GSK1265744 (sodiuM salt)

China [CN]

Mechanism of Action and Resistance

Mechanism: Inhibits the strand transfer reaction of HIV integrase, preventing viral DNA integration into the host genome and blocking viral replication.

Resistance:  Remains active against resistant strains such as Y143R and Q148K (FC < 6.1), which are resistant to raltegravir; high-level resistance mutations are unlikely to develop with long-term use.

Metabolism: Primarily metabolized by UGT1A1, with no significant CYP450-mediated drug interactions.

Clinical Applications

HIV Infection Treatment

Oral: Used in combination with other antiretroviral drugs, 30mg once daily.

Long-acting injection: 600mg once a month (intramuscular injection), requiring a 1-month oral lead-in period to ensure tolerance.

Pre-exposure Prophylaxis (PrEP)

Long-acting injection: 600mg every two months, used for HIV prevention in high-risk individuals.

Dosage Forms: Film-coated tablets (30mg); long-acting injectable suspension (600mg/3mL).