Nelfinavir
VIRACEPT
What it isHIV protease inhibitor; HIV.
Why this oneIt requires no ritonavir boosting, which simplified early regimens.
What limits itDiarrhea in most patients and a low resistance barrier; it is now rarely used. It induces and inhibits CYP3A4.
FDA-approved for
- HIV infection (1997)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 infection | Adults & adolescents ≥13 yr | 1250 mg BID or 750 mg TID with a meal | 1250 mg BID or 750 mg TID | 2500 mg/day |
| HIV-1 infection | Children 2 to <13 yr | 45–55 mg/kg BID or 25–35 mg/kg TID with a meal | weight-based (see label tables) | 2500 mg/day |
Renal Undefined (not established in renal impairment)
Hepatic Mild (Child-Pugh A): no adjustment; do not use in moderate-severe (Child-Pugh B/C)
Instructions
- Take with a meal
- Tablets may be dissolved in a small amount of water if unable to swallow
- Oral powder may be mixed in water/milk/formula (not acidic juice); contains phenylalanine (caution in PKU)
Cautions
- Serious CYP3A-mediated drug interactions
- Do not use in moderate-severe hepatic impairment
- Oral powder contains phenylalanine (phenylketonuria)
- New-onset or worsening diabetes mellitus / hyperglycemia
- Increased bleeding in hemophilia
- Fat redistribution
- Immune reconstitution syndrome
- QTc prolongation / torsades (postmarketing)
Adverse reactions
- Diarrhea
- Nausea
- Rash
- Flatulence
- Leukopenia/neutropenia (pediatric)
- Anorexia (pediatric)
- Abdominal pain (pediatric)
Pregnancy Consider alternative antiretrovirals; hepatic adverse events reported; APR birth-defect signal of uncertain significance
Lactation Do not breastfeed (HIV-1 transmission risk; present in human milk)
NO BOXED WARNINGS
Principal riskDiarrhea in most patients; a low resistance barrier
Cost, est. cash$300–$2,000/month
Generic entryNo US generic
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.
Mechanism of action: Nelfinavir ballicule
