. But first things first.

What is Psoriasis?

Psoriasis is a chronic inflammatory skin disease that is caused due to rash with itchy and scaly patches. It is most commonly found on the knees, scalp, elbows, and trunk. Psoriasis is a disease that is said to be caused by the dysfunction of the immune system or immune-mediated disease. It occurs due to the skill cell growth, which speeds up by the overactive immune system. 

Normally when we talk about skin cells, they grow and then fall off in a month. But with Psoriasis, the skin cells, instead of shedding, start piling up on the skin’s surface. Scales and plaque might appear on the body of some people, and one out of three people diagnosed with psoriasis also develop psoriatic arthritis. 

Major Signs and  Symptoms of Psoriasis

Symptoms of Psoriasis often start between the age of 15 and 25, and people belonging to any gender and having any skin color can get affected by this disease. Let us discuss the common signs and symptoms of Psoriasis:

  • Small scaling spots can be seen on the skin but are commonly seen in children.
  • Itching, burning sensation, or soreness can be seen along with dry and cracked skin, which even may bleed in some cases.
  • A patchy rash is observed, and its appearance varies from person to person. It might look like a spot of dandruff scaling to form a major eruption over the entire body. 
  • The colour of the rash again varies as per the skin colour of the affected person. It can be purple with a grayscale or pink or red with a silver scale. 

Types of Psoriasis

The signs and symptoms of Psoriasis also differ as per its type. Here we will be offering you insight into the kind of Psoriasis, and they are:

Erythrodermic Psoriasis

It is one of the rare types of Psoriasis and affects only two percent of people with Psoriasis. It is a type that causes discolouration or intense redness in the skin. People with Erythrodermic Psoriasis often shed layers of their skin like large sheets. 

Erythrodermic Psoriasis can be life-threatening as it affects the entire body. One symptom of this type of Psoriasis is the affected person’s heart rate and body temperature change. The affected person may feel dehydrated and face severe pain along with itching. 

Guttate Psoriasis

It is found that around 8% of people affected by Psoriasis may have Guttate Psoriasis. Although Guttate Psoriasis affects any body area, this type commonly appears on the torso, legs, and arms. Some of the signs and symptoms of Guttate Psoriasis is that it includes discoloured spots, which are caused due to inflammation. In this type of Psoriasis, small, round, and red-coloured spots can also be seen. 

Inverse Psoriasis

It is said that one-quarter of the people who have Psoriasis are affected by Inverse Psoriasis. This type of Psoriasis affects the skin folds within the body, such as under the breasts, genital areas, buttocks, and underarms. Some of the vital signs and symptoms of this Psoriasis type are that it darkens or changes the skin to deep red, and its texture does not remain smooth or scaly. People affected by Inverse Psoriasis can experience severe itching and pain. 

How do you Stop Psoriasis from Spreading?

As per the researchers, anyone can develop the condition of Psoriasis. It is not mandatory to have a family history of this disease. The combination of environmental triggers and genetics is likely to cause Psoriasis. Following are the factors which can flare up the condition of Psoriasis:

  • Obesity
  • Deficiency of Vitamin D
  • Anybody infection
  • Smoking and consuming too much alcohol
  • Stress and any skin injury

The treatment of Psoriasis can include different medications that help reduce the effect of this condition. Many API manufacturers offer Apremilast API, a strong chemical substance for preparing medicine for Psoriasis. But the affected person also needs to follow steps to prevent the spread of Psoriasis. Some of the important tips are:

Nutrient-Dense Diet

Consuming a nutrient-dense diet can help in reducing the spreading of Psoriasis. Eating and avoiding some specific types of food can help reduce the flare-up of the Psoriasis condition.

As per the research, it is found that the people reported improvement in their condition after reducing the intake of gluten, alcohol, eggplants, potatoes, tomatoes, and some other items. Progress was also recorded when the people with the Psoriasis condition were consuming fish oil and omega-3s, vitamin D supplements, and vegetables in their diet. 

Protecting Skin

Any skin-related infection, cuts, sunburn, and even some vaccinations can also trigger the condition of Psoriasis. If the skin goes under any trauma, it can cause the Koebner phenomenon. In this, the patches of Psoriasis are seen developing in the area where a person does not experience the flare-up. 

Get Enough Sleep

A healthy sleep schedule can support and boost the body’s immune system. It is one of the best ways to help maintain a good lifestyle and manage stress. All of these factors are considered vital to avoid the spreading of Psoriasis. 

Can Psoriasis be Cured Permanently?

