Drug intelligence / Profile preview

MK-0359

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

Overview

MK-0359 (also known as L-454560) is a selective and potent small molecule inhibitor of type 4 phosphodiesterases (PDE4). It acts by competitively and reversibly inhibiting PDE4, binding to both the apo-(Mg2+-free) and holoenzyme states. The drug was developed for oral administration and has demonstrated high potency in preclinical models, with nanomolar inhibitory activity against several PDE4 isoforms. Clinical development reached Phase 2 trials for asthma, chronic obstructive pulmonary disease (COPD), and rheumatoid arthritis. Despite promising results in these indications, further development appears to have been discontinued or is pending with no recent updates on approval or ongoing trials[1][2][5].

Other names
MK-0359 besylateMK0359 besylateMK 0359 besylateL-454560L454560L 454560
02

Targets

PDE4APDE4B (3',5'-cyclic-AMP phosphodiesterase 4B)PDE4D (Phosphodiesterase 4D)

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