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Upatinib is a highly efficient and selective Janus kinase (JAK) inhibitor. By inhibiting the activity of JAK enzyme, it blocks the JAK-STAT signaling pathway, inhibits the release of pro-inflammatory cytokines, and reduces inflammatory response.
Upatinib (trade name: RINVOQ/RINVOQLQ) is a Janus kinase (JAK) inhibitor, suitable for the following diseases:
Active PsA in adults and children ≥2 years of age with insufficient response to or intolerance to TNF inhibitors.
Adults and children ≥12 years old (weight ≥40kg) have moderate to severe refractory AD that is poorly controlled or not suitable for other systemic treatments (including biological agents).
Adults with moderate to severe active UC and insufficient response or intolerance to TNF inhibitors.
Adults with moderately to severely active CD and insufficient response or intolerance to TNF inhibitors.
Adults with active AS and insufficient response or intolerance to TNF inhibitors.
Active pJIA in children ≥2 years of age with inadequate response to or intolerance to TNF inhibitors.
It is prohibited to combine with other JAK inhibitors, biological agents (such as DMARDs) or powerful immunosuppressants (such as azathioprine, cyclosporine).
Patients with atopic dermatitis are prohibited from using other immunomodulators in combination.
Oral liquid (1mg/mL) requires a special adapter and syringe for administration and is not interchangeable with tablets.
Latent/active tuberculosis, viral hepatitis, routine blood tests (lymphocytes, neutrophils, hemoglobin), liver function and pregnancy status need to be checked before treatment, and vaccinations should be updated.
Avoid starting or interrupting treatment if lymphocytes <500/mm³, neutrophils <1000/mm³, or hemoglobin <8g/dL.
Adults: 15 mg once daily.
Adults: 15 mg once daily.
Children ≥2 years old: Dosage according to body weight (10~<20kg: 3mg oral solution, twice a day; 20~<30kg: 4mg oral solution, twice a day; ≥30kg: 6mg oral solution, twice a day or 15mg tablet once a day).
Adults <65 years old and children ≥12 years old (weight ≥40kg): Starting with 15 mg once a day, if the efficacy is insufficient, it can be increased to 30 mg once a day.
Adults ≥65 years old: 15 mg once daily.
Induction period: 45 mg once daily for 8 weeks.
Maintenance period: 15 mg once a day; refractory/severe patients may consider 30 mg once a day.
Induction period: 45 mg once daily for 12 weeks.
Maintenance period: 15 mg once a day; refractory/severe patients may consider 30 mg once a day.
Children aged ≥2 years old should be dosed according to body weight (same as psoriatic arthritis).
UC/CD with severe damage (eGFR15~<30mL/min): 30 mg once a day during the induction period and 15 mg once a day during the maintenance period.
AD with severe damage: 15mg once a day.
Disabled in patients with end-stage renal disease (eGFR<15mL/min).
UC/CD with mild to moderate damage (Child-PughA/B): 30 mg once a day during the induction period and 15 mg once a day during the maintenance period.
Heavy damage (Child-PughC) is disabled.
Strong CYP3A4 inhibitors (such as ketoconazole): Avoid combined use of 30 mg in patients with AD; reduce to 30 mg once daily in patients with UC/CD during the induction period.
Strong CYP3A4 inducers (such as rifampicin): avoid combined use.
1. Serious infections (including tuberculosis, bacterial/fungal/viral infections): may result in hospitalization or death, and signs of infection need to be monitored during treatment.
2. Increased mortality: JAK inhibitors have a higher all-cause mortality rate in RA patients than TNF inhibitors.
3. Malignant tumors (such as lymphoma, lung cancer): The risk is higher than that of TNF inhibitors, and smokers have a higher risk.
4. Major cardiovascular events (MACE, such as myocardial infarction, stroke): The risk is higher in RA patients than with TNF inhibitors.
5. Thrombosis (deep vein thrombosis, pulmonary embolism): Avoid use by high-risk patients.
Rheumatoid/psoriatic arthritis: Upper respiratory tract infection, shingles, herpes simplex, nausea, cough, fever, acne, headache.
Atopic dermatitis: upper respiratory tract infection, acne, herpes simplex, headache, elevated creatine phosphokinase, cough, allergies, folliculitis.
Ulcerative colitis: Upper respiratory tract infection, elevated creatine phosphokinase, acne, neutropenia, elevated liver enzymes, rash.
Crohn's disease: Upper respiratory tract infection, anemia, fever, acne, shingles, headache.
1. Risk of infection: It is contraindicated in patients with active infection (including local infection); if serious infection occurs during treatment, dosing must be interrupted.
2. Allergic reaction: Severe allergies (such as immediate allergy) require permanent discontinuation of the drug.
3. Gastrointestinal perforation: High-risk patients (such as diverticulitis, combined use of NSAIDs/glucocorticoids) need to monitor abdominal pain symptoms.
4. Laboratory monitoring: Regularly check blood routine, liver enzymes, and blood lipids (evaluated after 12 weeks of treatment).
5. Embryotoxicity: Animal experiments show the risk of teratogenesis. Women of childbearing age need to use contraception until 4 weeks after stopping the drug.
6. Vaccination: Avoid the use of live vaccines, and all immunizations must be completed before treatment.
7. Drug residues: People with shortened gastrointestinal transit time may have unabsorbed drugs in their feces, and the efficacy needs to be evaluated.
Pregnant women: May cause fetal harm, contraindicated during pregnancy. Contraception is required during medication and for 4 weeks after stopping medication.
Lactation period: The drug can be excreted in breast milk. It is recommended to avoid breastfeeding within 6 days after stopping the drug.
Children: ≥2 years old: applicable to pJIA and PsA; ≥12 years old (≥40kg): applicable to AD; <2 years old: safety of pJIA/PsA has not been established; <12 years old or weight <40kg: safety of AD has not been established.
Older adults (≥65 years): Patients with RA/PsA are at increased risk for adverse events (such as serious infections).
There is limited data on UC/CD/AS patients, so medication should be used with caution.
Hepatic and renal insufficiency: Dosage according to the "Adjustments for Special Populations" mentioned above.
Disabled by those allergic to upatinib or any excipients.