Drug intelligence / Profile preview

trilaciclib

Development stage
Approved
Lead developer
G1 Therapeutics
Modality
Small Molecules
Administration
Intravenous
01

Overview

Trilaciclib is a first-in-class, intravenous small molecule inhibitor of cyclin-dependent kinase 4 and 6 (CDK4/6). It is used to decrease the incidence of chemotherapy-induced myelosuppression in adults with extensive-stage small cell lung cancer (ES-SCLC) when administered prior to certain chemotherapy regimens. Trilaciclib works by transiently inhibiting CDK4/6, causing a reversible G1 phase cell cycle arrest in hematopoietic stem and progenitor cells. This protects these cells from the cytotoxic effects of chemotherapy without interfering with the anti-tumor efficacy against retinoblastoma protein-null cancer cells. The drug was developed by G1 Therapeutics and was approved by the FDA in February 2021 as the first therapy specifically designed for multilineage myeloprotection during chemotherapy.

Brand names
Cosela
Other names
1374743-00-62'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one
02

Targets

CDK6 (Cyclin-dependent kinase 6)CDK7CDK4 (Cyclin-dependent kinase 4)CDK2 (Cyclin-dependent kinase 2)CDK9 (Cyclin-dependent kinase 9)CDK5 (Cyclin-dependent kinase 5)

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