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cabotegravir

Integrase Inhibitor · Antiretroviral

Integrase InhibitorAntiretroviral
CDSCO approved
EXCRETION
not curated
INTERACTIONS
9 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 9
  • CarbamazepineSevereTextbookG&G 14e · p1245-1266
  • RifamycinsSevereTextbookG&G 14e · p1245-1266
  • St John S WortSevereTextbookG&G 14e · p1245-1266
  • OxcarbazepineSevereDatabaseDDInter

Mechanism

Cabotegravir blocks the catalytic activity of the HIV-encoded integrase of HIV-1 and HIV-2, preventing the integration of viral DNA into the host chromosome. It interferes with essential divalent cations in the enzyme’s catalytic core.

Indications

HIV treatment in adults with chronically suppressed plasma HIV RNA who are stable on an antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to cabotegravir or rilpivirine (in combination with LA rilpivirine)HIV prevention

Pharmacokinetics

Half-life
5.6 to 11.5 weeks (injectable nanoformulation)
Protein binding
99.8%
Metabolism
UGT1A1
Excretion
27% (renal, unchanged)

Side effects

Common
injection site reactionspyrexiafatigueheadachemusculoskeletal painhepatotoxicitydepressive symptoms

Drug interactions

Carbamazepine
Severe
Textbook

Decreased cabotegravir plasma concentrations, leading to loss of efficacy.

Should not be coadministered.

Source: G&G 14e · p1245-1266

Rifamycins
Severe
Textbook

Decreased cabotegravir plasma concentrations, leading to loss of efficacy.

Should not be coadministered.

Source: G&G 14e · p1245-1266

St John S Wort
Severe
Textbook

Decreased cabotegravir plasma concentrations, leading to loss of efficacy.

Should not be coadministered.

Source: G&G 14e · p1245-1266

Oxcarbazepine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Phenobarbital
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Phenytoin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Rifabutin
Severe
Database

Drug interaction classified as: others

Source: DDInter

Rifampicin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Rifapentine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

3 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.

Related guidelines

Ask House about cabotegravir

Continue into a citation-backed clinical answer with the drug context already attached.

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