Pyrazoles are organic compounds of the general formula C3H3N2H. It is a five-membered heterocycle consisting of three carbon atoms and two adjacent nitrogen atoms. As an H-bond-donating heterocycle, pyrazole has been used as a more lipophilic and metabolically more stable bioisomer of phenol. Pyrazoles have attracted more and more attention due to their broad spectrum of action and strong efficacy.
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Repare Therapeutics announces Fast Track Designation granted by the FDA for Lunresertib in combination with Camonsertib for the treatment of platinum-resistant ovarian cancer. Membrane-associated Tyrosine- and Threonine-specific cdc2-inhibitory kinase MYT1 (PKMYT1) is a regulator of CDK1 phosphorylation, and PKMYT1 is identified as synthetic lethal with cyclin E1 (CCNE1) amplification.
Lunresertib (RP-6306) is a first-in-class PKMYT1 inhibitor to enter clinical trial. Lunresertib is studied alone and in combination with Camonsertib in patients with advanced solid tumors. Camonsertib (RP-3500) is a potent and selective ATR inhibitor, that helps Lunresertib activate CDK1 and promotes premature mitosis. The combination is previously granted Fast Track Designation for the treatment of adult patients with CCNE1 amplified, or FBXW7 or PPP2R1A mutated endometrial cancer.
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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