Tofacitinib is an orally available Janus kinases (JAK) inhibitor used to treat rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis. This drug is sold under the common name Xeljanz. JAKs are intracellular, nonreceptor tyrosine kinases that propagate inflammation in rheumatoid arthritis. Tofacitinib suppresses this inflammation by activating transcription signal transducers and activators, thereby relieving arthritis problems.
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What is Tofacitinib?
Product Description
Molar Mass: 312.38
SMILES: C[C@@H]1CCN(C[C@@H]1N(C)c2ncnc3[nH]ccc23)C(=O)CC#N
InChIKey: UJLAWZDWDVHWOW-YPMHNXCESA-N
ALogP: 1.54
CAS Number: 477600-75-2
Chemical Formula: C16H20N6O
Therapeutic Category: Anti-Arthritis Musculoskeletal
Form: Oral tablet
Bioavailability: 74%
Assay: NLT 99.0%
Suitable for: Adults
IUPAC Name: 3-[(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
Approved Indications: 1
As per the clinical trials, there is one approved indication of the Tofacitinib drug:
- Arthritis, Rheumatoid
Experimental Indications: 64
As per clinical trials 1-4, the drug can be used in the following categories:
- Alopecia (Phase 2)
- Alopecia Areata (Phase 4)
- Arthritis (Phase 4)
- Arthritis, Juvenile (Phase 3)
- Arthritis, Psoriatic (Phase 4)
- Arthritis, Rheumatoid (Phase 4)
- Axial Spondyloarthritis (Phase 4)
- Cholangiocarcinoma (Phase 1)
- Colitis, Ulcerative (Phase 4)
- COVID-19 (Phase 2)
- Crohn’s Disease (Phase 2)
- Depression (Phase 1/Phase 2)
- Dermatitis, Atopic (Phase 2)
- Dermatology (Phase 2)
- Dermatomyositis (Phase 1)
- Diaphragm (Phase 1)
- Down Syndrome (Phase 2)
- Dry Eye Syndromes (Phase 2)
- Eczema (Phase 2)
- Glycogen Storage Disease Type II (Phase 3)
- Granulomatosis with Polyangiitis (Phase 4)
- Granulomatous Disease, Chronic (Phase 1/Phase 2)
- Healthy Volunteers (Phase 1)
- Hepatic Insufficiency (Phase 1)
- Hidradenitis Suppurativa (Phase 2)
- Ileum (Phase 2)
- Immune System Diseases (Phase 2)
- Immunomodulation (Phase 1)
- Inflammation (Phase 1/Phase 2)
- Intestinal Neoplasms (Phase 2)
- Keratoconjunctivitis Sicca (Phase 2)
- Kidney Failure, Chronic (Phase 1)
- Kidney Transplantation (Phase 2)
- Lung Diseases (Phase 4)
- Lung Diseases, Interstitial (Phase 4)
- Lupus Erythematosus, Cutaneous (Phase 2)
- Lupus Erythematosus, Discoid (Early Phase 1)
- Lupus Erythematosus, Systemic (Phase 1/Phase 2)
- Lymphoma, Extranodal NK-T-Cell (Phase 2)
- Mesothelioma (Phase 1)
- Methotrexate (Phase 4)
- Myasthenia Gravis (Early Phase 1)
- Neoplasms (Phase 1)
- Pancreatic Neoplasms (Phase 1)
- Pharmacokinetics (Phase 2)
- Polymyalgia Rheumatica (Phase 2)
- Pouchitis (Phase 2)
- Psoriasis (Phase 3)
- Renal Dialysis (Phase 1)
- Rheumatic Fever (Phase 4)
- Sacroiliitis (Phase 4)
- Sarcoidosis (Phase 1)
- Sarcoidosis, Pulmonary (Phase 1)
- Scleritis (Phase 2)
- Scleroderma, Systemic (Phase 2)
- Sjogren’s Syndrome (Phase 2)
- Spondylarthritis (Phase 4)
- Spondylitis (Phase 4)
- Spondylitis, Ankylosing (Phase 3)
- Substance Withdrawal Syndrome (Phase 3)
- Takayasu Arteritis (Phase 4)
- Therapeutics (Phase 4)
- Uveitis (Phase 2)
- Vitiligo (Phase 2)
Clinical Trials:
A total of 168 trials took place in four phases. 183 organizations participated in these trials.
Side Effects
Major side effects observed after the consumption of Tofacitinib are:
- Diarrhea
- Headache
- High Blood Pressure
Therapeutic Action
Tofacitinib is used to treat certain types of arthritis (such as psoriatic arthritis, rheumatoid arthritis, polyarticular course juvenile idiopathic arthritis-pcJIA). It helps to decrease pain/tenderness/swelling in the joints. Tofacitinib is also used to treat a certain bowel disease (ulcerative colitis).
Product CAS No
477600-75-2
Conclusion
Tofacitinib is an oral drug used to treat arthritis and related joint pain issues. The drug has a molar mass of 312.38 g/mol and is sold under the brand name Xeljanz. A total of 168 trials took place in four phases for this drug. Apart from joint pain, there are many other experimental indications for this drug: alopecia areata, COVID, lung disease, etc. Headache and high blood pressure are some common side effects seen with the intake of the Tofacitinib drug.
