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lenacapavir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals | 5704 | 2189684-44-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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).
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.19 | g | O |
| 5.10 | mg | P |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | PDK1,PDK2,PDK4 | 3 | |||
| kinase-selectivity-class | PDK1 | 1 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 |
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)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Injection site discharge | 1053.47 | 99.41 | 123 | 640 | 402 | 42620170 |
| Injection site nodule | 428.14 | 99.41 | 66 | 697 | 2095 | 42618477 |
| Product use in unapproved therapeutic environment | 284.38 | 99.41 | 37 | 726 | 321 | 42620251 |
| Injection site pain | 242.26 | 99.41 | 73 | 690 | 57725 | 42562847 |
| Injection site erythema | 103.50 | 99.41 | 30 | 733 | 20165 | 42600407 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Injection site discharge | 520.53 | 78.30 | 64 | 492 | 1396 | 110587347 |
| Product use in unapproved therapeutic environment | 226.25 | 78.30 | 26 | 530 | 298 | 110588445 |
| Injection site nodule | 207.38 | 78.30 | 33 | 523 | 4613 | 110584130 |
| Injection site pain | 142.06 | 78.30 | 47 | 509 | 177875 | 110410868 |
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 |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000998 | Antiviral Agents |
| MeSH PA | D019380 | Anti-HIV Agents |
| MeSH PA | D044966 | Anti-Retroviral Agents |
| FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| FDA MoA | N0000190114 | Cytochrome P450 3A Inhibitors |
| FDA MoA | N0000194086 | HIV Capsid Inhibitors |
| FDA EPC | N0000194088 | Human Immunodeficiency Virus 1 Capsid Inhibitor |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:64946 | anti-HIV agent |
| CHEBI has role | CHEBI:64947 | anti-HIV-1 agent |
Related Drugs by ATC class:
J05AX Other antivirals 15 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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) | YEZTUGO | GILEAD SCIENCES INC | N220018 | June 18, 2025 | RX | SOLUTION | SUBCUTANEOUS | 9951043 | Feb. 28, 2034 | FOR PRE-EXPOSURE PROPHYLAXIS TO REDUCE THE RISK OF SEXUALLY ACQUIRED HIV-1 IN ADULTS AND ADOLESCENTS WEIGHING AT LEAST 35 KG WHO ARE AT RISK FOR HIV-1 ACQUISITION |
| EQ 300MG BASE | YEZTUGO | GILEAD SCIENCES INC | N220020 | June 18, 2025 | RX | TABLET | ORAL | 9951043 | Feb. 28, 2034 | FOR PRE-EXPOSURE PROPHYLAXIS TO REDUCE THE RISK OF SEXUALLY ACQUIRED HIV-1 IN ADULTS AND ADOLESCENTS WEIGHING AT LEAST 35 KG WHO ARE AT RISK FOR HIV-1 ACQUISITION |
| 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 |
| EQ 463.5MG BASE/1.5ML (EQ 309MG BASE/ML) | YEZTUGO | GILEAD SCIENCES INC | N220018 | June 18, 2025 | RX | SOLUTION | SUBCUTANEOUS | 11807625 | Nov. 25, 2040 | FOR PRE-EXPOSURE PROPHYLAXIS TO REDUCE THE RISK OF SEXUALLY ACQUIRED HIV-1 IN ADULTS AND ADOLESCENTS WEIGHING AT LEAST 35 KG WHO ARE AT RISK FOR HIV-1 ACQUISITION |
| EQ 463.5MG BASE/1.5ML (EQ 309MG BASE/ML) | SUNLENCA | GILEAD SCIENCES INC | N215973 | Dec. 22, 2022 | RX | SOLUTION | SUBCUTANEOUS | 11944611 | Aug. 28, 2041 | 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 | 11944611 | Aug. 28, 2041 | 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 |
| EQ 463.5MG BASE/1.5ML (EQ 309MG BASE/ML) | YEZTUGO | GILEAD SCIENCES INC | N220018 | June 18, 2025 | RX | SOLUTION | SUBCUTANEOUS | Dec. 22, 2027 | NEW CHEMICAL ENTITY |
| EQ 300MG BASE | YEZTUGO | GILEAD SCIENCES INC | N220020 | June 18, 2025 | RX | TABLET | ORAL | Dec. 22, 2027 | NEW CHEMICAL ENTITY |
| EQ 463.5MG BASE/1.5ML (EQ 309MG BASE/ML) | YEZTUGO | GILEAD SCIENCES INC | N220018 | June 18, 2025 | RX | SOLUTION | SUBCUTANEOUS | June 18, 2028 | NEW PRODUCT |
| EQ 300MG BASE | YEZTUGO | GILEAD SCIENCES INC | N220020 | June 18, 2025 | RX | TABLET | ORAL | June 18, 2028 | NEW PRODUCT |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Gag polyprotein | Polyprotein | INHIBITOR | Kd | 8.85 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:234519 | CHEBI |
| QNG | PDB_CHEM_ID |
| CHEMBL4594438 | ChEMBL_ID |
| C000730993 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11446 | IUPHAR_LIGAND_ID |
| DB15673 | DRUGBANK_ID |
| 1351588006 | SNOMEDCT_US |
| 287801000202101 | SNOMEDCT_US |
| 4041942 | VANDF |
| C5244461 | UMLSCUI |
| CHEMBL4802249 | ChEMBL_ID |
| 11108 | INN_ID |
| 2283356-12-5 | SECONDARY_CAS_RN |
| D12161 | KEGG_DRUG |
| 133082658 | PUBCHEM_CID |
| 364535 | MMSL |
| 41171 | MMSL |
| d09962 | MMSL |
| 019243 | NDDF |
| 019244 | NDDF |
| A9A0O6FB4H | UNII |
| 2625651 | RXNORM |
| A9A0O6FB4H | INXIGHT DRUGS |
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 | 33 sections |
| Sunlenca | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61958-3001 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 33 sections |
| Yeztugo | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61958-3401 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 31 sections |
| Yeztugo | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61958-3401 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 31 sections |