voruciclib

Voruciclib is a selective, orally administered small molecule inhibitor of cyclin-dependent kinase 9 (CDK9), with additional activity against CDK4 and CDK6. It is being developed primarily for the treatment of hematological malignancies, especially acute myeloid leukemia (AML), and is also under investigation for solid tumors where MYC dysregulation plays a role. By inhibiting CDK9, voruciclib disrupts transcriptional regulation of key oncogenic proteins such as MCL1 and MYC, leading to cell cycle arrest and apoptosis in cancer cells. Preclinical studies have shown that it can decrease phosphorylation events critical for MYC stability and function, particularly in KRAS mutant cancers. Voruciclib has demonstrated anti-leukemic activity both as monotherapy and in combination with venetoclax (a BCL2 inhibitor), showing synergistic effects by overcoming resistance mechanisms related to MCL1 expression. The drug is currently being evaluated in Phase 1 clinical trials for relapsed or refractory AML[1][3][5][6].

Other names

voruciclib [INN]