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Trade names | Sunlenca |
Other names | GS-CA1, GS-6207 |
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Routes of administration | By mouth, subcutaneous |
Drug class | Capsid inhibitors |
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Formula | C39H32ClF10N7O5S2 |
Molar mass | 968.28 g·mol−1 |
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Lenacapavir, sold under the brand name Sunlenca, is an antiretroviral medication used to treat HIV/AIDS.[9] It is taken by mouth or by subcutaneous injection.[9]
The most common side effects include reactions at the injection site and nausea.[9][10]
Lenacapavir was approved for medical use in the European Union in August 2022,[9][11] in Canada in November 2022,[4][5] and in the United States in December 2022.[10][12][13] It is the first of a class of drugs called capsid inhibitors to be FDA-approved for treating HIV/AIDS.[10][14]
Lenacapavir, in combination with other antiretrovirals, is indicated for the treatment of HIV/AIDS. It is used in heavily treatment-experienced adults with multiple drug resistance in whom current antiretroviral therapy is ineffective due to resistance, intolerance or safety considerations.[8][10]
Lenacapavir works by binding directly to the interface between HIV-1 viral capsid protein (p24) subunits in capsid hexamers, interfering with essential steps of viral replication, including capsid-mediated nuclear uptake of HIV-1 proviral DNA, virus assembly and release, production of capsid protein subunits, and capsid core formation.[10][15] The US Food and Drug Administration considers it to be a first-in-class medication.[14][16]
Lenacapavir was developed by Gilead Sciences.[17]
As of 2021, it is in phase II/III clinical trials.[18] It is being investigated as a treatment for HIV patients infected with multidrug-resistant virus and as a twice-yearly injectable for pre-exposure prophylaxis.[18][19]
The safety and efficacy of lenacapavir were established through a multicenter clinical trial with 72 participants whose HIV infections were resistant to multiple classes of HIV medications.[10] These participants had to have high levels of virus in their blood despite being on antiretroviral drugs.[10] Participants were enrolled into one of two study groups.[10] One group was randomized to receive either lenacapavir or placebo in a double-blind fashion, and the other group received open-label lenacapavir.[10] The primary measure of efficacy was the proportion of participants in the randomized study group who achieved a certain level of reduction in virus during the initial 14 days compared to baseline.[10]
As of 2023, lenacapavir was approved by the FDA and EMA for people with limited treatment options.[8] Studies have also been conducted for its use in treatment-naive individuals.[20] For virally suppressed individuals switching treatment, early studies have tested lenacapavir injections in combination with infusions of the broadly neutralising antibodies teropavimab and zinlirvimab (a twice yearly regimen)[21] as well as lenacapavir with islatravir (a weekly oral regimen).[22]
The U.S. Food and Drug Administration granted the application for lenacapavir priority review, fast track, and breakthrough therapy designations.[10]
On 23 June 2022, the Committee for Medicinal Products for Human Use of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Sunlenca, intended for the treatment of adults with multidrug‑resistant human immunodeficiency virus type 1 (HIV‑1) infection.[23] The applicant for this medicinal product is Gilead Sciences Ireland UC.[23]
Lenacapavir was approved for medical use in the European Union in August 2022,[9][24] in Canada in November 2022,[4][5] and in the United States in December 2022.[10]