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Drug intelligence / Profile preview
MK-0533
- Development stage
- Discontinued
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
MK-0533 is a novel, investigational small molecule developed as a selective modulator of peroxisome proliferator-activated receptor gamma (PPARγ) for the treatment of type 2 diabetes mellitus. Unlike full PPARγ agonists such as rosiglitazone and pioglitazone, MK-0533 acts as a partial agonist, displaying diminished maximal activity in cell-based transcription assays and attenuated gene signatures in adipose tissue. In preclinical studies, it demonstrated comparable efficacy to existing thiazolidinediones but with reduced side effects related to fluid retention and cardiac hypertrophy. Clinical development reached phase II trials before being discontinued[2][4][9].
02
Targets
PPARG (Peroxisome proliferator-activated receptor gamma)
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