Everything You Need to Know about Apremilast

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Apremilast Structure

What is Apremilast?

Apremilast is a mixture of isomers, one of which is an inhibitor of phosphodiesterase 4 (PDE4). The Apremilast API is commonly sold under the brand name Otezla. It is an excellent medication used in treating psoriasis arthritis. It is a condition where the patient suffers from joint pain and itchiness/redness on the skin. Apremilast is generally given to patients that have shown no response to earlier medications or are intolerant (allergic) to other medications. 

Apremilast reduces arthritis psoriasis with the help of certain special chemical blockers. Besides arthritis psoriasis, Apremilast API also treats oral ulcers and plaque psoriasis (a condition where the skin becomes itchy, red, and flaky).  Aprelimast lowers the inflammation and pain of the patients by blocking the cells responsible for the spread of the disease. 

Here is the chemical structure of Apremilast API:

The other common details of Apremilast API are as follows:

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

Organizations and Clinical Trials of Apremilast

Apremilast API was clinically tested in four phases. A total of 94 organizations participated in 110 trials conducted by those organizations.

Most of the organizations that participated in the clinical trials of Apremilast were from the Research and Development field. To name a few organizations, we have:

However, some of those companies also took part in the marketing field. To name them, we have:

  • Hetero Labs Ltd
  • Amgen
  • MannKind Corp
  • Zydus Discovery DMCC 

Indications of Apremilast API

There are, so far, two approved indications of Apremilast:

  • Psoriasis
  • Arthritis, Psoriatic

There are 40 experimental indications of Apremilast:

  • Acne Conglobata (Phase 2)
  • Acne Vulgaris (Phase 2)
  • Alcoholism (Phase 2)
  • Alopecia (Phase 4)
  • Arthritis, Psoriatic ()
  • Arthritis, Rheumatoid (Phase 2)
  • Behcet Syndrome (Phase 3)
  • Cardiovascular Diseases (Phase 4)
  • Colitis, Ulcerative (Phase 2)
  • COVID-19 (Phase 3)
  • Dermatitis, Allergic Contact (Phase 2)
  • Dermatitis, Atopic (Phase 2)
  • Dermatology (Phase 2)
  • Dermatomyositis (Phase 2)
  • Digital Dermatitis (Phase 4)
  • Eczema (Phase 2)
  • Erythema (Phase 4)
  • Genital Diseases, Female (Phase 2)
  • Gout (Phase 2)
  • Healthy Volunteers (Phase 1)
  • Hidradenitis Suppurativa (Phase 2)
  • Lichen Planus (Phase 2)
  • Lichen Planus, Oral (Phase 2)
  • Lupus Erythematosus, Discoid (Phase 1/Phase 2)
  • Osteoarthritis (Phase 2)
  • Parapsoriasis (Phase 4)
  • Pharmacokinetics (Phase 1)
  • Prostatitis (Phase 2)
  • Prurigo (Phase 2)
  • Pruritus (Phase 2)
  • Psoriasis ()
  • Rosacea (Phase 2)
  • Sarcoidosis (Phase 3)
  • Spondylitis, Ankylosing (Phase 3)
  • Stomatitis, Aphthous (Phase 3)
  • Substance Withdrawal Syndrome (Phase 3)
  • Uveitis (Phase 1/Phase 2)
  • Vitiligo (Phase 2)
  • Vulva (Phase 2)
  • Vulvodynia (Phase 2)

How Does Apremilast Works?

Apremilast is a medicine that falls under the phosphodiesterase 4 inhibitors (PDE4) category and works by blocking the activities caused by PDE4. This cell is responsible for inflammation due to psoriasis, and blocking this cell helps to reduce the effects of arthritis psoriasis

Apremilast is available in tablet form and must be consumed orally under the supervision of your physician. The tablets come in 10mg, 20mg, and 30mg categories. Deciding the dosage as per your doctor’s prescription is strongly advised. The patients should not chew, break, or crush Apremilast tablets. Instead, they should swallow it using normal water. 

Pharmacology of Apremilast

Mechanism of Action: PDE4 Inhibitor

Black Box: No

Delivery Method: Oral in the form of Capsules

Pro Drug: No

ALogP: 2.43

Technology: Synthetic

Available Formulations: Oral Solid

What is the Main Use of Apremilast?

Apremilast is a widely used medicine used by adults to treat psoriasis or other skin infections. It is also used to treat a variety of inflammation-related diseases. To name the most prominent ones, we have:

  • Apremilast is majorly used in treating arthritis psoriasis condition. The Apremilast API blocks the activities of PDE4, thereby controlling the spread of inflammation and pain in the person’s body. 
  • It is widely used for treating Plaque psoriasis where patients have undergone phototherapy or other treatments for psoriasis.
  • Apremilast is also used to treat oral ulcers caused by Behcet’s disease (a disease caused by inflammation inside the blood vessels.)

Apremilast generally works on reducing inflammation and pain, thereby causing relief to the patients. The medicine acts directly on the psoriasis cells and stops the spread of disease inside the patient’s body. 

Read Also: Psoriatic Arthritis: Symptoms, Medications, and Cure

What are the Side Effects of Apremilast?

Although Apremilast is a safe medicine that treats psoriasis, there are some common side effects associated with this medication. To name a few, we have

  • Diarrhea
  • Nausea
  • Vomiting
  • Headache
  • Tension headache
  • Gastro-esophageal reflux disease
  • Back pain
  • Fatigue
  • Tooth abscess
  • Hair follicle inflammation
  • Joint pain

Some side effects, like cough and headache, are common. However, you must consult your doctor immediately if you experience any other side effects or extreme headaches.

Who Should Not Take Apremilast?

Any adult can take Apremilast with Plaque psoriasis, oral ulcers caused by Behcet’s disease, or arthritis psoriasis. However, some exceptions must limit themselves from taking this medicine. 

  • Patients with a history of depression should not be prescribed Apremilast.
  • Pregnant or breastfeeding women should also not consume Apremilast.
  • People experiencing loss of appetite or significant weight loss should also stop consuming Apremilast. 
  • Patients with past kidney disorders should also not be prescribed Apremilast. 

How to Store and Dispose of Apremilast?

There are certain ways to store and dispose of the Apremilast API. For instance, you must keep this drug in an air-tight container tightly closed and out of reach of children. Apremilast must be stored at room temperature and away from direct light, excess heat, and moisture. Always use a dry place to store the drug. 

It is to be noted that Apremilast is a highly reactive medicine. Hence, you must limit your children’s use of the Apremilast tablets container. Always use safety locks or far-reaching areas to store Apremilast medicine to prevent young children from poisoning. 

Unused medicine should be directly disposed of using special techniques that protect the environment and eliminates contact with stray animals, pets, and children. Remember not to flush the medicine if not in use. Instead, you can dispose of the medication using the medicine take-back method. If you do not know much about the take-back program, you must consult your pharmacist or local garbage/recycling department. You can even read FDA’s guidelines on the medicine take-back program. 

Conclusion

Apremilast is a highly reactive drug used by adults to treat arthritis psoriasis. Besides that, Apremilast is also used to treat Plaque psoriasis and oral ulcers. Apremilast weighs 460.5 and falls under the steroid category of medication. It blocks PDE4, thereby eliminating further inflammation and pain in the patients. 

Pregnant women, patients with kidney disorders, and depression must not take this medicine. Furthermore, you also should connect with your doctor if you experience significant weight loss or severe headaches. Apremilast must be stirred in a safe and dry condition away from direct sunlight and be disposed of using the medicine take-back method. 

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