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fostemsavir

Entry Inhibitor · Antiretroviral

Entry InhibitorAntiretroviral
CDSCO approved
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • AmiodaroneSevereDatabaseDDInter
  • AmisulprideSevereDatabaseDDInter
  • AnagrelideSevereDatabaseDDInter
  • ApalutamideSevereDatabaseDDInter

Mechanism

Fostemsavir is a methylphosphate prodrug that is rapidly hydrolyzed to temsavir. Temsavir binds to the viral envelope protein gp120, preventing its attachment to CD4 and subsequent cell entry.

Indications

heavily treatment-experienced adults with multidrug-resistant HIV-1 infection

Pharmacokinetics

Half-life
7–14
Metabolism
esterases, CYP3A4
Excretion
51% (renal, unchanged)

Side effects

Common
elevations of hepatic transaminases
Serious
  • QTc prolongation

Drug interactions

Amiodarone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amisulpride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Anagrelide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Arsenic Trioxide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Bedaquiline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Bepridil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cabozantinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Carbamazepine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Chloroquine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cisapride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Other Entry Inhibitor drugs

Ask House about fostemsavir

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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team