Pyrazolopyrimidine scaffolds are one of the most important heterocyclic compounds in drug discovery. This scaffold has various biological activities, among which anticancer is an important one.
Kronos Bio announces the first patient dosed in an expansion cohort with KB-0742 at a dose of 80mg given on a four-days-on, three-days-off schedule. This expansion cohort is enrolling platinum-resistant patients with high-grade serous ovarian cancer (HGSOC). Many cancers exhibit transcriptional deregulation, often characterized by gene amplifications of MYC family oncogene. Targeting the transcription elongation cofactor, cyclin-dependent kinase 9 (CDK9) has emerged as a therapeutic strategy to disrupt MYC oncogenic activity.
KB-0742 is an oral highly selective CDK9 inhibitor designed for the treatment of patients with MYC-amplified and other transcriptionally addicted relapsed or refractory solid tumors, including ovarian, lung, and triple-negative breast cancers.
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