Drug intelligence / Profile preview

telaglenastat + dexamethasone

Development stage
Unknown
Lead developer
Calithera Biosciences, Inc
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Telaglenastat + dexamethasone is an investigational combination therapy consisting of **telaglenastat**, a selective, noncompetitive glutaminase 1 (GLS1) inhibitor, and **dexamethasone**, a synthetic glucocorticoid corticosteroid. Telaglenastat inhibits GLS1, the enzyme that converts glutamine to glutamate in the tricarboxylic acid cycle, thereby disrupting mitochondrial respiration and metabolic processes critical for cancer cell survival and proliferation[1][3]. Dexamethasone acts via the glucocorticoid receptor to induce immunosuppressive and anti-inflammatory effects and promotes apoptosis in cancer cells. This combination is being explored primarily in hematologic malignancies, especially relapsed/refractory multiple myeloma[1][3][4].

Other names
telaglenastat + dexamethasone
02

Targets

GR (Glucocorticoid receptor)GLS1 (Glutaminase 1)

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