Ibcasertib

Summary

Ibcasertib (CHEMBL5095033) is a phase-3 clinical-stage small molecule targeting PDGFRA, PDGFRB, and KIT; indicated across 7 conditions including small cell lung carcinoma and neoplasm.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 8 (PDGFRA, PDGFRB, KIT…)
• Indications: 7 conditions
• Clinical trials: 16
• Chemistry: 435.5 Da · C27H21N3O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5095033
Name	Ibcasertib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	49779393
Molecular formula	C27H21N3O3
Molecular weight	435.5
InChIKey	BRKWREZNORONDU-UHFFFAOYSA-N

SMILES: COC1=CC2=NC=CC(=C2C=C1)OC3=CC4=C(C=C3)C(=CC=C4)C(=O)NC5=CC=CC=C5N

IUPAC name: N-(2-aminophenyl)-6-(7-methoxyquinolin-4-yl)oxynaphthalene-1-carboxamide

Also known as: Chiauranib, Cs-2164, CS-2164, CS2164, Ibcasertib, IBCASERTIB

Patent coverage: 203 distinct patent families (517 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 494 (96%) 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
PDGFRA	platelet derived growth factor receptor alpha	Inhibition	9	6.2%	P16234
PDGFRB	platelet derived growth factor receptor beta	Inhibition	7.03	2.3%	P09619
KIT	KIT proto-oncogene, receptor tyrosine kinase	Inhibition	8.4	0.5%	P10721
CSF1R	colony stimulating factor 1 receptor	Inhibition	8.15	0%	P07333
FLT1	fms related receptor tyrosine kinase 1	Inhibition	8.1	0.1%	P17948
KDR	kinase insert domain receptor	Inhibition	8.15	1.1%	P35968
FLT4	fms related receptor tyrosine kinase 4	Inhibition	8.05	0.2%	P35916
AURKB	aurora kinase B	Inhibition	8.05	99.7% (common-essential)	Q96GD4

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

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
PDGFRA	8.15	IC50	7	nM	CHEMBL_ACT_26132438

Target pathways

Aggregated over 8 target gene(s): PDGFRA, PDGFRB, KIT, CSF1R, FLT1, KDR, FLT4, AURKB.

Top Reactome pathways

89 total, by targets touching each:

Pathway	Targets	Genes
PIP3 activates AKT signaling	3	KIT, PDGFRA, PDGFRB
VEGF binds to VEGFR leading to receptor dimerization	3	FLT1, FLT4, KDR
Constitutive Signaling by Aberrant PI3K in Cancer	3	KIT, PDGFRA, PDGFRB
RAF/MAP kinase cascade	3	KIT, PDGFRA, PDGFRB
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	3	KIT, PDGFRA, PDGFRB
Signal Transduction	2	AURKB, KIT
Downstream signal transduction	2	PDGFRA, PDGFRB
Signaling by PDGF	2	PDGFRA, PDGFRB
Neuropilin interactions with VEGF and VEGFR	2	FLT1, KDR
Generic Transcription Pathway	2	AURKB, KIT
RNA Polymerase II Transcription	2	AURKB, KIT
Gene expression (Transcription)	2	AURKB, KIT
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells	2	FLT4, KDR
Developmental Biology	1	KIT
Amplification of signal from the kinetochores	1	AURKB
Amplification of signal from unattached kinetochores via a MAD2 inhibitory signal	1	AURKB
Signaling by SCF-KIT	1	KIT
Regulation of KIT signaling	1	KIT
Cell Cycle	1	AURKB
Disease	1	KIT
APC/C-mediated degradation of cell cycle proteins	1	AURKB
APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G1	1	AURKB
Signaling by Rho GTPases	1	AURKB
RHO GTPase Effectors	1	AURKB
Negative regulation of the PI3K/AKT network	1	KIT
Integrin cell surface interactions	1	KDR
PI3K/AKT Signaling in Cancer	1	KIT
Separation of Sister Chromatids	1	AURKB
Resolution of Sister Chromatid Cohesion	1	AURKB
Mitotic Metaphase and Anaphase	1	AURKB

