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Upadacitinib (Rinvoq)

JAK Inhibitorprescriptionoral · inferred

Selective JAK1 inhibitor (>60-fold selectivity over JAK2/3 at therapeutic concentrations). Approved for rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, non-radiographic axSpA, atopic dermatitis, ulcerative colitis, and Crohn's disease. Extended-release formulation. RA 15 mg QD; atopic dermatitis/IBD 15, 30, or 45 mg QD. Plasma half-life ~9-14h. High oral bioavailability. Primarily CYP3A4 metabolism. Same class boxed warnings as tofacitinib.

Projected serum levels — 15 mg, once daily

Upadacitinib (Rinvoq)
Upadacitinib (Rinvoq) modeled serum levels, 15 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 5 10 15 20 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1
Upadacitinib (Rinvoq) modeled serum levels with a loading dose of 18.7 mg, then 15 mg once daily The first dose is larger so levels approach steady state faster. 0 5 10 15 20 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule

Maintenance schedule: 15 mg once daily (oral).

Loading schedule: 18.7 mg on day 1, then 15 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~1 days: peak ≈ 11.9 mg, trough ≈ 2.7 mg body load. Population-based estimate over 15 days for a 15 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
JAK Inhibitor
Route modeled
Oral
Model confidence
inferred
Half-life
10 h
Common dose
15 mg
Suggested maximum
45 mg/day
Reference dose range
7.5–45 mg (single dose)
Suggested cadence
once daily
Validated against
15 mg oral — Cmax 0.043 mg/L at 2.5 h

Documented interactions

  • contraindicated
    Clarithromycin (Biaxin) + Upadacitinib (Rinvoq) CYP inhibition

    Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Upadacitinib (Rinvoq) AUC by ~5.00x

  • contraindicated
    Diltiazem + Upadacitinib (Rinvoq) CYP inhibition

    Diltiazem mechanism_based of CYP3A4 predicted to change Upadacitinib (Rinvoq) AUC by ~5.00x

  • contraindicated
    Efavirenz (Sustiva) + Upadacitinib (Rinvoq) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Upadacitinib (Rinvoq) AUC by ~0.14x

  • contraindicated
    Grapefruit (whole fruit) + Upadacitinib (Rinvoq) CYP inhibition

    Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Upadacitinib (Rinvoq) AUC by ~5.00x

  • contraindicated
    Grapefruit Juice + Upadacitinib (Rinvoq) CYP inhibition

    Grapefruit Juice mechanism_based of CYP3A4 predicted to change Upadacitinib (Rinvoq) AUC by ~5.00x

  • contraindicated
    Paxlovid (Nirmatrelvir/Ritonavir) + Upadacitinib (Rinvoq) CYP inhibition

    Paxlovid (Nirmatrelvir/Ritonavir) mechanism_based of CYP3A4 predicted to change Upadacitinib (Rinvoq) AUC by ~5.00x

Serum checks 87 modeled interaction pairings for upadacitinib (rinvoq) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Population pharmacokinetics of upadacitinib using the immediate-release and extended-release formulations in healthy subjects and subjects with rheumatoid arthritis Klünder B et al. · Clinical Pharmacokinetics, 2019 DOI

    Population PK model across formulations and populations: ER t1/2 ~9-14h, linear PK, basis for QD dosing.

  2. Safety and efficacy of upadacitinib in patients with rheumatoid arthritis and inadequate response to conventional synthetic DMARDs (SELECT-NEXT) Burmester GR et al. · Lancet, 2018 DOI

    Pivotal SELECT-NEXT phase 3 trial showing upadacitinib 15 mg and 30 mg QD efficacy in csDMARD-IR RA.

2 published studies referenced in the app, each with a plain-language summary.