Clinical data | |
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Trade names | Sunlenca |
Other names | GS-CA1, GS-6207 |
License data |
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Pregnancy category |
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Routes of administration | By mouth, subcutaneous |
Drug class | Capsid inhibitors |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
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CAS Number | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
PDB ligand | |
Chemical and physical data | |
Formula | C39H32ClF10N7O5S2 |
Molar mass | 968.28 g·mol−1 |
3D model ( JSmol) | |
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Lenacapavir, sold under the brand name Sunlenca, is an antiretroviral medication used to treat HIV/AIDS. [10] It is taken by mouth or by subcutaneous injection. [10]
The most common side effects include reactions at the injection site and nausea. [10] [11]
Lenacapavir was approved for medical use in the European Union in August 2022, [10] [12] in Canada in November 2022, [5] [6] and in the United States in December 2022. [11] [13] [14] It is the first of a class of drugs called capsid inhibitors to be FDA-approved for treating HIV/AIDS. [11] [15]
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. [9] [11]
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. [11] [16] The US Food and Drug Administration considers it to be a first-in-class medication. [15] [17]
Lenacapavir was developed by Gilead Sciences. [18]
As of 2021, it is in phase II/III clinical trials. [19] 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. [19] [20]
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. [11] These participants had to have high levels of virus in their blood despite being on antiretroviral drugs. [11] Participants were enrolled into one of two study groups. [11] One group was randomized to receive either lenacapavir or placebo in a double-blind fashion, and the other group received open-label lenacapavir. [11] 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. [11]
As of 2023, lenacapavir was approved by the FDA and EMA for people with limited treatment options. [9] Studies have also been conducted for its use in treatment-naive individuals. [21] 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) [22] as well as lenacapavir with islatravir (a weekly oral regimen). [23]
The U.S. Food and Drug Administration granted the application for lenacapavir priority review, fast track, and breakthrough therapy designations. [11]
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. [24] The applicant for this medicinal product is Gilead Sciences Ireland UC. [24]
Lenacapavir was approved for medical use in the European Union in August 2022, [10] [25] in Canada in November 2022, [5] [6] and in the United States in December 2022. [11]
Clinical data | |
---|---|
Trade names | Sunlenca |
Other names | GS-CA1, GS-6207 |
License data |
|
Pregnancy category |
|
Routes of administration | By mouth, subcutaneous |
Drug class | Capsid inhibitors |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
| |
CAS Number | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
PDB ligand | |
Chemical and physical data | |
Formula | C39H32ClF10N7O5S2 |
Molar mass | 968.28 g·mol−1 |
3D model ( JSmol) | |
| |
|
Lenacapavir, sold under the brand name Sunlenca, is an antiretroviral medication used to treat HIV/AIDS. [10] It is taken by mouth or by subcutaneous injection. [10]
The most common side effects include reactions at the injection site and nausea. [10] [11]
Lenacapavir was approved for medical use in the European Union in August 2022, [10] [12] in Canada in November 2022, [5] [6] and in the United States in December 2022. [11] [13] [14] It is the first of a class of drugs called capsid inhibitors to be FDA-approved for treating HIV/AIDS. [11] [15]
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. [9] [11]
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. [11] [16] The US Food and Drug Administration considers it to be a first-in-class medication. [15] [17]
Lenacapavir was developed by Gilead Sciences. [18]
As of 2021, it is in phase II/III clinical trials. [19] 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. [19] [20]
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. [11] These participants had to have high levels of virus in their blood despite being on antiretroviral drugs. [11] Participants were enrolled into one of two study groups. [11] One group was randomized to receive either lenacapavir or placebo in a double-blind fashion, and the other group received open-label lenacapavir. [11] 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. [11]
As of 2023, lenacapavir was approved by the FDA and EMA for people with limited treatment options. [9] Studies have also been conducted for its use in treatment-naive individuals. [21] 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) [22] as well as lenacapavir with islatravir (a weekly oral regimen). [23]
The U.S. Food and Drug Administration granted the application for lenacapavir priority review, fast track, and breakthrough therapy designations. [11]
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. [24] The applicant for this medicinal product is Gilead Sciences Ireland UC. [24]
Lenacapavir was approved for medical use in the European Union in August 2022, [10] [25] in Canada in November 2022, [5] [6] and in the United States in December 2022. [11]