Drug intelligence / Profile preview

MK-0557

Development stage
Phase 3
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK‑0557 is a highly selective, orally available small molecule antagonist of the neuropeptide Y5 receptor (NPY5R), with a Ki of approximately 1.6 nM. Neuropeptide Y (NPY) is an orexigenic neuropeptide involved in appetite regulation and energy homeostasis. By antagonizing the NPY5 receptor, MK‑0557 was developed as a potential anti-obesity agent and also investigated for cognitive impairment in schizophrenia. Despite reaching phase III clinical trials for obesity and being studied in phase II trials for cognitive dysfunction in schizophrenia, development was discontinued due to limited efficacy in weight loss or prevention of weight regain after diet-induced weight loss[1][2][3][4][5][6][7].

Other names
328232-95-7AC-35453AC35453AC 35453DA-55513DA55513DA 55513FF158573FF-158573FF 158573HY-15411HY15411HY 15411MS-26961MS26961MS 26961N-[1-(2-fluorophenyl)pyrazol-3-yl]-1'-oxospiro[cyclohexane–4,3'-furo[3,4-c]pyridine]-1-carboxamide
02

Targets

NPY5R (Neuropeptide Y receptor type 5)

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