Lerociclib

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable inhibitor of cyclin-dependent kinase (CDK) types 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon administration, lerociclib selectively inhibits CDK4 and CDK6, which inhibits the phosphorylation of retinoblastoma protein (Rb) early in the G1 phase, prevents CDK-mediated G1-S phase transition and leads to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of both cell cycle progression from the G1-phase into the S-phase and tumor cell proliferation.

**Synonyms:** - 7',8'-Dihydro-2'-((5-(4-(1-methylethyl)-1-piperazinyl)-2-pyridinyl)amino)spiro(cyclohexane-1,9'(6'H)-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one - CDK4/6 Inhibitor G1T38 - G1T38 - G1T38 Free Base - GB 491 - GB-491 - GB491 - LEROCICLIB