Drug intelligence / Profile preview

CYT-0851 + capecitabine

Development stage
Phase 2
Lead developer
Cyteir Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

CYT-0851 + capecitabine is a combination therapy under clinical investigation for advanced solid tumors, including platinum-refractory or -resistant ovarian cancer. CYT-0851 is a first-in-class small molecule inhibitor of monocarboxylate transporters (MCTs), which blocks lactate transport in cancer cells, leading to glycolytic cell death. It also inhibits homologous recombination (HR), resulting in the accumulation of unrepaired double-strand DNA breaks and tumor cell death. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU) that interferes with DNA synthesis and repair by inhibiting thymidylate synthase, leading to cytotoxicity in rapidly dividing cells. The combination has shown promising early clinical activity and a generally well-tolerated safety profile in heavily pretreated patients with advanced cancers[2][3][5][6][8].

02

Targets

SLC16A1 (Mitochondrial Pyruvate Carrier)RAD51 (RAD51 Recombinase)TS (Thymidylate synthase)MCT4 (Monocarboxylate transporter 4)

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