Drug intelligence / Profile preview

NRC-AN-019

Development stage
Phase 2
Lead developer
NATCO Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

NRC‑AN‑019 is an orally administered small molecule tyrosine kinase inhibitor developed as a potential treatment for cancers resistant to first-generation therapies. It specifically inhibits the Bcr-Abl protein tyrosine kinase by binding to its inactive conformation and disrupting ATP binding, thereby blocking catalytic activity. NRC‑AN‑019 also acts as an antagonist of the ERBB 2 (HER2/neu) receptor and has demonstrated inhibitory activity against Kit and PDGFR kinases. Preclinical studies showed that it is more effective than imatinib in certain models of chronic myeloid leukemia (CML), particularly in imatinib-resistant cases. The drug was developed by Natco Pharma and reached phase I clinical trials for CML but development appears to have been discontinued before approval[6][5][1][7]. Orphan drug status was granted for pancreatic cancer, glioma, and CML[3].

Other names
3,5-Bis(trifluoromethyl)-n-(4-methyl-3-(4-pyridin-3yl-pyrimidin2yl amino)phenyl)benzamideN-[4-methyl–3–(4-pyridin–3–ylpyrimidin–2–yl)amino]phenyl]-3,5-bis(trifluoromethyl)benzamideN-(4-methyl–3-(4-(pyridin–3-y)pyrimidin2-y)amino)phenyl)-3,5-bis(trifluoromethyl)benzamide
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFR (PDGFR family)

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