Lenacapavir

Human Immunodeficiency Virus 1 Capsid Inhibitor — ANTIINFECTIVES FOR SYSTEMIC USE

Key facts

Lenacapavir is an onp drug in the Human Immunodeficiency Virus 1 Capsid Inhibitor class catalogued in DrugCentral. It was first approved by the EMA in 2022. Its mechanism of action is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 3A Inhibitors and HIV Capsid Inhibitors. DrugCentral lists 1 molecular target, including gag. Recorded indications include Multidrug resistant HIV-1 infection.

• Approval status: onp (first approved 2022 by the EMA).
• Drug class: Human Immunodeficiency Virus 1 Capsid Inhibitor.
• Mechanism of action: Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 3A Inhibitors; HIV Capsid Inhibitors.
• Molecular targets: gag (1 listed in DrugCentral).
• Indications: Multidrug resistant HIV-1 infection.
• ATC code: J05AX31 (Other antivirals).
• Molecular formula: C39H32ClF10N7O5S2; molecular weight 968.28 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Multidrug resistant HIV-1 infection

Contraindications (3)

• Co-administration with P-gp inducers
• Co-administration with UGT1A1 inducers
• Drug induction of cytochrome p450 CYP3A enzyme

Mechanism & targets

• Mechanism of action (MoA): Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 3A Inhibitors; HIV Capsid Inhibitors; P-Glycoprotein Inhibitors
• Established pharmacologic class: Human Immunodeficiency Virus 1 Capsid Inhibitor

Molecular targets (1)

Target	Gene	Action	Activity
Gag polyprotein	gag	inhibitor	Kd 8.85

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2022-12-22	PMDA	—	GILEAD SCIENCES
2022-08-17	EMA	—	GILEAD SCIENCES IRELAND UNLIMITED COMPANY

ATC classification

ATC code	Therapeutic hierarchy
J05AX31	ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Other antivirals

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Injection site discharge	1224.9
Product use in unapproved therapeutic environment	543.8
Injection site nodule	515.3
Injection site pain	272.1
Labelled drug-drug interaction medication error	225.0
Off label use	175.1
Product use issue	150.7
Viral load increased	98.8
Injection site erythema	96.0
Injection site mass	94.8
Single component of a two-component product administered	80.9

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Lenacapavir is on its molecule page.

• Molecular formula: C₃₉H₃₂ClF₁₀N₇O₅S₂
• Molecular weight: 968.28 g/mol
• CAS number: 2189684-44-2
• InChIKey: BRYXUCLEHAUSDY-WEWMWRJBSA-N
• PubChem CID: 133082658

[H][C@]12C[C@@]1([H])C(F)(F)C1=C2C(=NN1CC(=O)N[C@@H](CC1=CC(F)=CC(F)=C1)C1=C(C=CC(=N1)C#CC(C)(C)S(C)(=O)=O)C1=CC=C(Cl)C2=C1N(CC(F)(F)F)N=C2NS(C)(=O)=O)C(F)(F)F

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Lenacapavir used for?

DrugCentral lists the following indications for Lenacapavir: Multidrug resistant HIV-1 infection.

How does Lenacapavir work?

Lenacapavir is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 3A Inhibitors and HIV Capsid Inhibitors; its molecular targets in DrugCentral include gag (inhibitor).

When was Lenacapavir first approved?

Lenacapavir was first approved by the EMA in 2022.

What drug class does Lenacapavir belong to?

Lenacapavir is in the Human Immunodeficiency Virus 1 Capsid Inhibitor class.

What is the chemical formula of Lenacapavir?

Lenacapavir has the molecular formula C39H32ClF10N7O5S2 and a molecular weight of 968.28 g/mol.

Sources

• DrugCentral drug card 5704 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL4594438 — compound record and bioactivity
• PubChem CID 133082658 — chemical identifiers
• DrugBank DB15673 — drug record
• FDA UNII A9A0O6FB4H — substance identity
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.