Epacadostat (Not yet branded)

Other Medications

US Experimental EU Experimental ES Not available Oral 4 Clinical Trials
IDO1

Description

Epacadostat (INCB024360) is an oral small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) that has been evaluated in combination regimens for colorectal cancer. This compound belongs to the class of immunomodulatory agents designed to enhance anti-tumor immune responses by blocking immune suppression pathways. In colorectal cancer, epacadostat has been tested alongside immune checkpoint inhibitors like pembrolizumab and in combination with preoperative chemoradiation for locally advanced rectal cancer.

Mechanism of Action

Epacadostat selectively inhibits IDO1, an enzyme that catalyzes the degradation of tryptophan to kynurenine in the tumor microenvironment. By blocking IDO1 activity, the drug aims to reduce immunosuppressive kynurenine metabolites and restore T-cell proliferation and function. This mechanism is intended to enhance the body's immune response against cancer cells and potentially improve the efficacy of concurrent immunotherapies.

Molecular Targets

Side Effects

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

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

Clinical Trials

NCT03516708 Phase 1
Recruiting
Epacadostat (INCB024360) Added to Preoperative Chemoradiation in Patients With Locally Advanced Rectal Cancer
United States
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
NCT02959437 Phase 1
Archived
Azacitidine Combined With Pembrolizumab and Epacadostat in Subjects With Advanced Solid Tumors (ECHO-206)
United States, Spain, United Kingdom
NCT02327078 Phase 1
Archived
A Study of the Safety, Tolerability, and Efficacy of Epacadostat Administered in Combination With Nivolumab in Select Advanced Cancers (ECHO-204)
United States, United Kingdom