Abivertinib
drugOn this page
Also known as A610AC-0010Ac0010ACEA100610AvitinibEX-ACEA0010
Summary
Abivertinib (CHEMBL4297865) is a phase-3 clinical-stage small molecule targeting EGFR, BTK, and JAK3; indicated across 3 conditions including non-small cell lung carcinoma and severe acute respiratory syndrome.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 3 (EGFR, BTK, JAK3)
- Indications: 3 conditions
- Clinical trials: 9
- Chemistry: 487.5 Da · C26H26FN7O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL4297865 |
| Name | Abivertinib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 72734520 |
| Molecular formula | C26H26FN7O2 |
| Molecular weight | 487.5 |
| InChIKey | UOFYSRZSLXWIQB-UHFFFAOYSA-N |
SMILES: CN1CCN(CC1)C2=C(C=C(C=C2)NC3=NC4=C(C=CN4)C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)F
IUPAC name: N-[3-[[2-[3-fluoro-4-(4-methylpiperazin-1-yl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]prop-2-enamide
Also known as: A610, Abivertinib, AC-0010, Ac0010, AC0010, ACEA100610, Avitinib, EX-ACEA0010, ABIVERTINIB
Parent form; salt/anhydrous children: CHEMBL4297866, CHEMBL5307684
Patent coverage: 462 distinct patent families (1,194 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 1,106 (93%) 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 | 8.11 | 17.5% | P00533 |
| BTK | Bruton tyrosine kinase | Inhibition | 9.4 | 0.7% | Q06187 |
| JAK3 | Janus kinase 3 | Inhibition | 10.05 | 0.6% | P52333 |
Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Epidermal growth factor receptor, Tyrosine-protein kinase JAK3, Tyrosine-protein kinase JAK1, Tyrosine-protein kinase JAK2, Tyrosine-protein kinase BTK.
Bioactivity
ChEMBL activities: 12 potent at pChembl ≥ 5 of 12 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| JAK3 | 10.04 | IC50 | 0.09 | nM | CHEMBL_ACT_26980111 |
| EGFR | 9.77 | IC50 | 0.17 | nM | CHEMBL_ACT_23243141 |
| BTK | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_26980108 |
| EGFR | 9.24 | IC50 | 0.58 | nM | CHEMBL_ACT_23243147 |
| EGFR | 8.74 | IC50 | 1.8 | nM | CHEMBL_ACT_23243135 |
| EGFR | 8.68 | IC50 | 2.1 | nM | CHEMBL_ACT_23243138 |
| EGFR | 7.68 | IC50 | 21 | nM | CHEMBL_ACT_23243132 |
| LRRK2 | 6.75 | IC50 | 177 | nM | CHEMBL_ACT_25654353 |
| EGFR | 6.55 | IC50 | 279 | nM | CHEMBL_ACT_23243150 |
| LRRK2 | 6.39 | IC50 | 410.3 | nM | CHEMBL_ACT_25654300 |
| JAK2 | 6.3 | IC50 | 501 | nM | CHEMBL_ACT_26980114 |
| JAK1 | 5.49 | IC50 | 3270 | nM | CHEMBL_ACT_26980117 |
Target pathways
Aggregated over 3 target gene(s): EGFR, BTK, JAK3.
