Aumolertinib

Summary

Aumolertinib (CHEMBL4761468) is a phase-3 clinical-stage small molecule (ATC L01EB11) targeting EGFR; indicated across 7 conditions including non-small cell lung carcinoma and lung neoplasm; with CIViC clinical evidence for 2 variant-indication associations (e.g. EGFR::MACF1 Fusion in lung adenocarcinoma).

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: L01EB11
• Targets: 1 (EGFR)
• Indications: 7 conditions
• Clinical trials: 54
• Precision-oncology evidence (CIViC): 2 variant–indication associations
• Chemistry: 525.6 Da · C30H35N7O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4761468
Name	Aumolertinib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	121280087
ATC	L01EB11
Molecular formula	C30H35N7O2
Molecular weight	525.6
InChIKey	DOEOECWDNSEFDN-UHFFFAOYSA-N

SMILES: CN(C)CCN(C)C1=CC(=C(C=C1NC(=O)C=C)NC2=NC=CC(=N2)C3=CN(C4=CC=CC=C43)C5CC5)OC

IUPAC name: N-[5-[[4-(1-cyclopropylindol-3-yl)pyrimidin-2-yl]amino]-2-[2-(dimethylamino)ethyl-methylamino]-4-methoxyphenyl]prop-2-enamide

Also known as: Almonertinib, Ameile, Amerol, Aumolertinib, Egfr t790m inhibitor hs-10296, EQ-143, EQ143, Hs 10296, HS-10206, Hs-10296, HS-10296, AUMOLERTINIB

Parent form; salt/anhydrous children: CHEMBL5095491

Patent coverage: 277 distinct patent families (611 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 565 (92%) 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	8.72	17.5%	P00533

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Epidermal growth factor receptor.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
EGFR	9.74	IC50	0.18	nM	CHEMBL_ACT_22814386
EGFR	9.74	IC50	0.18	nM	CHEMBL_ACT_26009387
EGFR	8.54	IC50	2.89	nM	CHEMBL_ACT_22814396
EGFR	8.54	IC50	2.89	nM	CHEMBL_ACT_26009396

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

7 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
lung neoplasm	3	MONDO:0021117	MONDO:0008903
neoplasm	3	MONDO:0005070	EFO:0000616
squamous cell carcinoma	2	MONDO:0005096	EFO:0000707
carcinoma	1	MONDO:0004993	EFO:0000313
liver disorder	1	MONDO:0005154	EFO:0001421

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 54.

