fadraciclib

Fadraciclib is a highly selective, potent, orally and intravenously available small molecule inhibitor of cyclin-dependent kinases 2 and 9 (CDK2 and CDK9). It was developed to improve upon earlier CDK inhibitors by increasing potency and selectivity for these targets. Fadraciclib works by binding to and inhibiting the activity of CDK2 and CDK9, leading to disruption of cell cycle progression, inhibition of transcriptional regulation pathways critical for cancer cell survival, downregulation of anti-apoptotic proteins such as MCL1, induction of apoptosis (including through anaphase catastrophe), and suppression of MYC oncoprotein levels. The drug has demonstrated preclinical efficacy in models of leukemia, colorectal cancer, chronic lymphocytic leukemia (CLL), acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), lymphoma, as well as solid tumors with alterations in the CDKN2A/B genes. Fadraciclib is being evaluated in mid-stage clinical trials both as monotherapy and in combination with other agents such as venetoclax. It was discovered through a collaboration between Cyclacel Pharmaceuticals and The Institute of Cancer Research[1][2][5][6][7][8].

Other names

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