Top Reactome pathways
98 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 2 | BTK, JAK3 |
| Disease | 2 | BTK, JAK3 |
| Immune System | 2 | BTK, JAK3 |
| Infectious disease | 2 | BTK, JAK3 |
| RAF/MAP kinase cascade | 2 | EGFR, JAK3 |
| Potential therapeutics for SARS | 2 | BTK, JAK3 |
| SARS-CoV Infections | 2 | BTK, JAK3 |
| Viral Infection Pathways | 2 | BTK, JAK3 |
| Signaling by ERBB2 | 1 | EGFR |
| Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants | 1 | EGFR |
| Signaling by ERBB4 | 1 | EGFR |
| ER-Phagosome pathway | 1 | BTK |
| Antigen processing-Cross presentation | 1 | BTK |
| SHC1 events in ERBB2 signaling | 1 | EGFR |
| PLCG1 events in ERBB2 signaling | 1 | EGFR |
| PIP3 activates AKT signaling | 1 | EGFR |
| Interleukin-7 signaling | 1 | JAK3 |
| Cytokine Signaling in Immune system | 1 | JAK3 |
| Adaptive Immune System | 1 | BTK |
| Toll Like Receptor 4 (TLR4) Cascade | 1 | BTK |
| MyD88:MAL(TIRAP) cascade initiated on plasma membrane | 1 | BTK |
| Toll Like Receptor TLR1:TLR2 Cascade | 1 | BTK |
| Toll Like Receptor TLR6:TLR2 Cascade | 1 | BTK |
| Innate Immune System | 1 | BTK |
| Toll-like Receptor Cascades | 1 | BTK |
| Signaling by EGFR | 1 | EGFR |
| GRB2 events in EGFR signaling | 1 | EGFR |
| GAB1 signalosome | 1 | EGFR |
| SHC1 events in EGFR signaling | 1 | EGFR |
| Toll Like Receptor 2 (TLR2) Cascade | 1 | BTK |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 3 |
| adaptive immune response | 2 |
| negative regulation of interleukin-10 production | 2 |
| intracellular signal transduction | 2 |
| innate immune response | 2 |
| immune system process | 2 |
| 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 |
Indications & clinical
Indications
3 indications (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 |
| severe acute respiratory syndrome | 2 | MONDO:0005091 | MONDO:0100096 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 9.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 4 |
| PHASE1/PHASE2 | 2 |
| PHASE1 | 2 |
| PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03058094 | PHASE3 | WITHDRAWN | A Study Comparing AC0010 and Chemotherapy in Patients With Advanced NSCLC Who Have Progressed Following Prior EGFR TKI |
| NCT02274337 | PHASE1/PHASE2 | UNKNOWN | Safety, Tolerability, Pharmacokinetics and Anti-tumour Activity of AC0010 in Advanced Non Small Cell Lung Cancer |
| NCT02330367 | PHASE1/PHASE2 | UNKNOWN | Safety, Pharmacokinetic and Preliminary Efficacy Study of AC0010 in Patients With EGFR T790M Positive NSCLC |
| NCT03300115 | PHASE2 | UNKNOWN | Clinical Trial of the Efficacy and Safety of AC0010 in the Treatment of EGFR T790M Patients With Advanded NSCLC |
| NCT03574402 | PHASE2 | UNKNOWN | Phase II Umbrella Study Directed by Next Generation Sequencing |
| NCT04440007 | PHASE2 | COMPLETED | Study of the Efficacy and Safety of STI-5656 (Abivertinib Maleate) in Subjects Hospitalized With COVID-19 |
| NCT05361915 | PHASE2 | SUSPENDED | Study to Assess Abivertinib in Combination With Abiraterone in Metastatic Castration Resistant Prostate Cancer |
| NCT03001609 | PHASE1 | COMPLETED | Study to Investigate the Absorption, Metabolism and Excretion of [14C] AC0010 in Patients With Advanced NSCLC |
| NCT03053219 | PHASE1 | COMPLETED | Preliminary Evaluation of Safety and Efficacy by [14C] AC0010 Trail and Subsequent AC0010 Treatment |
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.
