Rinvoq

Upadacitinib

As monotherapy or in combination w/ MTX for the treatment of moderate to severe active RA in adults w/ inadequate response to, or w/ intolerance to, ≥1 DMARDs. As monotherapy or in combination w/ MTX for the treatment of active psoriatic arthritis in adults w/ inadequate response to, or w/ intolerance to, ≥1 DMARDs. Treatment of active non-radiographic axial spondyloarthritis in adults w/ objective signs of inflammation as indicated by elevated C-reactive protein &/or MRI, who have responded inadequately to NSAIDs. Treatment of active ankylosing spondylitis in adults w/ inadequate response to conventional therapy. Treatment of moderate to severe atopic dermatitis in adults & adolescents ≥12 yr who are candidates for systemic therapy. Treatment of moderate to severe active ulcerative colitis in adults w/ inadequate response, lost response or were intolerant to either conventional therapy or a biologic agent. Treatment of moderate to severe active Crohn's disease in adults w/ inadequate response, lost response or were intolerant to either conventional therapy or a biologic agent.

RA, psoriatic arthritis, axial spondyloarthritis Adult 15 mg once daily. Atopic dermatitis Adult 15 or 30 mg once daily. 15 mg is recommended for patients at higher risk of VTE, major adverse CV events & malignancy; 30 mg once daily for patients w/ high disease burden not at higher risk of VTE, major adverse CV events & malignancy or patients w/ inadequate response to 15 mg once daily. Consider lowest effective dose for maintenance. Adolescent 12-17 yr, weighing at least 30 kg 15 mg once daily. Elderly ≥65 yr 15 mg once daily. Ulcerative colitis Adult Induction dose: 45 mg once daily for 8 wk. May be continued for additional 8 wk if no adequate therapeutic benefit by wk 8. Maintenance: 15 or 30 mg once daily. 15 mg is recommended for patients at higher risk of VTE, major adverse CV events & malignancy; 30 mg once daily for patients w/ high disease burden or requiring 16-wk induction treatment who are not at higher risk of VTE, major adverse CV events & malignancy or patients w/ inadequate response to 15 mg once daily. Consider lowest effective dose for maintenance. Elderly ≥65 yr Maintenance: 15 mg once daily. Crohn's disease Adult Induction dose: 45 mg once daily for 12 wk. Consider prolonged induction for additional 12 wk if no adequate therapeutic benefit after initial 12-wk induction. Maintenance: 15 or 30 mg once daily. 15 mg is recommended for patients at higher risk of VTE, major adverse CV events & malignancy; 30 mg once daily for patients w/ high disease burden not at higher risk of VTE, major adverse CV events & malignancy or patients w/ inadequate response to 15 mg once daily. Consider lowest effective dose for maintenance. Elderly ≥65 yr Maintenance: 15 mg once daily.

May be taken with or without food: Swallow whole, do not split/crush/chew. Avoid grapefruit-containing food/drink.

Hypersensitivity. Active TB or serious infections. Severe hepatic impairment. Pregnancy.

Should only be used if no suitable treatment alternatives are available in patients ≥65 yr; patients w/ history of atherosclerotic CV disease or other CV risk factors (eg, current or past long-time smokers); patients w/ malignancy risk factors (eg, current or history of malignancy). Discontinue treatment in case of clinically significant hypersensitivity reaction. Reports of serious & sometimes fatal infections; viral reactivation; lymphoma & other malignancies; non-melanoma skin cancer; haematological abnormalities; diverticulitis & GI perforations; VTE. Interrupt therapy if patient develops a serious or opportunistic infection. Screen patients for TB before starting therapy & monitor for development of TB signs & symptoms during therapy, including patients who tested -ve for latent TB infection prior to initiating therapy. Screen patients for viral hepatitis & monitor for reactivation before starting treatment & during therapy. Not recommended to use live, attenuated vaccines during or immediately prior to therapy. Bring patients up to date w/ all immunisations, including prophylactic zoster vaccinations, prior to treatment initiation. Periodic skin exam is recommended for all patients, particularly those w/ risk factors for skin cancer. Do not initiate or temporarily interrupt treatment in patients w/ ANC <1 x 10⁹ cells/L, absolute lymphocyte count <0.5 x 10⁹ cells/L or Hb <8 g/dL. Increased lipid parameters, including total, LDL & HDL cholesterol. Increased incidence of liver enzyme elevation. Not recommended to combine w/ other potent immunosuppressants (eg, azathioprine, 6-mercaptopurine, ciclosporin, tacrolimus, & biologic DMARDs or other JAK inhibitors). Caution in patients w/ severe renal impairment. Not recommended in patients w/ end stage renal disease. Women of childbearing potential should use effective contraception during treatment & for 4 wk following final dose. Should not be used during breast-feeding. RA, psoriatic arthritis, axial spondyloarthritis, ulcerative colitis, Crohn's disease: Safety & efficacy have not been established in childn & adolescent <18 yr. Atopic dermatitis: Safety & efficacy have not been established in childn <12 yr; adolescent weighing <40 kg.

URTI, acne. Bronchitis, herpes zoster, herpes simplex, folliculitis, flu, UTI, pneumonia; non-melanoma skin cancer; anaemia, neutropaenia, lymphopaenia; urticaria; hypercholesterolaemia, hyperlipidaemia; cough; abdominal pain, nausea; rash; fatigue, pyrexia; increased blood creatine phosphokinase, ALT, AST, wt; headache.

Increased exposure w/ strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, posaconazole, voriconazole, clarithromycin, grapefruit). Decreased exposure w/ strong CYP3A4 inducers (eg, rifampin & phenytoin). Risk of additive immunosuppression w/ other potent immunosuppressants eg, azathioprine, 6-mercaptopurine, ciclosporin, tacrolimus & biologic DMARDs or other JAK inhibitors.

Disease-Modifying Anti-Rheumatic Drugs (DMARDs) / Immunosuppressants

L04AF03 - upadacitinib ; Belongs to the class of Janus-associated kinase (JAK) inhibitors. Used as immunosuppressants.

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