Drug intelligence / Profile preview

bictegravir + lenacapavir

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral, Injectable
01

Overview

Bictegravir + lenacapavir is an investigational fixed-dose combination antiretroviral regimen for the treatment of HIV-1 infection. Bictegravir is an integrase strand transfer inhibitor (INSTI) that blocks the integration of viral DNA into the host genome, a critical step in HIV replication. Lenacapavir is a first-in-class capsid inhibitor that interferes with multiple stages of the HIV-1 life cycle by binding to the capsid protein p24, thereby inhibiting nuclear import of proviral DNA and disrupting proper assembly and disassembly of viral particles. This combination aims to simplify therapy for people with HIV who are virologically suppressed on complex regimens or have resistance/intolerance to other therapies. It is being developed as both oral and long-acting injectable formulations[1][2][3][5][6].

Other names
BIC + LENbictegravir + lenacapavirBIC/LEN
02

Targets

p24 (HIV-1 capsid protein p24)Integrase allosteric pocket (HIV)

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