Famitinib

Summary

Famitinib (CHEMBL1278146) is a phase-3 clinical-stage small molecule targeting PDGFRB, KIT, and KDR; indicated across 19 conditions including non-small cell lung carcinoma and colorectal adenocarcinoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 3 (PDGFRB, KIT, KDR)
• Indications: 19 conditions
• Clinical trials: 50
• Chemistry: 410.5 Da · C23H27FN4O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1278146
Name	Famitinib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	16662431
Molecular formula	C23H27FN4O2
Molecular weight	410.5
InChIKey	GKEYKDOLBLYGRB-LGMDPLHJSA-N

SMILES: CCN(CC)CCN1CCC2=C(C1=O)C(=C(N2)/C=C\3/C4=C(C=CC(=C4)F)NC3=O)C

IUPAC name: 5-[2-(diethylamino)ethyl]-2-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-3-methyl-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one

Also known as: Famitinib, Shr-1020, SHR1020, FAMITINIB

Patent coverage: 232 distinct patent families (618 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
PDGFRB	platelet derived growth factor receptor beta	Inhibition	8.4	2.3%	P09619
KIT	KIT proto-oncogene, receptor tyrosine kinase	Inhibition	8.7	0.5%	P10721
KDR	kinase insert domain receptor	Inhibition	8.3	1.1%	P35968

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Vascular endothelial growth factor receptor 2.

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
KIT	8.7	IC50	2	nM	CHEMBL_ACT_3561712
KDR	8.7	IC50	2	nM	CHEMBL_ACT_3561724
PDGFRB	8.4	IC50	4	nM	CHEMBL_ACT_3561700
KDR	8.3	IC50	5	nM	CHEMBL_ACT_3561688

Target pathways

Aggregated over 3 target gene(s): PDGFRB, KIT, KDR.

Top Reactome pathways

48 total, by targets touching each:

Pathway	Targets	Genes
PIP3 activates AKT signaling	2	KIT, PDGFRB
Constitutive Signaling by Aberrant PI3K in Cancer	2	KIT, PDGFRB
RAF/MAP kinase cascade	2	KIT, PDGFRB
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	2	KIT, PDGFRB
Developmental Biology	1	KIT
Signaling by SCF-KIT	1	KIT
Regulation of KIT signaling	1	KIT
Signal Transduction	1	KIT
Disease	1	KIT
Downstream signal transduction	1	PDGFRB
Signaling by PDGF	1	PDGFRB
Neuropilin interactions with VEGF and VEGFR	1	KDR
VEGF binds to VEGFR leading to receptor dimerization	1	KDR
Negative regulation of the PI3K/AKT network	1	KIT
Generic Transcription Pathway	1	KIT
Integrin cell surface interactions	1	KDR
PI3K/AKT Signaling in Cancer	1	KIT
VEGFA-VEGFR2 Pathway	1	KDR
VEGFR2 mediated cell proliferation	1	KDR
Diseases of signal transduction by growth factor receptors and second messengers	1	KIT
MAPK family signaling cascades	1	KIT
MAPK1/MAPK3 signaling	1	KIT
RNA Polymerase II Transcription	1	KIT
Gene expression (Transcription)	1	KIT
Transcriptional regulation by the AP-2 (TFAP2) family of transcription factors	1	KIT
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors	1	KIT
Intracellular signaling by second messengers	1	KIT
Signaling by Receptor Tyrosine Kinases	1	KIT
Dasatinib-resistant KIT mutants	1	KIT
Imatinib-resistant KIT mutants	1	KIT

Dominant GO biological processes

GO term	Targets
cell surface receptor protein tyrosine kinase signaling pathway	3
positive regulation of cell population proliferation	3
positive regulation of cell migration	3
protein autophosphorylation	3
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	3
protein phosphorylation	3
cell migration	3
angiogenesis	2
signal transduction	2
peptidyl-tyrosine phosphorylation	2
cell chemotaxis	2
positive regulation of ERK1 and ERK2 cascade	2
chemotaxis	2
ovarian follicle development	2
regulation of cell shape	2

