Home › Compound Library › Darunavir (Prezista)

Darunavir (Prezista)

Antiretroviralprescriptionoral · predicted

Second-generation HIV protease inhibitor with high genetic barrier to resistance; always co-administered with a pharmacokinetic booster (ritonavir 100 mg or cobicistat 150 mg). Boosted darunavir 800 mg QD (treatment-naive) or 600 mg BID (experienced) PO with food. Boosted half-life ~15h; unboosted oral F ~37% (rising to ~82% boosted). Extensive CYP3A4 metabolism. Sulfonamide moiety, caution with sulfa allergy. Common AEs: diarrhea, rash, dyslipidemia.

Projected serum levels — 800 mg, once daily

Darunavir (Prezista)
Darunavir (Prezista) modeled serum levels, 800 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 3 days. 0 500 1k 1.5k 2k Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 3
Darunavir (Prezista) modeled serum levels with a loading dose of 1.5k mg, then 800 mg once daily The first dose is larger so levels approach steady state faster. 0 500 1k 1.5k 2k Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule

Maintenance schedule: 800 mg once daily (oral).

Loading schedule: 1.5k mg on day 1, then 800 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~3 days: peak ≈ 1.1k mg, trough ≈ 602 mg body load. Population-based estimate over 15 days for a 800 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
15 h
Common dose
800 mg
Suggested maximum
800 mg/day
Reference dose range
400–800 mg (single dose)
Suggested cadence
once daily
Validated against
600 mg oral — Cmax 6.5 mg/L at 2.5 h

Documented interactions

  • contraindicated
    Carbamazepine (Tegretol) + Darunavir (Prezista) CYP induction

    Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Darunavir (Prezista) AUC by ~0.20x

  • contraindicated
    Clarithromycin (Biaxin) + Darunavir (Prezista) CYP inhibition

    Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Darunavir (Prezista) AUC by ~10.00x

  • contraindicated
    Dasatinib (Sprycel) + Darunavir (Prezista) CYP inhibition

    Dasatinib (Sprycel) time_dependent_inhibitor of CYP3A4 predicted to change Darunavir (Prezista) AUC by ~5.00x

  • contraindicated
    Diltiazem + Darunavir (Prezista) CYP inhibition

    Diltiazem mechanism_based of CYP3A4 predicted to change Darunavir (Prezista) AUC by ~10.00x

  • contraindicated
    Efavirenz (Sustiva) + Darunavir (Prezista) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Darunavir (Prezista) AUC by ~0.12x

  • contraindicated
    Grapefruit (whole fruit) + Darunavir (Prezista) CYP inhibition

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

Serum checks 327 modeled interaction pairings for darunavir (prezista) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. The pharmacokinetics of the HIV protease inhibitor darunavir Back D et al. · Clinical Pharmacokinetics, 2008 DOI

    PK review detailing darunavir's CYP3A4 metabolism, ritonavir-boosted exposure, food effect, and tissue distribution supporting QD/BID dosing.

  2. Clinical pharmacology perspective of cobicistat-boosted darunavir Kakuda TN et al. · Journal of Clinical Pharmacology, 2014 DOI

    Compares cobicistat vs ritonavir boosting of darunavir, showing bioequivalent exposure and supporting once-daily 800/150 mg regimen.

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