Drug intelligence / Profile preview

INCB001158 + oxaliplatin + leucovorin + 5-fluorouracil

Development stage
Unknown
Lead developer
Incyte
Modality
Small Molecules
Administration
Oral (INCB001158), Intravenous (oxaliplatin), Intravenous (leucovorin), Intravenous (5-fluorouracil)
01

Overview

INCB001158 + oxaliplatin + leucovorin + 5-fluorouracil is a combination therapy composed of the experimental small molecule arginase inhibitor INCB001158 with standard anticancer cytotoxic agents oxaliplatin, leucovorin, and 5-fluorouracil. INCB001158 inhibits arginase-1, an immunosuppressive enzyme produced by myeloid-derived suppressor cells in the tumor microenvironment, leading to increased arginine levels, reversal of local T cell suppression, and enhanced anti-tumor immune response. Oxaliplatin is a platinum-based DNA crosslinking agent, 5-fluorouracil is a pyrimidine antagonist that inhibits thymidylate synthase disrupting DNA replication, and leucovorin enhances the effect of 5-fluorouracil. The combination is under clinical investigation in advanced/metastatic solid tumors, particularly gastrointestinal/colorectal malignancies, aiming to improve anti-tumor immune activity and cytotoxicity[1][5][6][8].

Brand names
None known for the combination
Other names
None known for the combination
02

Targets

DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)DNAARG1 (Arginase 1)

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