Indications & clinical

Indications

19 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
colorectal adenocarcinoma	3	MONDO:0005008	EFO:0000365
triple-negative breast carcinoma	3	MONDO:0005494	EFO:0005537
gastrointestinal stromal tumor	3	MONDO:0011719	MONDO:0011719
nasopharyngeal neoplasm	2	MONDO:0005375	EFO:0004252
neoplasm	2	MONDO:0005070	EFO:0000616
renal cell carcinoma	2	MONDO:0005086	EFO:0000681
breast neoplasm	2	MONDO:0021100	EFO:0003869
carcinoid tumor	2	MONDO:0005369	MONDO:0024503
exocrine pancreatic carcinoma	2	MONDO:0005192	EFO:0002618
lung carcinoma	2	MONDO:0005138	EFO:0001071
esophageal squamous cell carcinoma	2	MONDO:0005580	EFO:0005922
intrahepatic cholangiocarcinoma	2	MONDO:0003210	EFO:1001961
melanoma	2	MONDO:0005105	EFO:0000756
small cell lung carcinoma	2	MONDO:0008433	EFO:0000702
nasopharyngeal carcinoma	1	MONDO:0015459	MONDO:0015459

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

Clinical trials

Total trials: 50.

Phase distribution

Phase	Trials
PHASE2	32
PHASE3	7
PHASE1/PHASE2	5
PHASE1	5
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05760378	PHASE3	RECRUITING	Famitinib in Combination With Camrelizumab and TPC in The First-line Treatment of Immunomodulatory Locally Advanced or Metastatic TNBC.
NCT05999149	PHASE3	RECRUITING	A Study of Camrelizumab Plus Chemotherapy in Combination With or Without Famitinib as Neoadjuvant Therapy in Participants With Triple Negative Breast Cancer (BCTOP-T-N01)
NCT07382687	PHASE3	NOT_YET_RECRUITING	Famitinib Combined With SHR-A1811, Versus SHR-A1811 for CDK4/6 Inhibitors-resistent Advanced HR+/HER2- Breast Cancer With SNF4 Subtype
NCT02390947	PHASE3	COMPLETED	Safety and Efficacy Study of Famitinib in Patients With Advanced Colorectal Adenocarcinoma（FACT）
NCT04409223	PHASE3	TERMINATED	Efficacy and Safety of Famitinib Versus Sunitinib in the Treatment of Advanced Gastrointestinal Stromal Tumour Patients After Failure of Imatinib
NCT05042375	PHASE3	UNKNOWN	A Trial of Camrelizumab Combined With Famitinib Malate in Treatment Naïve Subjects With PD-L1-Positive Recurrent or Metastatic Non-Small Cell Lung Cancer
NCT05106335	PHASE3	TERMINATED	A Study to Evaluate Camrelizumab Combined With Famitinib as Subsequent Therapy in Patients With Advanced NSCLC
NCT04888429	PHASE2	RECRUITING	Camrelizumab Plus Famitinib as Treatment in Patient With Advanced or Metastatic Pulmonary Sarcomatoid Carcinoma
NCT05582499	PHASE2	RECRUITING	Fudan University Shanghai Cancer Center Breast Cancer Precision Platform Series Study- Neoadjuvant Therapy
NCT05594095	PHASE2	RECRUITING	SNF Platform Study of HR+/ HER2-advanced Breast Cancer
NCT06306560	PHASE2	NOT_YET_RECRUITING	A Study of Adebrelimab Combined With Famitinib and Chemotherapy in the Treatment of ES-SCLC.
NCT06332950	PHASE1/PHASE2	NOT_YET_RECRUITING	Safety and Efficacy of Adebrelimab Plus Irinotecan Liposome (II) With or Without Famitinib in ES-SCLC Pre-treated With Immunotherapy
NCT06516289	PHASE2	RECRUITING	Neoadjuvant Treatment of gBRCA-Mutated HER2-Negative Breast Cancer With HRS-1167 and Famitinib ± Camrelizumab
NCT06649331	PHASE2	RECRUITING	Platform Study of ADC Rechallenge in ADC-treated Metastatic Breast Cancer
NCT07143292	PHASE2	NOT_YET_RECRUITING	A Prospective, Randomized, Parallel Trial of Famitinib Malate at Different Doses Combined With Camrelizumab for the Treatment of Recurrent and Metastatic Cervical Cancer
