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Monzosertib (AS-0141) is a potent, selective, and orally bioavailable small molecule inhibitor of Cell Division Cycle 7 (CDC7) kinase, currently under development by Carna Biosciences for the treatment of various cancers. CDC7 is a serine-threonine kinase that plays a pivotal role in the initiation of DNA replication; its inhibition leads to DNA replication stress and subsequent cell death in cancer cells through lethal S phase or M phase progression. Monzosertib has demonstrated significant anti-proliferative activity across a range of solid tumors and hematological malignancies in preclinical models and is currently being evaluated in Phase 1 clinical trials to determine its safety, tolerability, and preliminary efficacy in patients with advanced, metastatic, relapsed, or refractory malignancies.
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