molecules of the month


oral pan-TRK inhibitor

tumor regression NIH3T3/NTRK1 mice models

from in-house library screening and SBDD

J. Med. Chem.

Chugai Pharmaceutical, Shizuoka, JP

CH7057288 chemical structure oral pan-TRK inhibitor - Chugai Pharmaceutical, Shizuoka, JP
4 mins read

Context. CH7057288 (Chugai Pharmaceutical Co) is an oral pan-tropomyosin receptor kinase (TRK) inhibitor. Chromosomal rearrangements in the NTRK1–3 genes that encode gene fusions leading to TRK fusion proteins have been shown to drive oncogenesis in many human tumors. Several inhibitors targeting kinase fusions have been developed and are effective for cancers harboring specific fusion oncogenes. Seven of the currently approved kinase fusion inhibitors are tumor-agnostic treatments, two of which target NTRK gene fusion, the pan-TRK inhibitors larotrectinib and entrectinib. In developing CH7057288, Chugai scientists speculated that the strong selectivity for ALK and unique scaffold of the highly effective ALK inhibitor alectinib could be incorporated to yield a similarly effective pan-TRK inhibitor as a new treatment option for solid tumors with…

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