Dominant GO biological processes

GO term	Targets
protein phosphorylation	8
cell surface receptor protein tyrosine kinase signaling pathway	7
positive regulation of cell population proliferation	7
cell migration	7
positive regulation of cell migration	7
protein autophosphorylation	7
peptidyl-tyrosine phosphorylation	6
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	6
positive regulation of ERK1 and ERK2 cascade	5
chemotaxis	4
angiogenesis	4
positive regulation of MAPK cascade	4
regulation of actin cytoskeleton organization	3
cell chemotaxis	3
signal transduction	3

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
small cell lung carcinoma	3	MONDO:0008433	EFO:0000702
neoplasm	2	MONDO:0005070	EFO:0000616
ovarian cancer	2	MONDO:0008170	MONDO:0008170
triple-negative breast carcinoma	2	MONDO:0005494	EFO:0005537
soft tissue sarcoma	2	MONDO:0018078	EFO:1001968
hepatocellular carcinoma	1	MONDO:0007256	EFO:0000182
non-Hodgkin lymphoma	1	MONDO:0018908	EFO:0005952

Clinical trials

Total trials: 16.

Phase distribution

Phase	Trials
PHASE1/PHASE2	4
PHASE2	4
PHASE1	4
PHASE3	3
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04921527	PHASE3	RECRUITING	Chiauranib Plus Weekly Paclitaxel in Patients with Platinum-refractory or Platinum-resistant Recurrent Ovarian Cancer
NCT07445295	PHASE3	NOT_YET_RECRUITING	Chiauranib Plus PD-1 Inhibitor, Albumin-paclitaxel and Gemcitabine in Patients With Metastatic Pancreatic Ductal Adenocarcinoma
NCT04830813	PHASE3	COMPLETED	Phase 3 Clinical Study of Chiauranib Capsule in Patients With Small-cell Lung Cancer
NCT05271292	PHASE1/PHASE2	RECRUITING	Chiauranib for Advanced Solid Malignant Tumors and Relapsed/Refractory SCLC.
NCT06492915	PHASE2	ACTIVE_NOT_RECRUITING	Chiauranib in Patients With Locally Advanced or Metastatic Pancreatic Ductal Adenocarcinoma
NCT03166891	PHASE1/PHASE2	COMPLETED	Phase Ib Study of Chiauranib in Patients With Ovarian Cancer
NCT03245190	PHASE1/PHASE2	COMPLETED	Study of Chiauranib in Patients With Advanced Hepatocellular Carcinoma
NCT03901118	PHASE2	COMPLETED	Chiauranib in Combination With Chemotherapy in Patients With Ovarian Cancer
NCT03974243	PHASE1/PHASE2	COMPLETED	Chiauranib in Combination With Chidamide in Patients With Relapsed/Refractory Non-Hodgkin’s Lymphoma
NCT05336721	PHASE2	TERMINATED	A Phase II Study of Chiauranib in Combine With Capecitabine in TNBC
NCT05497843	PHASE2	COMPLETED	Chiauranib for Advanced or Unresectable Soft Tissue Sarcoma(STS)
NCT02122809	PHASE1	COMPLETED	Phase I Study of Chiauranib in Patients With Advanced Solid Tumors
NCT03074825	PHASE1	TERMINATED	Study of Chiauranib in Relapsed/Refractory Non-Hodgkin’s Lymphoma
NCT03216343	PHASE1	COMPLETED	Phase Ib/II Study of Chiauranib in Patients With Small Cell Lung Cancer
NCT05346601	PHASE1	COMPLETED	Trial of Chiauranib Capsule on Pharmacokinetics to Assess the Effect of High Fat Diet in Healthy Volunteers
NCT05371899	Not specified	COMPLETED	Mass Balance Study of [14C]Chiauranib

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.