NCT07147088	PHASE2	NOT_YET_RECRUITING	Cryoablation Combined With SHR-1701 Plus Famitinib in Patients With Advanced Intrahepatic Cholangiocarcinoma.
NCT07355010	PHASE2	NOT_YET_RECRUITING	A Randomized, Open-label, Double-cohort Study of Fluzoparib Combined With Famitinib Malate or SHR-1701 for Neoadjuvant Therapy in Patients With Advanced Ovarian Cancer
NCT07517653	PHASE2	NOT_YET_RECRUITING	Neoadjuvant SHR-1701 Plus Famitinib With Response-guided Adjuvant Therapy in Resectable Mucosal Melanoma
NCT01392235	PHASE2	COMPLETED	Famitinib in Treating Patients With Recurrent and/or Metastatic Nasopharyngeal Carcinoma (NPC)
NCT01653574	PHASE2	COMPLETED	A Study of Famitinib Malate in HER2-negative Metastatic Breast Cancer
NCT01762293	PHASE2	COMPLETED	A Study of Famitinib in Patients With Advanced Colorectal Cancer
NCT01829841	PHASE2	COMPLETED	A Study of Famitinib in Patients With Advanced Metastatic Renal Cell Cancer
NCT01994213	PHASE2	TERMINATED	A Study of Famitinib in Patients With Advanced or Metastatic Gastroenteropancreatic Neuroendocrine Tumor
NCT02336724	PHASE2	UNKNOWN	A Study of Famitinib in Patients With Gastrointestinal Stromal Tumor
NCT02356991	PHASE2	SUSPENDED	A Study of Famitinib in Patients With Advanced Non-squamous and Non-Small Cell Lung Cancer (NSCLC)
NCT03827837	PHASE2	UNKNOWN	Famitinib Plus Anti-PD1 Therapy for Advanced Urinary System Tumor, Advanced Gynecological Tumors
NCT04044378	PHASE1/PHASE2	WITHDRAWN	Famitinib Plus Camrelizumab & Famitinib Alone & Famitinib Plus Ifosfamide in Advanced Osteosarcoma
NCT04129996	PHASE2	UNKNOWN	A Trial of Camrelizumab in Combination With Nab-paclitaxel and Famitinib as a First Line Treatment in Patients With Unresectable Locally Advanced or Metastatic Immunomodulatory Triple Negative Breast Cancer(FUTURE-C-PLUS)
NCT04346381	PHASE2	COMPLETED	Study to Evaluate the Efficacy and Safety of Camrelizumab and Famitinib in Patients With Advanced Solid Tumor
NCT04355858	PHASE2	UNKNOWN	Molecularly Targeted Umbrella Study in Luminal Advanced Breast Cancer
NCT04395989	PHASE2	UNKNOWN	An Umbrella Trial Based on Molecular Pathway for Patients With Metastatic TNBC.
NCT04479904	PHASE2	WITHDRAWN	A Trial of Famitinib in Patients With Failure of First-Line Treatment For Intrahepatic Cholangiocarcinoma
NCT04679038	PHASE1/PHASE2	UNKNOWN	A Trial of SHR-1701 in Combination With Famitinib in Patients With Advanced Solid Tumors
NCT04680988	PHASE2	COMPLETED	A Study of SHR-1210± SHR-1020 Versus Chemotherapy in Patients With Recurrent or Metastatic Cervical Cancer
NCT04733417	PHASE2	UNKNOWN	A Study of SHR6390 Combined With Famitinib in the Treatment of HR + / HER2- Advanced Breast Cancer.
NCT04814485	PHASE2	UNKNOWN	Efficacy and Safety of SHR-1020 Combined With Albumin-bound Paclitaxel in the Second-line Treatment of Pancreatic Cancer
NCT04884009	PHASE2	UNKNOWN	A Trial of SHR-1701 in Combination With and Without Famitinib Malate in Patients With Extensive Stage Small Cell Lung Cancer
NCT05005468	PHASE2	UNKNOWN	A Phase II Trial of Camrelizumab Combined With Famitinib for Adjuvant Treatment of Stage II-IIIA NSCLC.
NCT05020925	PHASE1/PHASE2	UNKNOWN	SHR-1701 in Combination With Famitinib in Patients With Recurrent/Metastatic Nasopharyngeal Carcinoma
NCT05051865	PHASE2	UNKNOWN	To Explore the Efficacy and Safety of Camrelizumab Combined With SHR1020 in the Treatment of Advanced Melanoma

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.

