Drug intelligence / Profile preview

long-acting injectable antiretroviral

Development stage
Unknown
Lead developer
Bostal Pharma
Modality
Small Molecules
Administration
Intramuscular, Subcutaneous
01

Overview

Bostal Pharma's long-acting injectable antiretroviral (also known as HIV LAI, 12M) is an investigational 12-month long-acting injectable formulation of bictegravir, an integrase strand transfer inhibitor (INSTI), being developed for the treatment of HIV-1 infection. Bictegravir works by binding to the active site of the HIV-1 integrase enzyme and blocking the strand transfer step of retroviral DNA integration, which is essential for the viral replication cycle. By utilizing a long-acting injectable formulation, this therapy aims to provide sustained therapeutic drug levels for up to 12 months, potentially improving patient adherence and treatment outcomes compared to daily oral regimens. The drug is currently in Phase 2/3 clinical development.

Other names
Bictegravir LAIBictegravir LAI 12MBictegravir long-acting injectableHIV LAI, 12M
02

Targets

CYP3A4 (Cytochrome P450 3A4)ORM1 (Alpha-1-acid glycoprotein 1)UGT1A1 (UDP-glucuronosyltransferase 1A1)Integrase allosteric pocket (HIV)

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