No, the condition of Psoriasis can not be cured permanently, but it can be controlled from spreading. Several treatment options can relieve the symptoms of Psoriasis, including Aprimilast API. Some other creams, lotions, and medicated shampoos can improve the rash that has affected a small portion of your skin. But if you have an inflammation that has affected a larger area or are experiencing joint pain, you would need to check for Psoriasis arthritis. It is the Psoriasis condition under which the patients suffer from joint pain and face redness or itchiness on their skin. 

Apremilast: Medicine to Treat Psoriasis

One of the most efficacious drugs used for Psoriasis is Apremilast. It is commonly sold under Otezla and is considered one of the best medications for treating Psoriasis arthritis. This drug is a mixture of isomers, and phosphodiesterase 4 (PDE4) is also one of its inhibitors. If the patient does not respond to their other medications or is found allergic to them, then Apremilast is offered. 

Apremilast contains special chemical blockers, which are useful for reducing the effect of Psoriasis arthritis. PDE4 is the cell responsible for the inflammation caused due to Psoriasis, and apremilast can block the activities driven by this cell. 

API manufacturing companies offer Aprimilast API to the companies for the preparation of Psoriasis medicine. 

The chemical structure of Apremilast API is as follows:

Some of the other vital details about the Apremilast API are:

Chemical Formula: C22H24N2O7S

Weight: 460.5

CAS Number: 608141-41-9

InChI Key: IMOZEMNVLZVGJZ-QGZVFWFLSA-N

IUPAC Name: N-{2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide

SMILES: CCOC1=CC(=CC=C1OC)[C@@H](CS(C)(=O)=O)N1C(=O)C2=CC=CC(NC(C)=O)=C2C1=O

Conclusion

Yes, there is no permanent cure for Psoriasis, but multiple medications are available that can prevent the condition of Psoriasis. No, this disease is not contagious, and treatment for the same can improve the symptoms. Even therapies are available if medication is not working, but the best is maintaining a healthy lifestyle. The best medicine way is to get Apremilast API from a reliable API manufacturing company to prepare the medicine for Psoriasis. 

That’s where Bulat Pharmaceutical come into play!

With over a decade-long experience in offering quality API, intermediates, and other formulations, we have been amongst the top pharma raw materials provider across the globe. Many leading pharma companies have partnered with us to source quality raw materials to develop their pharma products. We offer a fully checked and quality-controlled API that ensures effective drug development. You can connect with us today to learn more about us or to begin your drug development journey.

Ledipasvir: Uses, Side Effects, and Precautions

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Ledipasvir: Uses, Side Effects, and Precautions

What is Ledipasvir?

Ledipasvir, also sold under the common name of Harvoni, is an antiviral medicine used to treat certain types of Hepatitis C disease and liver malfunctioning in adults and children aged three years and above. Ledipasvir API is generally used in combination with Sofosbuvir as an antiviral medicine. 

Sofosbuvir falls under the medication category called nucleotide polymerase inhibitors that reduces the growth of the Hepatitis C virus inside the human body. On the other hand, Ledipasvir falls under the category of medication called HCV NS5A inhibitors, which prevent the growth of Hepatitis C from spreading in the body. 

Here’s the chemical structure of ledipasvir API:

The other chemical details of ledipasvir API are as follows:

Chemical Formula: C49H54F2N8O6

Molar Mass: 888.99 

CAS Number: 1256388-51-8

InChI Key: VRTWBAAJJOHBQU-KMWAZVGDSA-N

IUPAC Name: methyl N-[(2S)-1-[(6S)-6-[5-[9,9-difluoro-7-[2-[(1R,3S,4S)-2-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]-2-azabicyclo[2.2.1]heptan-3-yl]-3H-benzimidazol-5-yl]fluoren-2-yl]-1H-imidazol-2-yl]-5-azaspiro[2.4]heptan-5-yl]-3-methyl-1-oxobutan-2-yl]carbamate

SMILES: COC(=O)N[C@@H](C(C)C)C(=O)N1CC2(CC2)C[C@H]1C3=NC=C(N3)C4=CC=C5C(=C4)C(F)(F)C6=C5C=CC(=C6)C7=CC8=C(C=C7)N=C(N8)[C@@H]9[C@H]%10CC[C@H](C%10)N9C(=O)[C@@H](NC(=O)OC)C(C)C

What are the Most Common Uses of Ledipasvir?

There are multiple uses of Ledipasvir API:

  • Ledipasvir and Sofosbuvir tablets are used to treat the Hepatitis C virus in adults and children above three years. 
  • Ledipasvir can also be used as a combination therapy to treat chronic Hepatitis C, an infectious condition caused by the Hepatitis C virus. 

