Drug intelligence / Profile preview

TSN084

Development stage
Phase 1
Lead developer
Tyligand Bioscience
Modality
Small Molecules
Administration
Oral
01

Overview

TSN084 is a novel orally bioavailable type II small molecule protein kinase inhibitor that targets multiple tyrosine kinases implicated in cancer. Its primary targets include c-Met (hepatocyte growth factor receptor), FMS-like tyrosine kinase 3 (FLT3), tropomyosin-related kinases (TRK), and cyclin-dependent kinases CDK8 and CDK19. By inhibiting these kinases, TSN084 blocks oncogenic signaling pathways involved in tumor cell proliferation, survival, invasion, treatment resistance, and immune evasion. Preclinical studies have demonstrated anti-tumor effects both in vitro and in vivo. The drug is currently being evaluated for safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with advanced or metastatic malignancies[2][5][7].

Other names
3-pyridinecarboxamide, N-(3-fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-1,2-dihydro-6-(1-methylethoxy)-2-oxo-N-[3-fluoro–4–[[1-methyl–6–(1H-pyrazol–4–yl)–1H-indazol–5–yl]oxy]phenyl]-1-(4-fluorophenyl)-1,2-dihydro‑6‑(1‑methylethoxy)‑2‑oxo‑3-pyridinecarboxamide
02

Targets

AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)CDK8 (Cyclin-dependent kinase 8)Trk (Trk receptor family)DDR1 (Discoidin domain receptor 1)CDK19FLT3 (Fms related receptor tyrosine kinase 3)

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