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Doravirine (Pifeltro)

Antiretroviralprescriptionoral · inferred

Next-generation NNRTI with improved tolerability and retained activity against common NNRTI-resistance mutations (K103N, Y181C, G190A). 100 mg PO once daily with or without food. Plasma half-life ~15h. High oral bioavailability (~64-70%, formulation-dependent). Metabolized primarily by CYP3A4. Less CNS toxicity and better lipid profile than efavirenz. Pivotal DRIVE-FORWARD and DRIVE-AHEAD trials established non-inferiority to boosted darunavir and efavirenz-based regimens.

Projected serum levels — 100 mg, once daily

Doravirine (Pifeltro)
Doravirine (Pifeltro) modeled serum levels, 100 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 25 50 75 100 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1
Doravirine (Pifeltro) modeled serum levels with a loading dose of 143 mg, then 100 mg once daily The first dose is larger so levels approach steady state faster. 0 25 50 75 100 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule

Maintenance schedule: 100 mg once daily (oral).

Loading schedule: 143 mg on day 1, then 100 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~1 days: peak ≈ 82.4 mg, trough ≈ 27.1 mg body load. Population-based estimate over 15 days for a 100 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
inferred
Half-life
15 h
Common dose
100 mg
Suggested maximum
100 mg/day
Reference dose range
50–100 mg (single dose)
Suggested cadence
once daily
Validated against
100 mg oral — Cmax 0.96 mg/L at 2 h

Documented interactions

  • contraindicated
    Carbamazepine (Tegretol) + Doravirine (Pifeltro) CYP induction

    Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Doravirine (Pifeltro) AUC by ~0.20x

  • contraindicated
    Clarithromycin (Biaxin) + Doravirine (Pifeltro) CYP inhibition

    Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Doravirine (Pifeltro) AUC by ~10.00x

  • contraindicated
    Dasatinib (Sprycel) + Doravirine (Pifeltro) CYP inhibition

    Dasatinib (Sprycel) time_dependent_inhibitor of CYP3A4 predicted to change Doravirine (Pifeltro) AUC by ~5.00x

  • contraindicated
    Diltiazem + Doravirine (Pifeltro) CYP inhibition

    Diltiazem mechanism_based of CYP3A4 predicted to change Doravirine (Pifeltro) AUC by ~10.00x

  • contraindicated
    Efavirenz (Sustiva) + Doravirine (Pifeltro) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Doravirine (Pifeltro) AUC by ~0.12x

  • contraindicated
    Grapefruit (whole fruit) + Doravirine (Pifeltro) CYP inhibition

    Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Doravirine (Pifeltro) AUC by ~10.00x

Serum checks 80 modeled interaction pairings for doravirine (pifeltro) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Clinical pharmacokinetics of doravirine, a novel HIV-1 non-nucleoside reverse transcriptase inhibitor Sanchez RI et al. · Clinical Pharmacokinetics, 2019 DOI

    Comprehensive PK review: t1/2 ~15h, CYP3A4 metabolism, minimal food effect, and minimal interaction potential supporting QD dosing.

  2. Doravirine versus ritonavir-boosted darunavir in antiretroviral-naive adults with HIV-1 (DRIVE-FORWARD) Molina JM et al. · Lancet HIV, 2018 DOI

    Phase 3 trial demonstrating doravirine non-inferiority vs boosted darunavir with superior lipid profile.

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