Lenacapavir Sodium

China [CN]

Lenacapavir Sodium is the world's first approved HIV-1 capsid inhibitor, a long-acting, subcutaneously administered drug for the treatment of multidrug-resistant HIV-1 infection and HIV pre-exposure prophylaxis (PrEP).

I. Basic Information

Generic Name: Lenacapavir Sodium

English Name: Lenacapavir Sodium

CAS: 2138403-61-1

Molecular Formula: C₃₉H₃₁ClF₁₀N₇NaO₅S₂

Molecular Weight: 998.27

Category: HIV-1 Capsid Inhibitor

Original Developer: Gilead

Dosage Forms: Tablets, Injection

Administration: Subcutaneous injection once every 6 months (long-acting)

II. Mechanism of Action

Binds to the HIV-1 capsid protein (p24), blocking viral replication at multiple stages:

Inhibits viral DNA entry into the cell nucleus

Prevents viral core disassembly

Interferes with viral particle assembly

No cross-resistance with existing anti-HIV drugs.

III. Indications

Treatment: Adult multidrug-resistant HIV-1 infection (in combination with other antiretroviral drugs).

Prevention: Adult/adolescent (≥35 kg) HIV pre-exposure prophylaxis (PrEP).

IV. Dosage and Administration

Loading Dose: Oral 300 mg once daily for 14 days or a single subcutaneous injection of 600 mg.

Maintenance Dose: Subcutaneous injection of 600 mg every 6 months.

V. Adverse Reactions

Common: Injection site reactions, headache, nausea, fatigue.

Important Warnings:

HBsAg-positive individuals require monitoring for hepatitis B reactivation.

Contraindicated with strong CYP3A inducers (e.g., rifampicin).

Must not be used as monotherapy; must be used in combination therapy.