elvitegravir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals | 4300 | 697761-98-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Elvitegravir inhibits the strand transfer activity of HIV-1 integrase (integrase strand transfer inhibitor; INSTI), an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the viral infection. Elvitegravir does not inhibit human topoisomerases I or II.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 27, 2012 | FDA | GILEAD SCIENCES INC | |
| March 25, 2013 | PMDA | Japan Tobacco Inc. | |
| May 24, 2013 | EMA | Gilead Sciences Ireland UC |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Renal dysplasia | 89.52 | 78.77 | 10 | 117 | 238 | 63488657 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Renal dysplasia | 54.18 | 46.94 | 6 | 337 | 56 | 79743989 |
| Drug resistance | 47.30 | 46.94 | 14 | 329 | 42199 | 79701846 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AJ02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Integrase inhibitors |
| ATC | J05AR09 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations |
| ATC | J05AR18 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations |
| FDA MoA | N0000000127 | HIV Integrase Inhibitors |
| MeSH PA | D019380 | Anti-HIV Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D044966 | Anti-Retroviral Agents |
| MeSH PA | D000998 | Antiviral Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D019429 | Integrase Inhibitors |
| FDA EPC | N0000175887 | Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor |
| FDA MoA | N0000185507 | Cytochrome P450 2C9 Inducers |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Human immunodeficiency virus infection | indication | 86406008 | DOID:526 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.37 | acidic |
| pKa2 | 12.88 | acidic |
| pKa3 | 3.44 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 150MG;150MG;200MG;300MG | STRIBILD | GILEAD SCIENCES INC | N203100 | Aug. 27, 2012 | RX | TABLET | ORAL | 8592397 | Jan. 13, 2024 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;300MG | STRIBILD | GILEAD SCIENCES INC | N203100 | Aug. 27, 2012 | RX | TABLET | ORAL | 8716264 | Jan. 13, 2024 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;300MG | STRIBILD | GILEAD SCIENCES INC | N203100 | Aug. 27, 2012 | RX | TABLET | ORAL | 9457036 | Jan. 13, 2024 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;300MG | STRIBILD | GILEAD SCIENCES INC | N203100 | Aug. 27, 2012 | RX | TABLET | ORAL | 9744181 | Jan. 13, 2024 | TREATMENT OF HIV INFECTION |
| 150MG | VITEKTA | GILEAD SCIENCES INC | N203093 | Sept. 24, 2014 | DISCN | TABLET | ORAL | 7176220 | Aug. 27, 2026 | TREATMENT OF HIV INFECTION |
| 85MG | VITEKTA | GILEAD SCIENCES INC | N203093 | Sept. 24, 2014 | DISCN | TABLET | ORAL | 7176220 | Aug. 27, 2026 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;300MG | STRIBILD | GILEAD SCIENCES INC | N203100 | Aug. 27, 2012 | RX | TABLET | ORAL | 7176220 | Aug. 27, 2026 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;EQ 10MG BASE | GENVOYA | GILEAD SCIENCES INC | N207561 | Nov. 5, 2015 | RX | TABLET | ORAL | 7176220 | Aug. 27, 2026 | TREATMENT OF HIV INFECTION |
| 150MG | VITEKTA | GILEAD SCIENCES INC | N203093 | Sept. 24, 2014 | DISCN | TABLET | ORAL | 7635704 | Oct. 26, 2026 | TREATMENT OF HIV INFECTION |
