Rezivertinib
drugOn this page
Also known as Bpi-7711BPI7711
Summary
Rezivertinib (CHEMBL5314952) is a phase-3 clinical-stage small molecule targeting EGFR; indicated across 1 condition including non-small cell lung carcinoma.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (EGFR)
- Indications: 1 condition
- Clinical trials: 6
- Chemistry: 486.6 Da · C27H30N6O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL5314952 |
| Name | Rezivertinib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 118912975 |
| Molecular formula | C27H30N6O3 |
| Molecular weight | 486.6 |
| InChIKey | BPMZUKYFIDPLEA-UHFFFAOYSA-N |
SMILES: CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=CC(=C(C=C4OC)OCCN(C)C)NC(=O)C=C
IUPAC name: N-[2-[2-(dimethylamino)ethoxy]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide
Also known as: Bpi-7711, BPI7711, Rezivertinib, REZIVERTINIB
Patent coverage: 81 distinct patent families (196 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 132 (67%) 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
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| EGFR | epidermal growth factor receptor | Inhibition | 17.5% | P00533 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
Aggregated over 1 target gene(s): EGFR.
Top Reactome pathways
37 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signaling by ERBB2 | 1 | EGFR |
| Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants | 1 | EGFR |
| Signaling by ERBB4 | 1 | EGFR |
| SHC1 events in ERBB2 signaling | 1 | EGFR |
| PLCG1 events in ERBB2 signaling | 1 | EGFR |
| PIP3 activates AKT signaling | 1 | EGFR |
| Signaling by EGFR | 1 | EGFR |
| GRB2 events in EGFR signaling | 1 | EGFR |
| GAB1 signalosome | 1 | EGFR |
| SHC1 events in EGFR signaling | 1 | EGFR |
| EGFR downregulation | 1 | EGFR |
| GRB2 events in ERBB2 signaling | 1 | EGFR |
| PI3K events in ERBB2 signaling | 1 | EGFR |
| EGFR interacts with phospholipase C-gamma | 1 | EGFR |
| EGFR Transactivation by Gastrin | 1 | EGFR |
| Constitutive Signaling by Aberrant PI3K in Cancer | 1 | EGFR |
| Signal transduction by L1 | 1 | EGFR |
| Constitutive Signaling by EGFRvIII | 1 | EGFR |
| Inhibition of Signaling by Overexpressed EGFR | 1 | EGFR |
| RAF/MAP kinase cascade | 1 | EGFR |
| ERBB2 Regulates Cell Motility | 1 | EGFR |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 1 | EGFR |
| ERBB2 Activates PTK6 Signaling | 1 | EGFR |
| Cargo recognition for clathrin-mediated endocytosis | 1 | EGFR |
| Clathrin-mediated endocytosis | 1 | EGFR |
| PTK6 promotes HIF1A stabilization | 1 | EGFR |
| Downregulation of ERBB2 signaling | 1 | EGFR |
| TFAP2 (AP-2) family regulates transcription of growth factors and their receptors | 1 | EGFR |
| Extra-nuclear estrogen signaling | 1 | EGFR |
| NOTCH3 Activation and Transmission of Signal to the Nucleus | 1 | EGFR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cell morphogenesis | 1 |
| ossification | 1 |
| embryonic placenta development | 1 |
| positive regulation of protein phosphorylation | 1 |
| hair follicle development | 1 |
| ubiquitin-dependent protein catabolic process | 1 |
| signal transduction | 1 |
| cell surface receptor signaling pathway | 1 |
| epidermal growth factor receptor signaling pathway | 1 |
| salivary gland morphogenesis | 1 |
| learning or memory | 1 |
| positive regulation of cell population proliferation | 1 |
| gene expression | 1 |
| protein ubiquitination | 1 |
| cerebral cortex cell migration | 1 |
Indications & clinical
Indications
1 indication (0 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 |
|---|---|---|---|
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
Clinical trials
Total trials: 6.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 2 |
| PHASE1 | 2 |
| PHASE1/PHASE2 | 1 |
| PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03866499 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of BPI-7711 Capsule in Non-small Cell Lung Cancer Patients |
| NCT06955325 | PHASE3 | NOT_YET_RECRUITING | Umbrella Trial of Adjuvant Therapy in Completely Resected High-risk Stage IA-IB NSCLC: Focus on Driver Mutations |
| NCT03386955 | PHASE1/PHASE2 | COMPLETED | BPI-7711 Capsule in Patients With EGFR Mutation T790M Positive Non-small Cell Lung Cancer |
