Incb001158 (Not yet branded)

Other Medications

US Experimental EU Experimental ES Not available IV 3 Clinical Trials
Arginase 1 Arginase 2

Description

INCB001158 is an arginase inhibitor that blocks the enzyme arginase, which depletes arginine in the tumor microenvironment. This compound is designed to restore arginine availability to immune cells, particularly T cells, which require arginine for optimal function and proliferation. In colorectal cancer, it is evaluated primarily in combination with immunotherapy agents and chemotherapy regimens to enhance anti-tumor immune responses.

Mechanism of Action

INCB001158 selectively inhibits arginase enzymes (arginase 1 and arginase 2) that convert arginine to ornithine and urea. By preventing arginine depletion in the tumor microenvironment, this inhibition helps restore T cell function and proliferation, as these immune cells are highly dependent on arginine availability for their metabolic processes and cytotoxic activity.

Molecular Targets

Side Effects

Fatigue Nausea Diarrhea Decreased appetite Skin rash Elevated liver enzymes Headache Vomiting

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT03361228 Phase 1
Archived
A Study to Evaluate the Safety, Tolerability, and Antitumor Activity of INCB001158 Plus Epacadostat, With or Without Pembrolizumab, in Advanced Solid Tumors
United States
NCT03314935 Phase 1
Archived
A Phase 1/2 Study of INCB001158 in Combination With Chemotherapy in Subjects With Solid Tumors
United States, Belgium, United Kingdom
NCT02903914 Phase 1
Archived
Arginase Inhibitor INCB001158 as a Single Agent and in Combination With Immune Checkpoint Therapy in Patients With Advanced/Metastatic Solid Tumors
United States, Italy, Netherlands, Spain