Drug intelligence / Profile preview

MK-0873

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

Overview

MK‑0873 is a selective small molecule inhibitor of phosphodiesterase 4 (PDE4), developed as an anti-inflammatory agent. It was investigated for the treatment of chronic obstructive pulmonary disease (COPD), rheumatoid arthritis, and plaque psoriasis. By inhibiting PDE4, it increases intracellular cyclic adenosine monophosphate (cAMP) levels, leading to reduced production of pro-inflammatory cytokines and chemokines. Preclinical studies demonstrated potent inhibition of antigen-induced bronchoconstriction and anti-inflammatory effects in animal models. Clinical trials showed that it was generally well tolerated but development has been discontinued[1][2][3][5][6][7].

Other names
N-Cyclopropyl-1-(3-((1-oxidopyridin-3-yl)ethynyl)phenyl)-1,4-dihydro(1,8)naphthyridin-4-one-3-carboxamideN-cyclopropyl-1-[3-[2-(1-oxidopyridin-1-ium-3-yl)ethynyl]phenyl]-4-oxo-1,8-naphthyridine‑3-carboxamide– CHEMBL485629
02

Targets

PDE4 (Phosphodiesterase 4A1)

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