Upanib: Each extended-release film coated tablet contains Upadacitinib Hemihydrate INN equivalent to Upadacitinib 15 mg.
Upadacitinib 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. Upadacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.
Upanib is indicated for the treatment of:
Moderately to severely active rheumatoid arthritis in adults who have had an inadequate response or intolerance to one or more TNF blockers. Active psoriatic arthritis in adults who have had an inadequate response or intolerance to one or more TNF blockers.
Active ankylosing spondylitis in adults who have had an inadequate response or intolerance to one or more TNF blockers. Moderately to severely active ulcerative colitis in adults who have had an inadequate response or intolerance to one or more TNF blockers. Refractory, moderate to severe atopic dermatitis in adults and pediatric patients 12 years of age and older whose disease is not adequately controlled with other systemic drug products, including biologics, or when use of those therapies are inadvisable.
Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis: The recommended dosage is 15 mg once daily. Atopic Dermatitis: Initiate treatment with 15 mg once daily. If an adequate response is not achieved, consider increasing the dosage to 30 mg once daily. Discontinue upanib if an adequate response is not achieved with the 30 mg dose. Use the lowest effective dose needed to maintain response. Adults 65 Years of Age and Older: The recommended dosage is 15 mg once daily. Ulcerative Colitis: The recommended induction dosage is 45 mg once daily for 8 weeks. The recommended maintenance dosage is 15 mg once daily. A maintenance dosage of 30 mg once daily may be considered for patients with refractory, severe, or extensive disease.
Prior to start treatment with Upanib, updating immunizations and evaluation of active and latent tuberculosis, viral hepatitis, hepatic function, and pregnancy status is required. Avoid initiation or interrupt Upanib if absolute lymphocyte count is less than 500 cells/mm 3 , absolute neutrophil count is less than 1000 cells/mm 3 , or hemoglobin level is less than 8 g/dL.
Serious Infections: Avoid use of Upadacitinib in patients with active, serious infection, including localized infections.
Malignancy: Consider the risks and benefits of Upadacitinib treatment prior to initiating therapy in patients with a known malignancy.
Thrombosis: Consider the risks and benefits prior to treating patients who may be at increased risk of thrombosis. Promptly evaluate patients with symptoms of thrombosis and treat appropriately.
Gastrointestinal Perforations: Use with caution in patients who may be at increased risk.
Laboratory Monitoring: Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids.
Embryo-Fetal Toxicity: Upadacitinib may cause fetal harm based on animal studies. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception.
Vaccinations: Avoid use of Upadacitinib with live vaccines.
Pregnancy: The limited human data on use of Upadacitinib in pregnant women are not sufficient to evaluate a drug-associated risk for major birth defects or miscarriage.
Based on animal studies, upadacitinib has the potential to adversely affect a developing fetus. Pediatric Use: The safety and efficacy of Upadacitinib in children and adolescents aged 0 to 18 years have not yet been established. No data are available.
Upanib: Each carton contains 3X10’s tablets in blister pack.
Strong CYP3A4 Inhibitors
Upadacitinib exposure is increased when co administered with strong CYP3A4 inhibitors (such as ketoconazole). Upadacitinib should be used with caution in patients receiving chronic treatment with strong CYP3A4 inhibitors.
Strong CYP3A4 Inducers
Upadacitinib exposure is decreased when co-administered with strong CYP3A4 inducers (such as rifampin), which may lead to reduced therapeutic effect of Upadacitinib. Coadministration of Upadacitinib with strong CYP3A4 inducers is not recommended.
Upadacitinib was administered in clinical trials up to doses equivalent in daily AUC to 60 mg extended-release once daily. Adverse events were comparable to those seen at lower doses and no specific toxicities were identified. Approximately 90% of upadacitinib in the systemic circulation is eliminated within 24 hours of dosing (within the range of doses evaluated in clinical studies). In case of an overdose, it is recommended that the patient be monitored for signs and symptoms of adverse reactions. Patients who develop adverse reactions should receive appropriate treatment.
Do not store above 25Degree C. Protect from light. Keep out of reach of children.