Description: Trilaciclib is an intravenously administered, small molecule inhibitor of cyclin-dependent kinases 4 and 6, that is used to decrease chemotherapy-induced myelosuppression. Serum aminotransferase elevations arise in a small proportion of patients treated with the highest doses of trilaciclib, but episodes of clinically apparent liver injury have not been reported with its use. (Source: PubChem)
Description: Trilaciclib (G1T28) is selective for CDK4/6 over other CDKs. Inhibition of off-target kinases with high affinity binding is reported- e.g. of the enzymes inhibited by >90% at 100nM G1T28, FLT3(D835V), GAK, NEK10, PRKD1, PRKD3, SNARK and ULK2 all have an affinity constant (Kd) <10nM [1]. In the tumour microenvironment trilaciclib promotes a neutrophil and CD8+ effector T cell-driven antitumour immune response (Source: IUPHAR/BPS Guide to Pharmacology)
Description: Trilaciclib (G1T28) is selective for CDK4/6 over other CDKs. Inhibition of off-target kinases with high affinity binding is reported- e.g. of the enzymes inhibited by >90% at 100nM G1T28, FLT3(D835V), GAK, NEK10, PRKD1, PRKD3, SNARK and ULK2 all have an affinity constant (Kd) <10nM [1]. In the tumour microenvironment trilaciclib promotes a neutrophil and CD8+ effector T cell-driven antitumour immune response (Source: PubChem)
Description: A medication to lower the risk of some chemotherapies weakening the immune system (Source: DrugBank)
Clinical Indication: In the prelicensure clinical trials of trilaciclib in patients with advanced cancer receiving cytotoxic chemotherapy, serum AST elevations arose in 17% of trilaciclib vs 14% of placebo recipients. The AST elevations were usually self-limited and mild and elevations above 5 times the upper limit of normal (ULN) were uncommon, being found in (Source: PubChem)
Clinical Indication: Pre-chemotherapy intravenous administration of trilaciclib (G1T28) was evaluated in a number of clinical trials (Source: IUPHAR/BPS Guide to Pharmacology)
Drug Label Annotation: The concentration or amount of drug in body reduced by one-half in 14 hours (Source: Drug Map)