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Tofacent (Tofacitinib)
Therapeutic Group: Monoclonal Antibody
Presentation
Tofacent

Tofacent 5: Each tablet contains Tofacitinib Citrate INN equivalent to Tofacitinib 5 mg

Descriptions
Tofacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1/JAK3, JAK1/JAK2, JAK1/TyK2, JAK2/JAK2). Tofacitinib inhibited the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively. However, the relevance of specific JAK combinations to therapeutic effectiveness is not known.
Indications
Tofacitinib is an inhibitor of Janus kinases (JAKs) indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to Methotrexate. It may be used as monotherapy or in combination with Methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs).



Limitations of Use: Use of Tofacitinib in combination with biologic DMARDs or potent immunosuppressant such as Azathioprine and cyclosporine is not recommended
Dosage & Administration
Rheumatoid Arthritis
• Recommended dose of Tofacitinib is 5 mg twice daily
• Recommended dose in patients with moderate and severe renal impairment and moderate hepatic impairment is Tofacitinib 5 mg once daily
• Use of Tofacitinib in patients with severe hepatic impairment is not recommended
Side Effects
The most commonly reported adverse reactions during the first 3 months in controlled clinical trials (occurring in greater than or equal to 2% of patients treated with Tofacitinib monotherapy or in combination with DMARDs) were upper respiratory tract infections, headache, diarrhea and nasopharyngitis.
Precautions
Use of Tofacitinib during an active serious infection, including localized infections should be avoided
Gastrointestinal Perforations – Should be used with caution in patients that may be at increased risk
Laboratory Monitoring – Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids
Immunizations – Live vaccines: Should be avoided
Contraindications
None
Use in Pregnancy & Lactation
Pregnancy Category C
There are no adequate and well-controlled studies in pregnant women. Tofacitinib should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
It is not known whether Tofacitinib is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Tofacitinib, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug for the mother
Pediatric Use
The safety and effectiveness of Tofacitinib in pediatric patients have not been established.
Geriatric Use
The frequency of serious infection among Tofacitinib-treated subjects 65 years of age and older was higher than among those under the age of 65. As there is a higher incidence of infections in the elderly population in general, caution should be used when treating the elderly.
Drug Interaction
Potent inhibitors of Cytochrome P450 3A4 (CYP3A4) (e.g., Ketoconazole):
• Recommended dose is Tofacitinib 5 mg once daily : One or more concomitant medications that result in both moderate inhibition of CYP3A4 and potent inhibition of CYP2C19 (e.g., fluconazole):
• Recommended dose is Tofacitinib 5 mg once daily Potent CYP inducers (e.g.Rifampin): May result in loss of or reduced clinical response.
Commercial Packaging
Tofacent 5: Each box contains 1 blister strip of 10 tablets
Tofacent 5: Each bottle contains 60 tablets
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