Phase distribution

Phase	Trials
PHASE2	24
PHASE3	16
PHASE1/PHASE2	4
PHASE1	4
Not specified	4
PHASE2/PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04687241	PHASE3	ACTIVE_NOT_RECRUITING	Almonertinib Versus Placebo as Adjuvant Therapy in Resected Stage II-IIIB Non-Small Cell Lung Cancer With EGFR-sensitive Mutations
NCT04762459	PHASE3	ENROLLING_BY_INVITATION	Efficacy and Safety of Almonertinib Combined With or Without Chemotherapy as an Adjuvant Treatment for Stage II-IIIA Non-small Cell Lung Carcinoma Following Complete Tumour Resection
NCT04841811	PHASE3	ACTIVE_NOT_RECRUITING	MDT-bridged Radical Therapy After Aumolertinib With MRD-guided Maintenance in EGFRm+ Unresectable Stage III NSCLC (APPROACH)
NCT04923906	PHASE3	ACTIVE_NOT_RECRUITING	Aumolertinib with or Without Chemotherapy As 1st Line Treatment in Locally Advanced or Metastatic Non-Small Cell Lung Cancer with Sensitizing EGFR Mutations
NCT04951635	PHASE3	RECRUITING	A Phase III Study to Assess the Effects of Almonertinib Following Chemoradiation in Patients With Stage III Unresectable Non-small Cell Lung Cancer
NCT05768490	PHASE3	RECRUITING	Early or Delayed Intervention of Brain Radiotherapy Combined With Almonertinib in EGFR Mutated NSCLC With Brain Metastases
NCT05800223	PHASE3	RECRUITING	Armatinib Alone or in Combination With SRT for Brain Metastases EGFR-mutated Non-small Cell Lung Cancer
NCT06043973	PHASE3	RECRUITING	Almonertinib Combined With Anlotinib as First-line Treatment for Advanced Non-small Cell Lung Cance
NCT06417008	PHASE2/PHASE3	RECRUITING	A Study of HS-20117 Combined With Aumolertinib in Participants With Advanced Non-Squamous Non-Small Cell Lung Cancer
NCT07183189	PHASE3	RECRUITING	A Study of SHR-A2009 Combined With Aumolertinib Versus Aumolertinib for First-line Treatment in EGFR-mutated, Advanced or Metastatic NSCLC
NCT03849768	PHASE3	UNKNOWN	A Study to Evaluate Safety and Efficacy of HS-10296 as First-Line Treatment in Patients
NCT04500704	PHASE3	UNKNOWN	Almonertinib Plus Chemotherapy as First-line Treatment in Patients With EGFR Concomitant Non-EGFR Driver Gene Mutant, Locally Advanced or Metastatic NSCLC
NCT04500717	PHASE3	UNKNOWN	Almonertinib Plus Chemotherapy as First-line Treatment in Patients With EGFR Concomitant Tumor Suppressor Gene Mutation
NCT04870190	PHASE3	UNKNOWN	Almonertinib Versus Osimertinib in the Patients With EGFR Mutations in Advanced NSCLC With Brain Metastases
NCT04951648	PHASE3	UNKNOWN	A Phase III Study to Assess the Efficacy and Safety of Almonertinib Versus Platinum-based Chemotherapy as First-line Therapy in Patients With Locally Advanced or Metastatic NSCLC Harbouring Uncommon EGFR Mutation
NCT05493501	PHASE3	TERMINATED	Aumolertinib With Chemotherapy or Alone Compared With Osimertinib in Patients With Epidermal Growth Factor Receptor-Mutant Non-Small Cell Lung Cancer
NCT05994339	PHASE2/PHASE3	UNKNOWN	Radiotherapy Combined With Almonertinib for Stage III EGFR-Mutated Lung Cancer
NCT06110663	PHASE3	UNKNOWN	A Study of HS-10241 Combined With Almonertinib Versus Platinum-based Chemotherapy in Treatment of Advanced NSCLC With MET Amplification After Failure of EGFR-TKI Therapy
NCT04423185	PHASE2	RECRUITING	PLATFORM Study of Precision Medicine for Rare Tumors
NCT04685070	PHASE2	ACTIVE_NOT_RECRUITING	Neoadjuvant HS-10296 (Almonertinib) Therapy for Potential Resectable Stage III EGFR Mutation-Positive Non-small Cell Lung Cancer
NCT05503888	PHASE1/PHASE2	NOT_YET_RECRUITING	Phase Ib/II Study of Almonertinib Combined With SHR-1701 in the Treatment of Relapsed or Advanced Non-small Cell Lung Cancer
NCT05778149	PHASE2	NOT_YET_RECRUITING	Safety and Efficacy of Aumolertinib Combined With Anlotinib as 1st Line Treatment in Advanced Lung Cancer EGFR Mutation With TP53 Co-Mutation
NCT06300424	PHASE2	ACTIVE_NOT_RECRUITING	Neoadjuvant Almonertinib Followed by Chemo-immunotherapy in II-IIIB EGFR-mutant NSCLC
NCT06463171	PHASE2	NOT_YET_RECRUITING	Phase II Trial of Almonertinib Plus Lastet for EGFR+ Non-small Cell Lung Cancer
NCT06474455	PHASE1/PHASE2	RECRUITING	A Phase IB/II Clinical Study of SHR-9839 for Injection Combined With Other Anti-tumor Therapies in Patients With Advanced Solid Tumors
NCT06752408	PHASE2	NOT_YET_RECRUITING	Aumolertinib Versus Osimertinib As First-line Therapy for Patients with EGFR Mutated Locally Advanced or Metastatic Non-small-cell Lung Cancer
NCT06947811	PHASE1/PHASE2	RECRUITING	A Study of Almonertinib Combined With Palbociclib in Patients With Advanced Solid Tumors Harboring KRAS Mutations
NCT06951464	PHASE2	RECRUITING	A Study of BL-B01D1 and Almonertinib in Patients With Resectable EGFR+ Stage II-IIIB NSCLC
NCT02981108	PHASE1/PHASE2	UNKNOWN	A Study to Evaluate Safety, PK and Efficacy of HS-10296 in Patients With NSCLC
NCT04354961	PHASE2	UNKNOWN	Almonertinib as First-line Treatment in Patients With EGFR+ Positive Pulmonary Adenosquamous Carcinoma or Combined Adenocarcinoma and Squamous Cell Carcinoma
NCT04455594	PHASE2	UNKNOWN	Almonertinib Vs. Erlotinib/Chemotherapy for Neo-adjuVant Treatment of Stage IIIA-N2 EGFR-mutated NSCLC
NCT04519983	PHASE2	UNKNOWN	Efficacy of SRT as Salvage Therapy in Patients With Brain Oligo-progression of EGFR-mutant Non-small Cell Lung Cancer After Failure of the Third-generation EGFR-TKIs
NCT04553887	PHASE2	UNKNOWN	Almonertinib as Upfront Treatment for Uncommon EGFR Mutation Harboring Non-Small-Cell Lung Cancer Patients: A Multicenter, Open-Label, Phase II Trial
NCT04592666	PHASE2	UNKNOWN	Almonertinib/Pemetrexed/Carboplatin in EGFR T790M+ Advanced Lung Cancer
NCT04636593	PHASE2	UNKNOWN	A Phase 2 Trial of Almonertinib With Concurrent Radiotherapy in The Treatment of Local Advanced EGFR-mutant NSCLC
NCT04643847	PHASE2	UNKNOWN	A Phase II Trial of Upfront Radiotherapy Plus Almonertinib for Epidermal Growth Factor Receptor(EGFR)-Mutant Non-small-cell Lung Cancer(NSCLC) Patients With Brain Metastases
NCT04785742	PHASE2	UNKNOWN	Almonertinib for Advanced NSCLC Patients With Rare Mutations in EGFR
NCT04808752	PHASE2	UNKNOWN	Almonertinib as First-line Treatment in Patients With EGFR Mutations Positive in Advanced NSCLC With Brain Metastases
NCT04882345	PHASE2	UNKNOWN	Almonertinib Treats Advanced NSCLC Patients With EGFR Mutations Who Are Safety Intolerant After Osimertinib Treatment
NCT04905550	PHASE2	UNKNOWN	Almonertinib Combined With Cerebral Radiation Treat Brain Metastases From EGFR Positive NSCLC

Clinical evidence (CIViC)

Variant × indication × effect (2 predictive associations from 2 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
EGFR::MACF1 Fusion	Lung Adenocarcinoma	Sensitivity/Response	Aumolertinib	CIViC C	EID12365
EGFR::GNAT3 Fusion	Lung Adenocarcinoma	Resistance	Aumolertinib	CIViC C	EID12366

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.

157 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