237 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Crizotinib	ChEMBL + PubChem	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
AXITINIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
FEDRATINIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
NINTEDANIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
QUIZARTINIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
SORAFENIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
SUNITINIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
VANDETANIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
CEDIRANIB	ChEMBL	Phase 3	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
DOVITINIB	ChEMBL	Phase 3	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
LESTAURTINIB	ChEMBL	Phase 3	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
LINIFANIB	ChEMBL	Phase 3	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
DEFOSBARASERTIB	ChEMBL	Phase 2	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
FORETINIB	ChEMBL	Phase 2	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
ILORASERTIB	ChEMBL	Phase 2	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
R-406	ChEMBL	Phase 2	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
SU-014813	ChEMBL	Phase 2	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
TANDUTINIB	ChEMBL	Phase 2	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
TOZASERTIB	ChEMBL	Phase 2	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
Afatinib	PubChem	Approved	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
Selumetinib	PubChem	Approved	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
Gefitinib	ChEMBL + PubChem	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA
DASATINIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, KDR, KIT, PDGFRA, PDGFRB
ERLOTINIB	ChEMBL	Phase 4 (approved)	AURKB, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
LENVATINIB	ChEMBL	Phase 4 (approved)	AURKB, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
PEXIDARTINIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, KDR, KIT, PDGFRA, PDGFRB
TIVOZANIB	ChEMBL	Phase 4 (approved)	AURKB, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
BRIVANIB	ChEMBL	Phase 3	CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
MOTESANIB	ChEMBL	Phase 3	CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
SEMAXANIB	ChEMBL	Phase 3	CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
VATALANIB	ChEMBL	Phase 3	CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
CENISERTIB	ChEMBL	Phase 2	CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
DORAMAPIMOD	ChEMBL	Phase 2	CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
RAF-265	ChEMBL	Phase 2	CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
Idelalisib	PubChem	Approved	AURKB, CSF1R, FLT1, FLT4, KIT, PDGFRA, PDGFRB
ENTRECTINIB	ChEMBL	Phase 4 (approved)	AURKB, CSF1R, FLT1, FLT4, KDR, KIT
PONATINIB	ChEMBL	Phase 4 (approved)	CSF1R, FLT1, KDR, KIT, PDGFRA, PDGFRB
CANERTINIB	ChEMBL	Phase 3	AURKB, FLT1, KDR, KIT, PDGFRA, PDGFRB
OSI-632	ChEMBL	Phase 2	AURKB, FLT1, FLT4, KDR, PDGFRA, PDGFRB
REBASTINIB	ChEMBL	Phase 2	CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA
IMATINIB	ChEMBL + PubChem	Phase 4 (approved)	CSF1R, KDR, KIT, PDGFRA, PDGFRB
CABOZANTINIB	ChEMBL	Phase 4 (approved)	AURKB, FLT1, FLT4, KDR, KIT
INFIGRATINIB	ChEMBL	Phase 4 (approved)	FLT1, FLT4, KDR, KIT, PDGFRA
NINTEDANIB ESYLATE	ChEMBL	Phase 4 (approved)	FLT1, FLT4, KDR, PDGFRA, PDGFRB
BARASERTIB	ChEMBL	Phase 3	AURKB, KDR, KIT, PDGFRA, PDGFRB
AT-9283	ChEMBL	Phase 2	AURKB, FLT1, FLT4, KDR, PDGFRA
BFH-772	ChEMBL	Phase 2	FLT1, FLT4, KDR, KIT, PDGFRB
CEP-32496	ChEMBL	Phase 2	CSF1R, FLT1, KDR, KIT, PDGFRB
ENMD-2076	ChEMBL	Phase 2	AURKB, CSF1R, KDR, KIT, PDGFRA
LUCITANIB	ChEMBL	Phase 2	AURKB, FLT1, FLT4, KDR, PDGFRB
BOSUTINIB	ChEMBL	Phase 4 (approved)	CSF1R, KIT, PDGFRA, PDGFRB
BRIGATINIB	ChEMBL	Phase 4 (approved)	CSF1R, FLT4, KDR, KIT
NILOTINIB	ChEMBL	Phase 4 (approved)	CSF1R, KIT, PDGFRA, PDGFRB
MASITINIB	ChEMBL	Phase 3	CSF1R, KIT, PDGFRA, PDGFRB
ORANTINIB	ChEMBL	Phase 3	AURKB, FLT1, KDR, PDGFRB
SARACATINIB	ChEMBL	Phase 3	KDR, KIT, PDGFRA, PDGFRB
VIMSELTINIB	ChEMBL	Phase 3	CSF1R, KIT, PDGFRA, PDGFRB