Olmutinib

Summary

Olmutinib (CHEMBL3786343) is an approved small molecule (ATC L01EB06) targeting EGFR; indicated across 2 conditions including neoplasm and non-small cell lung carcinoma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EB06
• Targets: 1 (EGFR)
• Indications: 2 conditions
• Clinical trials: 6
• Chemistry: 486.6 Da · C26H26N6O2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3786343
Name	Olmutinib
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	54758501
ATC	L01EB06
Molecular formula	C26H26N6O2S
Molecular weight	486.6
InChIKey	FDMQDKQUTRLUBU-UHFFFAOYSA-N

SMILES: CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)SC=C4

IUPAC name: N-[3-[2-[4-(4-methylpiperazin-1-yl)anilino]thieno[3,2-d]pyrimidin-4-yl]oxyphenyl]prop-2-enamide

Also known as: BI 1482694, BI-1482694, Hm-61713, HM-61713, HM61713, Olmutinib, OLMUTINIB, Olmitunib, olmutinib

Parent form; salt/anhydrous children: CHEMBL3989930

Patent coverage: 737 distinct patent families (1,776 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 1,496 (84%) 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	7	17.5%	P00533

Broader ChEMBL bioactivity targets: 21 (assay-derived). Sample: Alpha-2A adrenergic receptor, Epidermal growth factor receptor, D(1A) dopamine receptor, Estrogen receptor, Thromboxane A2 receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter, Alpha-1A adrenergic receptor.

Bioactivity

ChEMBL activities: 27 potent at pChembl ≥ 5 of 30 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
EGFR	9.05	IC50	0.9	nM	CHEMBL_ACT_22968056
BTK	9	IC50	1	nM	CHEMBL_ACT_16606453
ADORA3	8.52	AC50	3	nM	CHEMBL_ACT_25198577
EGFR	8.04	IC50	9.2	nM	CHEMBL_ACT_24862042
EGFR	8.04	IC50	9.2	nM	CHEMBL_ACT_26039770
EGFR	8	IC50	10	nM	CHEMBL_ACT_16532776
EGFR	8	IC50	10	nM	CHEMBL_ACT_24862043
EGFR	7.9	IC50	12.7	nM	CHEMBL_ACT_22894494
EGFR	7.75	IC50	18	nM	CHEMBL_ACT_18415118
EGFR	7.41	IC50	39	nM	CHEMBL_ACT_22968077
EGFR	7.32	IC50	48	nM	CHEMBL_ACT_22894486
SLC6A3	7.25	AC50	55.9	nM	CHEMBL_ACT_25124779
Q01827	6.36	AC50	440	nM	CHEMBL_ACT_25197345
DRD3	6.34	AC50	453.5	nM	CHEMBL_ACT_25194347
KCNH2	6.27	AC50	540	nM	CHEMBL_ACT_25117300
ADRA2A	6.05	AC50	881.2	nM	CHEMBL_ACT_25156249
HRH3	6.03	AC50	940	nM	CHEMBL_ACT_25199352
CHRM2	5.78	AC50	1643	nM	CHEMBL_ACT_25195556
EGFR	5.7	IC50	2000	nM	CHEMBL_ACT_18415143
KDR	5.69	AC50	2058	nM	CHEMBL_ACT_25168098
CHRM1	5.64	AC50	2286	nM	CHEMBL_ACT_25210057
HTR1A	5.61	AC50	2443	nM	CHEMBL_ACT_25164844
PDE4A	5.5	AC50	3187	nM	CHEMBL_ACT_25206907
DRD1	5.42	AC50	3811	nM	CHEMBL_ACT_25115030
TBXA2R	5.36	AC50	4354	nM	CHEMBL_ACT_25197681
ADRA1A	5.31	AC50	4915	nM	CHEMBL_ACT_25218698
OPRM1	5.26	AC50	5497	nM	CHEMBL_ACT_25157995

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

2 indications (1 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
neoplasm	4	MONDO:0005070	EFO:0000616
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060

Clinical trials

Total trials: 6.

Phase distribution

Phase	Trials
PHASE2	3
PHASE1	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01588145	PHASE1/PHASE2	COMPLETED	Phase I/II Trial to Evaluate Safety, Tolerability and Pharmacokinetic Profile of HM61713 in NSCLC Patients
NCT02444819	PHASE2	COMPLETED	Phase II Trial to Evaluate the Efficacy and Safety of HM61713 as the 1st-line NSCLC Anticancer Therapy
NCT02485652	PHASE2	TERMINATED	Phase II Trial of HM61713 for the Treatment of ≥2nd Line T790M Mutation Positive Adenocarcinoma of the Lung
NCT03228277	PHASE2	COMPLETED	Olmutinib Trial in T790M (+) NSCLC Patients Detected by Liquid Biopsy Using BALF Extracellular Vesicular DNA
NCT01894399	PHASE1	COMPLETED	Study to Evaluate a Pharmacokinetic of HM61713 in Healthy Male Subjects
NCT04510415	PHASE1	TERMINATED	Olmutinib 600 mg QD in Patients With T790M-positive NSCLC After Treatment With an EGFR-TKI

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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
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
TUCATINIB	ChEMBL	Phase 4 (approved)	EGFR