Darunavir
PREZISTA
Pronunciation: da-ROON-a-veer (pre-ZIS-ta)
What it isHIV protease inhibitor; treatment-experienced and first-line HIV.
Why this oneThe highest resistance barrier of the protease inhibitors, so it holds up against resistant virus.
What limits itIt requires ritonavir or cobicistat boosting, bringing CYP3A4 interactions. Rash; it is a sulfonamide.
FDA-approved for
- HIV infection (2006)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 infection (with ritonavir + other ARVs) — treatment-naïve, or experienced with no darunavir RAMs | Adults | 800 mg + ritonavir 100 mg QD with food | 800 mg + ritonavir 100 mg QD | 800 mg QD |
| HIV-1 infection — treatment-experienced with ≥1 darunavir RAM (or no genotype) | Adults | 600 mg + ritonavir 100 mg BID with food | 600 mg + ritonavir 100 mg BID | 600 mg BID |
| HIV-1 infection during pregnancy | Pregnant adults | 600 mg + ritonavir 100 mg BID with food | 600 mg + ritonavir 100 mg BID | 600 mg BID |
| HIV-1 infection — treatment-naïve or no darunavir RAMs | Peds 3–<18 y, ≥10 kg | 10–<15 kg: 35 mg/kg + ritonavir 7 mg/kg QD (suspension); 15–<30 kg: 600 mg + RTV 100 mg QD; 30–<40 kg: 675 mg + RTV 100 mg QD; ≥40 kg: 800 mg + RTV 100 mg QD | weight-band dose QD with food | Adult dose (800 mg QD) |
| HIV-1 infection — treatment-experienced with ≥1 darunavir RAM | Peds 3–<18 y, ≥10 kg | 10–<15 kg: 20 mg/kg + ritonavir 3 mg/kg BID (suspension); 15–<30 kg: 375 mg + RTV 48 mg BID; 30–<40 kg: 450 mg + RTV 60 mg BID; ≥40 kg: 600 mg + RTV 100 mg BID | weight-band dose BID with food | Adult dose (600 mg BID) |
Renal No adjustment specified; PK not significantly affected in moderate impairment (CrCl 30–60); no data in severe/ESRD; unlikely removed by dialysis.
Hepatic Mild–moderate: no adjustment; severe: not recommended (no data).
Pregnancy: 800 mg + RTV 100 mg QD only for patients already stable and suppressed (HIV-1 RNA <50) pre-pregnancy. Not recommended <3 y (juvenile rat toxicity). See ritonavir label for its contraindications/ARs.
Instructions
- Must be co-administered with ritonavir and with food.
- Oral suspension (100 mg/mL) for patients unable to swallow tablets; shake well; give an 8 mL dose as two 4 mL administrations with the dosing syringe.
- Genotypic/phenotypic testing recommended in treatment-experienced patients; check liver tests before and during therapy.
Available strengths
- tab 75, 150, 300, 400, 600, 800 mg
- susp 100 mg/mL
Contraindications
- CYP3A-dependent narrow-therapeutic-index drugs: alfuzosin; colchicine (renal/hepatic impairment); lurasidone, pimozide; dronedarone, ivabradine, ranolazine; ergot derivatives; lomitapide, lovastatin, simvastatin; naloxegol; sildenafil for PAH; oral midazolam, triazolam
- Rifampin or St. John's wort (reduced darunavir efficacy)
- Elbasvir/grazoprevir
- Ritonavir contraindications also apply
Cautions
- Must co-administer with ritonavir and food
- Hepatotoxicity (drug-induced hepatitis; monitor LFTs)
- Severe skin reactions (SJS/TEN, DRESS, AGEP)
- Sulfonamide allergy
- Serious drug interactions (CYP3A)
- Diabetes mellitus/hyperglycemia
- Fat redistribution
- Immune reconstitution syndrome
- Increased bleeding in hemophilia
- Not recommended in children <3 years
Adverse reactions
- Diarrhea
- Nausea
- Rash
- Headache
- Abdominal pain
- Vomiting
Pregnancy Limited APR data show no significant increase in major birth defects vs background; exposures lower in pregnancy, so 600 mg + ritonavir 100 mg BID is recommended.
Lactation Do not breastfeed (HIV transmission, resistance, infant ARs); darunavir present in rat milk, no human data.
Cost
| Strength | #/mo | generic $ | CostPlus | |
|---|---|---|---|---|
| 75 mg | tab | 30 qd | not offered | |
| 150 mg | tab | 30 qd | not offered | |
| 300 mg | tab | 30 qd | not offered | |
| 400 mg | tab | 30 qd | not offered | |
| 600 mg | tab | 30 qd | $34.89/mo | offered |
| 800 mg | tab | 30 qd | $71.46/mo | not offered |
| 100 mg/mL | susp | per unit | not offered |
Generic entry2026
NO BOXED WARNINGS
Principal riskBoosting brings CYP3A4 interactions; it is a sulfonamide
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.