| NCT03812809 | PHASE2 | COMPLETED | A Phase IIb Study of BPI-7711 Capsule in Non-small Cell Lung Cancer Patients With T790M Mutation Positive |
| NCT04135820 | PHASE1 | COMPLETED | A Phase I Study to Determine the Effect of Food on the Pharmacokinetic Profile of BPI-7711 |
| NCT04135833 | PHASE1 | COMPLETED | A Phase I Study to Assess the Effect of Itraconazole and Rifampicin on Pharmacokinetics Profile of BPI-7711 |
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
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
158 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AFATINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR |
| SELUMETINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | EGFR |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| AFATINIB DIMALEATE | ChEMBL | Phase 4 (approved) | EGFR |
| ALECTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | EGFR |
| AXITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| BACITRACIN | ChEMBL | Phase 4 (approved) | EGFR |
| BITHIONOL | ChEMBL | Phase 4 (approved) | EGFR |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| CERITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | EGFR |
| CHROMIC CHLORIDE | ChEMBL | Phase 4 (approved) | EGFR |
| CISPLATIN | ChEMBL | Phase 4 (approved) | EGFR |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | EGFR |
| COLISTIN | ChEMBL | Phase 4 (approved) | EGFR |
| CRIZOTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| DACOMITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| DASATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| DOBUTAMINE | ChEMBL | Phase 4 (approved) | EGFR |
| DOCETAXEL | ChEMBL | Phase 4 (approved) | EGFR |
| EBASTINE | ChEMBL | Phase 4 (approved) | EGFR |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | EGFR |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | EGFR |
| GEFITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| GENTIAN VIOLET | ChEMBL | Phase 4 (approved) | EGFR |
| GILTERITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | EGFR |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| IMATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| LAPATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| LAPATINIB DITOSYLATE | ChEMBL | Phase 4 (approved) | EGFR |
| LAZERTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| LEVODOPA | ChEMBL | Phase 4 (approved) | EGFR |
| LORLATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| METHYLDOPA | ChEMBL | Phase 4 (approved) | EGFR |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | EGFR |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | EGFR |
| MITOXANTRONE | ChEMBL | Phase 4 (approved) | EGFR |
| MOBOCERTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| MONTELUKAST | ChEMBL | Phase 4 (approved) | EGFR |
| NELFINAVIR | ChEMBL | Phase 4 (approved) | EGFR |
| NERATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| NICLOSAMIDE | ChEMBL | Phase 4 (approved) | EGFR |
| OLMUTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | EGFR |
| PERHEXILINE | ChEMBL | Phase 4 (approved) | EGFR |
| PONATINIB | ChEMBL | Phase 4 (approved) | EGFR |
| SORAFENIB | ChEMBL | Phase 4 (approved) | EGFR |
| SULOCTIDIL | ChEMBL | Phase 4 (approved) | EGFR |
| SUNITINIB | ChEMBL | Phase 4 (approved) | EGFR |
| TAMOXIFEN | ChEMBL | Phase 4 (approved) | EGFR |
| TERFENADINE | ChEMBL | Phase 4 (approved) | EGFR |
| THIORIDAZINE | ChEMBL | Phase 4 (approved) | EGFR |
| TRIBROMSALAN | ChEMBL | Phase 4 (approved) | EGFR |
Related Atlas pages
- Genes: EGFR
- Diseases: non-small cell lung carcinoma
- Drugs: Afatinib, Selumetinib, Abemaciclib, Acalabrutinib, Alectinib, Astemizole, Axitinib, Bacitracin, Bithionol, Bosutinib, Brigatinib, Cabozantinib, Ceritinib, Chlorpromazine, Chromic Chloride, Cisplatin, Clotrimazole, Colistin, Crizotinib, Dacomitinib, Dasatinib, Dobutamine, Docetaxel, Ebastine, Econazole, Erlotinib, Fedratinib, Fluphenazine, Gefitinib, Gilteritinib, Hexachlorophene, Ibrutinib, Imatinib, Lapatinib, Lazertinib, Levodopa, Lorlatinib, Methyldopa, Miconazole, Midostaurin, Mitoxantrone, Mobocertinib, Montelukast, Nelfinavir, Neratinib, Niclosamide, Olmutinib, Osimertinib, Perhexiline, Ponatinib, Sorafenib, Suloctidil, Sunitinib, Tamoxifen, Terfenadine, Thioridazine, Tribromsalan