Elvitegravir
drugOn this page
Also known as Elvitegravir component of genvoyaElvitegravir component of stribildElvitegravir component of vitektaGS-9137JTK-303VitektaELVITEGRAVIR (GS-9137)
Summary
Elvitegravir (CHEMBL204656) is an approved small-molecule HIV-1 integrase inhibitor (ATC J05AJ02); indicated across 5 conditions including hiv infectious disease and viral infectious disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: J05AJ02
- Indications: 5 conditions
- Clinical trials: 11
- Chemistry: 447.9 Da · C23H23ClFNO5
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL204656 |
| Name | Elvitegravir |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 5277135 |
| ChEBI | CHEBI:72289 |
| ATC | J05AJ02 |
| Molecular formula | C23H23ClFNO5 |
| Molecular weight | 447.9 |
| InChIKey | JUZYLCPPVHEVSV-LJQANCHMSA-N |
SMILES: CC(C)[C@@H](CO)N1C=C(C(=O)C2=C1C=C(C(=C2)CC3=C(C(=CC=C3)Cl)F)OC)C(=O)O
IUPAC name: 6-[(3-chloro-2-fluorophenyl)methyl]-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid
ChEBI definition: A quinolinemonocarboxylic acid that is 7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid substited at position 1 by a 1-hydroxy-3-methylbutan-2-yl group and at position 6 by a 3-chloro-2-fluorobenzyl group (the S-enantiomer). It is used in combination therapy for the treatment of HIV-1 infection.
Pharmacological roles (ChEBI): HIV-1 integrase inhibitor.
Also known as: Elvitegravir, Elvitegravir component of genvoya, Elvitegravir component of stribild, Elvitegravir component of vitekta, GS-9137, JTK-303, Vitekta, elvitegravir, ELVITEGRAVIR, ELVITEGRAVIR (GS-9137), Elvitegravir (GS-9137)
Patent coverage: 1,166 distinct patent families (2,944 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,940 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: N6-adenosine-methyltransferase catalytic subunit.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| METTL3 | 8.32 | Kd | 4.79 | nM | CHEMBL_ACT_25528199 |
| METTL3 | 8.32 | Kd | 4.8 | nM | CHEMBL_ACT_26037632 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
5 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| HIV infectious disease | 4 | MONDO:0005109 | EFO:0000180 |
| viral infectious disease | 4 | MONDO:0005108 | EFO:0000763 |
| AIDS | 3 | MONDO:0012268 | EFO:0000765 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 11.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 4 |
| PHASE4 | 3 |
| PHASE1 | 2 |
| PHASE3 | 1 |
| PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT02198443 | PHASE4 | COMPLETED | Comparison of Two Combinations in Antiretroviral Post-Exposure Prophylaxis for HIV-1: Tenofovir/Emtricitabine (Truvada ®) + Lopinavir/Ritonavir (Kaletra ®) vs Tenofovir/Emtricitabine/Cobicistat/Elvitegravir (Stribild ®). Prospective, Randomized, Open. |
| NCT02351908 | PHASE4 | COMPLETED | Renal Integrase Study |
| NCT02470650 | PHASE4 | WITHDRAWN | Cost-effectiveness of Different Antiretroviral Treatment in Patients HIV Naive |
| NCT00708162 | PHASE3 | COMPLETED | Multicenter, Randomized, Double-Blind, Double-Dummy, Phase 3 Study of the Safety and Efficacy of Elvitegravir Versus Raltegravir |
| NCT02859558 | PHASE2 | COMPLETED | Early ART to Limit Infection and Establishment of Reservoir |
| NCT02203461 | PHASE1 | COMPLETED | Changes in Insulin Resistance in Healthy Volunteers on STRIBILD® Medication |
| NCT02475135 | PHASE1 | COMPLETED | Relative Bioavailability and Food Effect for Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide Fixed Dose Combination |
| NCT00042289 | Not specified | COMPLETED | Pharmacokinetic Study of Antiretroviral Drugs and Related Drugs During and After Pregnancy |
| NCT02882230 | Not specified | TERMINATED | Evaluation of Neurologic and Psychiatric Adverse Events of Several Antiretroviral Drugs in Real Life Setting |
| NCT03405194 | Not specified | WITHDRAWN | Same-Day Treatment With Genvoya vs. EFV/TDF/3TC |
| NCT03425994 | Not specified | UNKNOWN | Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide as Maintenance Treatment for HIV/HBV-coinfection |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Diseases: HIV infectious disease, viral infectious disease, AIDS