Drug intelligence / Profile preview

telaglenastat + palbociclib

Development stage
Unknown
Lead developer
Calithera Biosciences, Inc
Modality
Small Molecules
Administration
Oral
01

Overview

**Telaglenastat + palbociclib** is a combination therapy composed of *telaglenastat*, a selective, oral inhibitor of human glutaminase (CB-839), and *palbociclib*, an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). Telaglenastat blocks glutamine consumption by tumor cells, targeting a critical metabolic dependence often caused by genetic alterations, such as KRAS mutations, while palbociclib inhibits CDK4/6-driven cell cycle progression. The rationale for combination treatment is preclinical evidence for synergistic anti-tumor activity, notably in cancers with KRAS and/or CDKN2A mutations, enhancing cell cycle arrest and blocking proliferation. This combination is being investigated in phase 1/2 trials for advanced/metastatic KRAS-mutated colorectal cancer, KRAS-mutated non-small cell lung cancer, and pancreatic ductal adenocarcinoma with KRAS and CDKN2A mutations[1][3][5][7]. Telaglenastat was developed by Calithera Biosciences; palbociclib was developed and is manufactured by Pfizer.

Brand names
Ibrance + telaglenastat
Other names
telaglenastatpalbociclib
02

Targets

CDK6 (Cyclin-dependent kinase 6)GLS1 (Glutaminase 1)CDK4 (Cyclin-dependent kinase 4)

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