227 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AFATINIB | ChEMBL + PubChem | Phase 4 (approved) | BTK, EGFR, JAK3 |
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | BTK, EGFR, JAK3 |
| DACOMITINIB | ChEMBL + PubChem | Phase 4 (approved) | BTK, EGFR, JAK3 |
| MOBOCERTINIB | ChEMBL + PubChem | Phase 4 (approved) | BTK, EGFR, JAK3 |
| Pazopanib | ChEMBL + PubChem | Phase 4 (approved) | BTK, EGFR, JAK3 |
| SELUMETINIB | ChEMBL + PubChem | Phase 4 (approved) | BTK, EGFR, JAK3 |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| CERITINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| DASATINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| NERATINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| ZANUBRUTINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR, JAK3 |
| CANERTINIB | ChEMBL | Phase 3 | BTK, EGFR, JAK3 |
| DOVITINIB | ChEMBL | Phase 3 | BTK, EGFR, JAK3 |
| LESTAURTINIB | ChEMBL | Phase 3 | BTK, EGFR, JAK3 |
| REMIBRUTINIB | ChEMBL | Phase 3 | BTK, EGFR, JAK3 |
| ROCILETINIB | ChEMBL | Phase 3 | BTK, EGFR, JAK3 |
| BRANEBRUTINIB | ChEMBL | Phase 2 | BTK, EGFR, JAK3 |
| CENISERTIB | ChEMBL | Phase 2 | BTK, EGFR, JAK3 |
| PELITINIB | ChEMBL | Phase 2 | BTK, EGFR, JAK3 |
| R-406 | ChEMBL | Phase 2 | BTK, EGFR, JAK3 |
| SPEBRUTINIB | ChEMBL | Phase 2 | BTK, EGFR, JAK3 |
| SU-014813 | ChEMBL | Phase 2 | BTK, EGFR, JAK3 |
| TOZASERTIB | ChEMBL | Phase 2 | BTK, EGFR, JAK3 |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR, JAK3 |
| RITLECITINIB | ChEMBL + PubChem | Phase 4 (approved) | BTK, JAK3 |
| AXITINIB | ChEMBL | Phase 4 (approved) | EGFR, JAK3 |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | BTK, JAK3 |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | EGFR, JAK3 |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | EGFR, JAK3 |
| MITOXANTRONE | ChEMBL | Phase 4 (approved) | BTK, EGFR |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | BTK, JAK3 |
| OLMUTINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR |
| PONATINIB | ChEMBL | Phase 4 (approved) | BTK, EGFR |
| SORAFENIB | ChEMBL | Phase 4 (approved) | EGFR, JAK3 |
| VANDETANIB | ChEMBL | Phase 4 (approved) | BTK, EGFR |
| ALISERTIB | ChEMBL | Phase 3 | BTK, EGFR |
| ALVOCIDIB | ChEMBL | Phase 3 | EGFR, JAK3 |
| CEDIRANIB | ChEMBL | Phase 3 | BTK, EGFR |
| EVOBRUTINIB | ChEMBL | Phase 3 | BTK, EGFR |
| ORELABRUTINIB | ChEMBL | Phase 3 | BTK, EGFR |
| POZIOTINIB | ChEMBL | Phase 3 | BTK, EGFR |
| PYROTINIB | ChEMBL | Phase 3 | BTK, EGFR |
| RUBOXISTAURIN | ChEMBL | Phase 3 | EGFR, JAK3 |
| SARACATINIB | ChEMBL | Phase 3 | BTK, EGFR |
| TESEVATINIB | ChEMBL | Phase 3 | BTK, EGFR |
| TOLEBRUTINIB | ChEMBL | Phase 3 | BTK, EGFR |
| APITOLISIB | ChEMBL | Phase 2 | BTK, EGFR |
| AT-9283 | ChEMBL | Phase 2 | BTK, JAK3 |
| ATUZABRUTINIB | ChEMBL | Phase 2 | BTK, EGFR |
| BMS-919373 | ChEMBL | Phase 2 | BTK, JAK3 |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | BTK, EGFR |
| FORETINIB | ChEMBL | Phase 2 | BTK, EGFR |
| ILORASERTIB | ChEMBL | Phase 2 | BTK, EGFR |
| POSELTINIB | ChEMBL | Phase 2 | BTK, JAK3 |
Related Atlas pages
- Genes: EGFR, BTK, JAK3
- Diseases: non-small cell lung carcinoma
- Drugs: Afatinib, Crizotinib, Dacomitinib, Mobocertinib, Pazopanib, Selumetinib, Acalabrutinib, Bosutinib, Ceritinib, Dasatinib, Fedratinib, Ibrutinib, Neratinib, Osimertinib, Sunitinib, Zanubrutinib, Canertinib, Dovitinib, Lestaurtinib, Remibrutinib, Rociletinib, Gefitinib, Ritlecitinib, Axitinib, Brigatinib, Entrectinib, Erlotinib, Midostaurin, Mitoxantrone, Nintedanib, Olmutinib, Ponatinib, Sorafenib, Vandetanib, Alisertib, Alvocidib, Cediranib, Evobrutinib, Orelabrutinib, Poziotinib, Pyrotinib, Ruboxistaurin, Saracatinib, Tesevatinib, Tolebrutinib