Upadacitinib

Category: pharmacological

Aliases: Rinvoq, ABT-494

Pharmacological Mechanism

JAK1-selective inhibitor — designed for higher JAK1 selectivity vs tofacitinib (less JAK2/JAK3 hit, theoretically less anemia/lymphopenia). Indications: rheumatoid arthritis, atopic dermatitis, ulcerative colitis, Crohn disease, ankylosing spondylitis, psoriatic arthritis, giant cell arteritis. CYP3A4 substrate. Black-box warning for MACE / malignancy / VTE (JAK class effect from ORAL Surveillance). PK (Rinvoq label, 15 mg ER PO qd): t½ 9-14 h, Tmax 2-3 h fasting / 4 h fed, F 76% relative to IR (absolute F not stated). Apparent CL/F 53.7 L/h, V/F 294 L. Steady state by day 4 with no accumulation. CYP3A4 substrate (avoid strong CYP3A4 inhibitors).

Half-Life (t½)

PO: 11.5h

Dosing Guidelines

Target Organ Systems