Tofacitinib – Everything You Need to Know

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Tofacitinib

What is Tofacitinib?

Tofacitinib is a prescribed medication called the Janus Kinase inhibitor. It acts as an immune suppressor, which comes in the list of disease-modifying anti-rheumatic drugs. It is available as a tablet, extended-release tablet, and oral solution. 

Tofacitinib treats a few inflammatory conditions in people who have already tried tumor necrosis factor blockers.  

History 

The Food and Drug Administration approved Tofacitinib in 2012; the JAK inhibitor approved it for treating rheumatoid Arthritis. 

In over a decade, it is the first oral DMARD to get approval for the condition. 

API Information 

Tofacitinib is the cell-permeable Janus KInase inhibitor with the preference to inhibit JAK1 and JAK3. It inhibits JAK isoforms 1,2 and 3 with IC50. According to research, Tofactinib primarily blocks cytokine receptors and inhibits the production of cytokine. The overall impact of tofacitinib is to reduce inflammatory response through the selective inhibition of the JAK family. 

This drug is used to treat moderate to severe rheumatoid arthritis, psoriatic arthritis, and inflammatory bowel disease. Tofacitinib is associated with transient and usually mid-elevations in serum aminotransferase levels during the therapy. 

Tofacitinib is the pyrrolopyrimidine which is pyrrole ( 2,3-d) pyrimidine replaced at position 4 by an N-methyl, N ( 1- cyanocetyl-4-methylpiperidin-3-yl) amino moiety. This has a role as an EC 2.7.20.2 inhibitor, and it is an antirheumatic drug. Tofacitinib is a pyrrolopyrimidine, a nitrile, and a tertiary amino compound. 

Product Usuage Information 

Tofactinib is supplied as the lyophilized powder. The length of the treatment and working concentratiins may vary depending up on the desired effect, but that is typically ised at 5-500 nM for 1-72hr. 

Product Description 

Molecular Weight 312.37 g/mol
Purity 99%
Molecular FormulaC16H20N6O
CAS936487-63-7
SolubilitySoluble in DMSO and EtOH at 100mg/ml

Clinical uses of Tofacitinib

  • Tofacitinib comes in the form of tablets, and the Tofacitinib XR is used to treat adults with moderate to severely active rheumatoid Arthritis. During the treatment of Arthritis, one or more medicines, called TNF blockers, have already been used. In Rheumatoid Arthritis and Psoriatic Arthritis, Tofacitinib helps reduce the inflammation in joints and improve their function. In ulcerative colitis, it helps curb the inflammation in the colon & rectum, thus helping with diarrhea & abdominal pain that comes with the disease.  
  • These tablets are used to treat adults with Psoriatic Arthritis and have shown promising results. In earlier research, TNF Blockers were used, which did not work well and had serious side effects. 
  • It can also be used to treat adults with active Ankylosing Spondylitis. Tofacitinib helps in reducing inflammation in certain parts of the spine. 
  • Tofacitinib can be used for children two years older or more than that with active polyarticular course juvenile arthritis.

Market Scenario of Tofacitinib

It’s important to note that the market environment for tofacitinib has changed over time as a result of a variety of variables, such as regulatory adjustments and safety worries. Using greater dosages of tofacitinib is associated with an increased risk of significant heart-related events, cancer, and blood clots, according to a safety communication sent by the U.S. Food and Drug Administration (FDA) in February 2021. As a result, the FDA demanded changes to the prescribing instructions and issued a Boxed Warning for tofacitinib, which is the agency’s most conspicuous warning. The market dynamics for tofacitinib may be impacted by this regulatory decision.

The availability of alternative therapy choices, such as other JAK inhibitors, biologic medicines, and non-pharmacological interventions, may also impact the market for tofacitinib. Pricing and reimbursement can all have an impact.

Side Effects of Tofacitinib

Tofacitinib can have some serious impacts on your body, including:

  • Infections

Tofacitinib can affect the immune system by lowering its ability to fight infections. People may experience serious infections when taking Tofacitinib, including Tuberculosis and infections caused by fungi, bacteria, or viruses, which can spread throughout the body. Some people have faced fatal consequences due to the drug as well. 

The healthcare provider must test you for TB before starting the Tofactinib and during treatment. They can also closely monitor your health condition and the symptoms of TB infection during the treatment with Tofacitinib.

If you have any kind of infection, it would be better not to take Tofacitinib. There is a high chance that you may develop the risk of herpes zoster (HZ). 

Before you start taking Tofacitinib, make sure to consult your healthcare provider and tell them if you have the following:

  1. Cough
  2. Fever, Sweating, or chills.
  3. Blood in Phlegm
  4. Warm, red, or painful sores
  5. Muscle ache
  6. Shortness of breath
  7. Weight loss
  8. Stomach pain or diarrhea
  9. Feeling fatigued
  10. Being treated for any infection
  11. Got a lot of infections or infections which keep coming back.
  12. Have TB or have been in the close contact with someone who has TB.
  13. Have or had Hepatitis B or C.
  • It increases the risk of death in people over 50 years of age and with at least one heart disease risk factor.
  • It may increase the risk of certain cancers by changing how the immune system works. 
  • Intake of Tofacitinib increases the risk of major cardiovascular events such as stroke, death, and heart attack in people above 50. 

Get emergency help immediately if you have any symptoms of the heart attack or a stroke when you start taking Tofacitinib, including.

  • Nausea or vomiting
  • Breaking out in a cold sweat
  • Discomfort or pain in the arms, back, jaw, or stomach. 
  • Feeling lightheaded
  • Weakness in one part or on the other side of the body.
  • Slurred speech. 
  • Discomfort in the chest can last more than a few minutes. 
  • Tears in the stomach or the intestines. 
  • An allergic response such as lips, throat, tongue, or hives swelling means you have an allergic reaction.

Common side effects of Tofacitinib tablets include:

  • rash
  • headache
  • increased cholesterol levels
  • diarrhea
  • shingles
  • upper respiratory tract infections

Conclusion

Tofacitinib is a prescription medication used to treat certain autoimmune diseases, such as rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis. It works by blocking certain enzymes that contribute to inflammation and joint damage. 

Patients should inform their doctor of any medical conditions or medications they are taking before beginning treatment with Tofacitinib. Regular monitoring of blood tests and liver function is also recommended.

Overall, Tofacitinib can be a valuable treatment option for individuals with autoimmune diseases, but it is important for patients to weigh the potential risks and benefits carefully and to work closely with their healthcare provider to monitor and manage any side effects or complications that may arise. For any queries, reach out to Bulat Pharmaceuticals, the top active pharma ingredient manufacturers in the industry. 

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