Drug intelligence / Profile preview

CPL304110

Development stage
Phase 1
Lead developer
Celon Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

CPL304110 is a potent, orally active, and selective small molecule inhibitor of fibroblast growth factor receptors FGFR1, FGFR2, and FGFR3. It exhibits nanomolar inhibitory activity against these receptor tyrosine kinases (IC50 values of 0.75 nM for FGFR1, 0.5 nM for FGFR2, and 3.05 nM for FGFR3), leading to the inhibition of downstream signal transduction pathways involved in tumor cell proliferation and survival. Preclinical studies have demonstrated its efficacy in both cell lines and patient-derived xenograft models with active FGFR signaling. CPL304110 is being developed primarily as a targeted therapy for advanced solid malignancies characterized by aberrant activation or mutation of the FGFR pathway—including bladder cancer, gastric (stomach) cancer, squamous non-small cell lung cancer (NSCLC), endometrial carcinoma, sarcoma, bile duct neoplasms (cholangiocarcinoma), and other gastrointestinal cancers. The drug is currently undergoing Phase I clinical trials to assess its safety and efficacy in these indications. Developed and manufactured by Celon Pharma.

02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)CSF1R (Macrophage colony-stimulating factor receptor)FLT3 (Fms related receptor tyrosine kinase 3)RET (Rearranged during transfection receptor tyrosine kinase)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)VEGFR2 (Vascular endothelial growth factor receptor 2)CB (Cannabinoid receptors)LCK (Proto-oncogene tyrosine-protein kinase Lck)FGFR3 (Fibroblast growth factor receptor 3)NTRK1 (Tropomyosin-related receptor kinase A)FGFR1 (Fibroblast growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)HTR3A (5-hydroxytryptamine receptor 3A)FGFR2 (Keratinocyte growth factor receptor)TYK2 (Tyrosine kinase 2)RIPK1 (Receptor-interacting serine/threonine-protein kinase 1)

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