Roniciclib (BAY1000394) is a pan-cyclin-dependent kinase inhibitor that has been developed for treatment in small cell lung carcinoma and solid tumors. Roniciclib targets certain key proteins that are essential for the survival of cancer cells, resulting in decreased tumor growth. Phase I studies to evaluate the safety, tolerability and pharmacokinetics of roniciclib have been completed successfully. In phase II studies, roniciclib was found to be well tolerated and showed promising efficacy when combined with chemotherapy in small cell lung carcinoma patients. However, due to an observed safety signal (treatment-emergent adverse events) in one phase II study, other clinical trials have been discontinued and further development of roniciclib was terminated.

An orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. CDK2/TRKA inhibitor PHA-848125 AC potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. Inhibition of these kinases may result in cell cycle arrest and apoptosis of tumor cells that express these kinases. Milciclib is currently in phase II clinical trials for thymic carcinoma, glioma and liver cancer. The most common adverse events are nausea and asthenia, vomiting, myasthenic syndrome, dehydration, hypophosphatemia, cytolytic hepatitis and plantar fasciitis.

3-Amino-N-(2,6-difluorophenyl)-5-(4-sulfamoylanilino)-1,2,4-triazole-1-carbothioamide (CDK1/2 INHIBITOR III) is potent inhibitor of Cyclin-dependent kinase 1/2 (IC50=0.6nM and 0,5nM) with marked antiproliferative activity.

An orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. CDK2/TRKA inhibitor PHA-848125 AC potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. Inhibition of these kinases may result in cell cycle arrest and apoptosis of tumor cells that express these kinases. Milciclib is currently in phase II clinical trials for thymic carcinoma, glioma and liver cancer. The most common adverse events are nausea and asthenia, vomiting, myasthenic syndrome, dehydration, hypophosphatemia, cytolytic hepatitis and plantar fasciitis.