Organizations and Clinical Trials of Ledipasvir

124 organizations clinically tested Ledipasvir API for research and development purposes. However, one organization also tested it for marketing purposes. The trials were conducted in four stages, and a total of 1123 trials were conducted to test ledipasvir API for medicinal purposes. 

Clinical trial data

A few organizations that took part in those trials were:

  • Gilead Sciences
  • Jhonson & Jhonson
  • Genuine Research Centre, Egypt

Indications of Ledipasvir

There are two approved indications of Ledipasvir API:

  • Hepatitis C
  • Hepatitis C, Chronic

There are 27 experimental indications of the ledipasvir API as concluded in the four trials:

  • beta-Thalassemia (Phase 4)
  • Carcinoma, Hepatocellular (Phase 4)
  • COVID-19 (Phase 4)
  • Cryoglobulinemia (Phase 2/Phase 3)
  • Fibrosis (Phase 4)
  • Gaucher Disease (Phase 4)
  • Healthy Volunteers (Phase 1)
  • Heart Failure (Phase 4)
  • Hematologic Neoplasms (Phase 1/Phase 2)
  • Hematopoietic Stem Cell Transplantation (Phase 4)
  • Hepacivirus (Phase 3)
  • Hepatitis (Phase 1)
  • Hepatitis B (Phase 3)
  • Hepatitis C ()
  • Hepatitis C, Chronic ()
  • HIV (Phase 4)
  • HIV Infections (Phase 4)
  • Insulin Resistance (Phase 4)
  • Liver Cirrhosis (Phase 3)
  • Liver Diseases (Phase 4)
  • Lung Diseases, Interstitial (Phase 4)
  • Lymphoma (Phase 2)
  • Lymphoma, B-Cell (Phase 2)
  • Porphyria Cutanea Tarda (Phase 2)
  • Pregnancy (Phase 1)
  • Pulmonary Disease, Chronic Obstructive (Phase 4)
  • Substance Abuse, Intravenous (Phase 3)

Read Also: Everything You Need to Know about Apremilast

Safety and Hazards for Ledipasvir and Sofosbuvir API

Pictogram(s): Health Hazard

Signal: Warning

GHS Hazard Statements: H371 (100%)

Precautionary Statement Codes: P260, P264, P270, P308+P316, P405, and P501

Pharmacology of Ledipasvir

Mechanism of Action: Non-structural Protein 5A Inhibitor

Black Box: No  

Pro Drug: No

ALogP: 8.61

Delivery Methods: Oral

Protein Building: >99.8%

Half-life: 47 hours

Common Side Effects of Ledipasvir

Although ledipasvir API has many excellent benefits in treating Hepatitis C disease, some common side effects are seen with some patients taking this medication. To name a few, we have:

  • tiredness
  • headache
  • difficulty falling asleep or staying asleep
  • Nausea
  • diarrhea

Who Should Not Take Ledipasvir?

Ledipasvir and Sofosbuvir API have shown tremendous effects in treating Hepatitis C conditions in adults. However, there are some limitations to the people consuming this medicine. 

  • Patients allergic to Sofosbuvir and Ledipasvir must not use this medicine
  • Women who are pregnant, planning to become pregnant, or are breastfeeding must consult with their doctors before taking Ledipasvir. 
  • Patients who are on dialysis, have HIV, or have had a liver transplant must consult their doctors before using Ledipasvir medicine. 

How to Store and Dispose of Ledipasvir?

Ledipasvir should always be stored in an air-tight container and out of reach of children. You should also store ledipasvir API at room temperature, away from light, and free from excess moisture.

Since this medicine is highly active, it should also be disposed of in special conditions. You must never throw away unused drugs in the toilet or water bodies. Instead, you must follow the medicine take-back program to dispose of the remaining medicine. You can check the FDA’s Safe Disposal of Medicine website to learn more about the medicine take-back program. 

Conclusion

API manufacturers commonly use Ledipasvir API to create medicine for treating Hepatitis C conditions. Ledipasvir API is used with Sofosbuvir to cure adults and children above three years. The medicine has a molar mass of 888.99 and is sold by the name Harvoni.

Ledipasvir API was clinically tested in four phases, and 124 organizations participated in those trials. The most common side effects experienced by the patients consuming Ledipasvir and Sofosbuvir are headache, tiredness, and cough. Sometimes, rashes can also be seen in some patients. People who are allergic or pregnant must limit themselves from consuming Ledipasvir drugs. 

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