Fostemsavir
RUKOBIA
What it isgp120 attachment inhibitor prodrug; multidrug-resistant HIV.
Why this oneIt blocks viral attachment, a step no other class targets, so it works against fully resistant virus.
What limits itReserved for heavily treatment-experienced patients. QT prolongation; strong inducers are contraindicated.
FDA-approved for
- multidrug-resistant HIV-1 infection (2020)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| HIV-1 (heavily treatment-experienced, multidrug-resistant) | Adults | 600 mg BID | 600 mg BID | 600 mg BID |
Renal Undefined
Hepatic Undefined
Instructions
- Swallow tablets whole; do not chew, crush, or split
- Take with or without food
Contraindications
- Coadministration with strong CYP3A inducers (e.g., carbamazepine, phenytoin, rifampin, enzalutamide, mitotane, St John's wort) — may cause loss of virologic response
Cautions
- Immune reconstitution syndrome
- QTc prolongation — caution with QT history, cardiac disease, or drugs prolonging QT
- Hepatic transaminase elevations in HBV/HCV co-infection
Adverse reactions
- Nausea
Pregnancy Insufficient human data; no adverse developmental effects in animals at clinically relevant exposures
Lactation Unknown if present in human milk; breastfeeding not recommended in HIV-1
NO BOXED WARNINGS
Principal riskQT prolongation
Cost, est. cash$1,000–$30,000/month or course
Generic entry2029 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.
Active metabolites
Mechanism of action: Fostemsavir ballicule