| 85MG | VITEKTA | GILEAD SCIENCES INC | N203093 | Sept. 24, 2014 | DISCN | TABLET | ORAL | 7635704 | Oct. 26, 2026 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;300MG | STRIBILD | GILEAD SCIENCES INC | N203100 | Aug. 27, 2012 | RX | TABLET | ORAL | 7635704 | Oct. 26, 2026 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;EQ 10MG BASE | GENVOYA | GILEAD SCIENCES INC | N207561 | Nov. 5, 2015 | RX | TABLET | ORAL | 7635704 | Oct. 26, 2026 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;300MG | STRIBILD | GILEAD SCIENCES INC | N203100 | Aug. 27, 2012 | RX | TABLET | ORAL | 8148374 | Sept. 3, 2029 | TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE |
| 150MG;150MG;200MG;300MG | STRIBILD | GILEAD SCIENCES INC | N203100 | Aug. 27, 2012 | RX | TABLET | ORAL | 9891239 | Sept. 3, 2029 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;EQ 10MG BASE | GENVOYA | GILEAD SCIENCES INC | N207561 | Nov. 5, 2015 | RX | TABLET | ORAL | 8148374 | Sept. 3, 2029 | TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE |
| 150MG;150MG;200MG;EQ 10MG BASE | GENVOYA | GILEAD SCIENCES INC | N207561 | Nov. 5, 2015 | RX | TABLET | ORAL | 9891239 | Sept. 3, 2029 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;300MG | STRIBILD | GILEAD SCIENCES INC | N203100 | Aug. 27, 2012 | RX | TABLET | ORAL | 8633219 | April 30, 2030 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;EQ 10MG BASE | GENVOYA | GILEAD SCIENCES INC | N207561 | Nov. 5, 2015 | RX | TABLET | ORAL | 8633219 | April 30, 2030 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;EQ 10MG BASE | GENVOYA | GILEAD SCIENCES INC | N207561 | Nov. 5, 2015 | RX | TABLET | ORAL | 8754065 | Aug. 15, 2032 | TREATMENT OF HIV INFECTION |
| 150MG;150MG;200MG;EQ 10MG BASE | GENVOYA | GILEAD SCIENCES INC | N207561 | Nov. 5, 2015 | RX | TABLET | ORAL | 9296769 | Aug. 15, 2032 | TREATMENT OF HIV INFECTION |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Integrase | Enzyme | INHIBITOR | IC50 | 8.14 | CHEMBL | CHEMBL | |||
| Gag-Pol polyprotein | Polyprotein | IC50 | 8 | WOMBAT-PK | |||||
| Reverse transcriptase/RNaseH | Enzyme | IC50 | 4.04 | CHEMBL | |||||
| Reverse transcriptase | Enzyme | IC50 | 4.04 | CHEMBL | |||||
| Integrase | Enzyme | IC50 | 8.75 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4031665 | VUID |
| N0000185512 | NUI |
| D06677 | KEGG_DRUG |
| 4031665 | VANDF |
| CHEBI:72289 | CHEBI |
| ELV | PDB_CHEM_ID |
| CHEMBL204656 | ChEMBL_ID |
| C509700 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11574 | IUPHAR_LIGAND_ID |
| 8871 | INN_ID |
| DB09101 | DRUGBANK_ID |
| 4GDQ854U53 | UNII |
| 1306286 | RXNORM |
| 28749 | MMSL |
| d07898 | MMSL |
| 014621 | NDDF |
| 708828000 | SNOMEDCT_US |
| 714795001 | SNOMEDCT_US |
| C2606637 | UMLSCUI |
| 5277135 | PUBCHEM_CID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Stribild | HUMAN PRESCRIPTION DRUG LABEL | 4 | 53808-0887 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 30 sections |
| Stribild | HUMAN PRESCRIPTION DRUG LABEL | 4 | 61958-1201 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 31 sections |
| Stribild Access | HUMAN PRESCRIPTION DRUG LABEL | 4 | 61958-1202 | TABLET, FILM COATED | 150 mg | ORAL | Export only | 32 sections |
| Stribild Access | HUMAN PRESCRIPTION DRUG LABEL | 4 | 61958-1202 | TABLET, FILM COATED | 150 mg | ORAL | Export only | 32 sections |
| Genvoya | HUMAN PRESCRIPTION DRUG LABEL | 4 | 61958-1901 | TABLET | 150 mg | ORAL | NDA | 32 sections |
| Stribild | HUMAN PRESCRIPTION DRUG LABEL | 4 | 69189-1201 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 30 sections |
| Genvoya | HUMAN PRESCRIPTION DRUG LABEL | 4 | 70518-0568 | TABLET | 150 mg | ORAL | NDA | 31 sections |