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

Molecule	Source	Status	Shared targets
Crizotinib	ChEMBL + PubChem	Phase 4 (approved)	KDR, KIT, PDGFRB
IMATINIB	ChEMBL + PubChem	Phase 4 (approved)	KDR, KIT, PDGFRB
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	KDR, KIT, PDGFRB
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	KDR, KIT, PDGFRB
AXITINIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
DASATINIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
ERLOTINIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
FEDRATINIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
LENVATINIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
NINTEDANIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
PEXIDARTINIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
PONATINIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
QUIZARTINIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
SORAFENIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
SUNITINIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
TIVOZANIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
VANDETANIB	ChEMBL	Phase 4 (approved)	KDR, KIT, PDGFRB
BARASERTIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
BRIVANIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
CANERTINIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
CEDIRANIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
DOVITINIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
LESTAURTINIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
LINIFANIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
MOTESANIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
SARACATINIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
SEMAXANIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
VATALANIB	ChEMBL	Phase 3	KDR, KIT, PDGFRB
BFH-772	ChEMBL	Phase 2	KDR, KIT, PDGFRB
CENISERTIB	ChEMBL	Phase 2	KDR, KIT, PDGFRB
CEP-32496	ChEMBL	Phase 2	KDR, KIT, PDGFRB
DEFOSBARASERTIB	ChEMBL	Phase 2	KDR, KIT, PDGFRB
DORAMAPIMOD	ChEMBL	Phase 2	KDR, KIT, PDGFRB
FORETINIB	ChEMBL	Phase 2	KDR, KIT, PDGFRB
ILORASERTIB	ChEMBL	Phase 2	KDR, KIT, PDGFRB
R-406	ChEMBL	Phase 2	KDR, KIT, PDGFRB
RAF-265	ChEMBL	Phase 2	KDR, KIT, PDGFRB
SU-014813	ChEMBL	Phase 2	KDR, KIT, PDGFRB
TANDUTINIB	ChEMBL	Phase 2	KDR, KIT, PDGFRB
TELATINIB	ChEMBL	Phase 2	KDR, KIT, PDGFRB
TOZASERTIB	ChEMBL	Phase 2	KDR, KIT, PDGFRB
Afatinib	PubChem	Approved	KDR, KIT, PDGFRB
Selumetinib	PubChem	Approved	KDR, KIT, PDGFRB
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	KDR, KIT
BOSUTINIB	ChEMBL	Phase 4 (approved)	KIT, PDGFRB
BRIGATINIB	ChEMBL	Phase 4 (approved)	KDR, KIT
CABOZANTINIB	ChEMBL	Phase 4 (approved)	KDR, KIT
CERITINIB	ChEMBL	Phase 4 (approved)	KDR, KIT
ENTRECTINIB	ChEMBL	Phase 4 (approved)	KDR, KIT
INFIGRATINIB	ChEMBL	Phase 4 (approved)	KDR, KIT
NICLOSAMIDE	ChEMBL	Phase 4 (approved)	KDR, KIT
NILOTINIB	ChEMBL	Phase 4 (approved)	KIT, PDGFRB
NINTEDANIB ESYLATE	ChEMBL	Phase 4 (approved)	KDR, PDGFRB
SUNITINIB MALATE	ChEMBL	Phase 4 (approved)	KDR, PDGFRB
CATEQUENTINIB	ChEMBL	Phase 3	KDR, PDGFRB
ENZASTAURIN	ChEMBL	Phase 3	KIT, PDGFRB
FLUMATINIB	ChEMBL	Phase 3	KIT, PDGFRB
MASITINIB	ChEMBL	Phase 3	KIT, PDGFRB
ORANTINIB	ChEMBL	Phase 3	KDR, PDGFRB