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Rilpivirine (RPV / Edurant)

Antiretroviralprescriptionoral · predicted

Second-generation NNRTI used for HIV treatment in patients with baseline viral load <100,000 copies/mL; component of Complera, Odefsey, Juluca, and (as long-acting IM) Cabenuva with cabotegravir. Oral half-life ~45h enables once-daily; IM depot apparent t1/2 ~600-800h. Requires food for absorption (F ~40% with meal). Metabolized by CYP3A4.

Projected serum levels — 25 mg, once daily

Rilpivirine (RPV / Edurant)
Rilpivirine (RPV / Edurant) modeled serum levels, 25 mg once daily over 17 days Population-based pharmacokinetic estimate. Steady state reached after approximately 7 days. 0 12.5 25 37.5 50 Day 0 Day 4 Day 9 Day 13 Day 17 Time on a regular schedule ≈ steady state · day 7
Rilpivirine (RPV / Edurant) modeled serum levels with a loading dose of 75 mg, then 25 mg once daily The first dose is larger so levels approach steady state faster. 0 12.5 25 37.5 50 Day 0 Day 4 Day 9 Day 13 Day 17 Time on a regular schedule

Maintenance schedule: 25 mg once daily (oral).

Loading schedule: 75 mg on day 1, then 25 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~7 days: peak ≈ 32.3 mg, trough ≈ 25.7 mg body load. Population-based estimate over 17 days for a 25 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Antiretroviral
Route modeled
Oral
Model confidence
predicted
Half-life
2.1 days
Common dose
25 mg
Suggested maximum
50 mg/day
Reference dose range
25–50 mg (single dose)
Suggested cadence
once daily
Validated against
25 mg oral — Cmax 0.25 mg/L at 4 h

Documented interactions

  • contraindicated
    Clarithromycin (Biaxin) + Rilpivirine (RPV / Edurant) CYP inhibition

    Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Rilpivirine (RPV / Edurant) AUC by ~6.67x

  • contraindicated
    Diltiazem + Rilpivirine (RPV / Edurant) CYP inhibition

    Diltiazem mechanism_based of CYP3A4 predicted to change Rilpivirine (RPV / Edurant) AUC by ~6.67x

  • contraindicated
    Efavirenz (Sustiva) + Rilpivirine (RPV / Edurant) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Rilpivirine (RPV / Edurant) AUC by ~0.13x

  • contraindicated
    Grapefruit (whole fruit) + Rilpivirine (RPV / Edurant) CYP inhibition

    Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Rilpivirine (RPV / Edurant) AUC by ~6.67x

  • contraindicated
    Grapefruit Juice + Rilpivirine (RPV / Edurant) CYP inhibition

    Grapefruit Juice mechanism_based of CYP3A4 predicted to change Rilpivirine (RPV / Edurant) AUC by ~6.67x

  • contraindicated
    Paxlovid (Nirmatrelvir/Ritonavir) + Rilpivirine (RPV / Edurant) CYP inhibition

    Paxlovid (Nirmatrelvir/Ritonavir) mechanism_based of CYP3A4 predicted to change Rilpivirine (RPV / Edurant) AUC by ~6.67x

Serum checks 254 modeled interaction pairings for rilpivirine (rpv / edurant) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Clinical pharmacokinetics of rilpivirine: a review Crauwels H et al. · HIV Clinical Trials, 2013 DOI

    Comprehensive PK review characterizing rilpivirine's ~45h half-life, food-dependent absorption, and CYP3A4 metabolism.

  2. Long-acting cabotegravir and rilpivirine after oral induction for HIV-1 infection (FLAIR) Orkin C et al. · New England Journal of Medicine, 2020 DOI

    FLAIR trial establishing long-acting IM cabotegravir + rilpivirine non-inferior to oral DTG/ABC/3TC, validating monthly injectable HIV treatment.

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