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elvitegravir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.222 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.438 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 71.450 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 14.125 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.090 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.750 | % | High | 1 |
| herg | hERG pIC50 | 4.891 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 36.224 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 110.917 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.740 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,CDK5,EIF2AK3,ERBB2,GRK2,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TGFBR1 | 14 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CDK9,DYRK1B,EIF2AK3,EPHB4,GRK2,MAP2K6,MAPK7,PDK4,PIK3CB,PIK3CD,PIK3CG,PRKDC,STK33,TEK,TGFBR1,TTK | 19 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 2.838 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.887 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 34.594 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.760 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 37.584 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 2.050 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.033 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 64.565 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 16.510 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.640 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 50.350 | uM | High | 1 |
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 | 84.43 | 74.19 | 10 | 182 | 374 | 90627881 |
| Single functional kidney | 76.09 | 74.19 | 9 | 183 | 332 | 90627923 |
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 | 64.81 | 50.05 | 7 | 390 | 62 | 110588840 |
| Single functional kidney | 54.29 | 50.05 | 7 | 390 | 303 | 110588599 |
| Drug interaction | 51.60 | 50.05 | 28 | 369 | 500155 | 110088747 |
| Drug resistance | 50.07 | 50.05 | 15 | 382 | 56359 | 110532543 |
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 | D000890 | Anti-Infective Agents |
| MeSH PA | D000998 | Antiviral Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D019380 | Anti-HIV Agents |
| MeSH PA | D019429 | Integrase Inhibitors |
| MeSH PA | D044966 | Anti-Retroviral Agents |
| FDA EPC | N0000175887 | Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor |
| FDA MoA | N0000185507 | Cytochrome P450 2C9 Inducers |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:50864 | insulin-sensitizing drug |
| CHEBI has role | CHEBI:64946 | anti-HIV agent |
| CHEBI has role | CHEBI:67268 | HIV-1 integrase inhibitor |
Related Drugs by ATC class:
J05AJ Integrase inhibitors 3 drugs
J05AR Antivirals for treatment of HIV infections, combinations 19 drugs
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 | 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 | |||
| Integrase | Enzyme | IC50 | 8.75 | CHEMBL | |||||
| Gag-Pol polyprotein | Polyprotein | IC50 | 8 | WOMBAT-PK | |||||
| Reverse transcriptase/RNaseH | Enzyme | IC50 | 4.04 | CHEMBL | |||||
| Reverse transcriptase | Enzyme | IC50 | 4.04 | 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 |
| DB09101 | DRUGBANK_ID |
| 4GDQ854U53 | UNII |
| 1306286 | RXNORM |
| 28749 | MMSL |
| d07898 | MMSL |
| 014621 | NDDF |
| 708828000 | SNOMEDCT_US |
| 714795001 | SNOMEDCT_US |
| C2606637 | UMLSCUI |
| 8871 | INN_ID |
| 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 |
| 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 |