lenacapavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antivirals	5704	2189684-44-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: lenacapavir lenacapavir sodium sunlenca GS-HIV GS-6207 GS-CA-2 GS-CA2 GS-714207	Lenacapavir is a multistage, selective inhibitor of HIV-1 capsid function that directly binds to the interface between capsid protein (CA) subunits. Lenacapavir inhibits HIV-1 replication by interfering with multiple, essential steps of the viral lifecycle, including capsid-mediated nuclear uptake of HIV-1 proviral DNA (by blocking nuclear import proteins binding to capsid), virus assembly and release (by interfering with Gag/Gag-Pol functioning, reducing production of CA subunits), and capsid core formation (by disrupting the rate of capsid subunit association, leading to malformed capsids). Molecular weight: 968.28 Formula: C39H32ClF10N7O5S2 CLOGP: 3.47 LIPINSKI: 3 HAC: 12 HDO: 2 TPSA: 157.94 ALOGS: -5.43 ROTB: 14 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lenacapavir
lenacapavir sodium
sunlenca
GS-HIV
GS-6207
GS-CA-2
GS-CA2
GS-714207

Lenacapavir is a multistage, selective inhibitor of HIV-1 capsid function that directly binds to the interface between capsid protein (CA) subunits. Lenacapavir inhibits HIV-1 replication by interfering with multiple, essential steps of the viral lifecycle, including capsid-mediated nuclear uptake of HIV-1 proviral DNA (by blocking nuclear import proteins binding to capsid), virus assembly and release (by interfering with Gag/Gag-Pol functioning, reducing production of CA subunits), and capsid core formation (by disrupting the rate of capsid subunit association, leading to malformed capsids).

Molecular weight: 968.28
Formula: C39H32ClF10N7O5S2
CLOGP: 3.47
LIPINSKI: 3
HAC: 12
HDO: 2
TPSA: 157.94
ALOGS: -5.43
ROTB: 14

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Aug. 17, 2022	EMA	GILEAD SCIENCES IRELAND UNLIMITED COMPANY
Dec. 22, 2022	PMDA	GILEAD SCIENCES

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	J05AX31	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Other antivirals

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID
Multidrug resistant HIV-1 infection	indication	40780007
Drug induction of cytochrome p450 CYP3A enzyme	contraindication	423236002
Co-administration with P-gp inducers	contraindication
Co-administration with UGT1A1 inducers	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 463.5MG BASE/1.5ML (EQ 309MG BASE/ML)	SUNLENCA	GILEAD SCIENCES INC	N215973	Dec. 22, 2022	RX	SOLUTION	SUBCUTANEOUS	9951043	Feb. 28, 2034	IN COMBINATION WITH OTHER ANTIRETROVIRAL(S), FOR THE TREATMENT OF HIV-1 INFECTION IN HEAVILY-TREATMENT EXPERIENCED ADULTS WITH MULTIDRUG RESISTANT HIV-1 INFECTION
EQ 300MG BASE	SUNLENCA	GILEAD SCIENCES INC	N215974	Dec. 22, 2022	RX	TABLET	ORAL	9951043	Feb. 28, 2034	IN COMBINATION WITH OTHER ANTIRETROVIRAL(S), FOR THE TREATMENT OF HIV-1 INFECTION IN HEAVILY-TREATMENT EXPERIENCED ADULTS WITH MULTIDRUG RESISTANT HIV-1 INFECTION
EQ 463.5MG BASE/1.5ML (EQ 309MG BASE/ML)	SUNLENCA	GILEAD SCIENCES INC	N215973	Dec. 22, 2022	RX	SOLUTION	SUBCUTANEOUS	10654827	Aug. 17, 2037	IN COMBINATION WITH OTHER ANTIRETROVIRAL(S), FOR THE TREATMENT OF HIV-1 INFECTION IN HEAVILY-TREATMENT EXPERIENCED ADULTS WITH MULTIDRUG RESISTANT HIV-1 INFECTION
EQ 300MG BASE	SUNLENCA	GILEAD SCIENCES INC	N215974	Dec. 22, 2022	RX	TABLET	ORAL	10654827	Aug. 17, 2037	IN COMBINATION WITH OTHER ANTIRETROVIRAL(S), FOR THE TREATMENT OF HIV-1 INFECTION IN HEAVILY-TREATMENT EXPERIENCED ADULTS WITH MULTIDRUG RESISTANT HIV-1 INFECTION

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 463.5MG BASE/1.5ML (EQ 309MG BASE/ML)	SUNLENCA	GILEAD SCIENCES INC	N215973	Dec. 22, 2022	RX	SOLUTION	SUBCUTANEOUS	Dec. 22, 2027	NEW CHEMICAL ENTITY
EQ 300MG BASE	SUNLENCA	GILEAD SCIENCES INC	N215974	Dec. 22, 2022	RX	TABLET	ORAL	Dec. 22, 2027	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Gag polyprotein	Enzyme		GAG_HV1N5	INHIBITOR	Kd	8.85		DRUG LABEL	DRUG LABEL

External reference:

ID	Source
QNG	PDB_CHEM_ID
CHEMBL4594438	ChEMBL_ID
11446	IUPHAR_LIGAND_ID
DB15673	DRUGBANK_ID
019243	NDDF
019244	NDDF
4041942	VANDF
C5244461	UMLSCUI
CHEMBL4802249	ChEMBL_ID
11108	INN_ID
2283356-12-5	SECONDARY_CAS_RN
D12161	KEGG_DRUG
133082658	PUBCHEM_CID
2625651	RXNORM
364535	MMSL
41171	MMSL
d09962	MMSL
A9A0O6FB4H	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Sunlenca	HUMAN PRESCRIPTION DRUG LABEL	1	61958-3001	TABLET, FILM COATED	300 mg	ORAL	NDA	31 sections