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telaglenastat + dexamethasone
- Development stage
- Phase 1
- 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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