Drug intelligence / Profile preview

BMS-182874

Development stage
Discontinued
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

BMS-182874 is a **selective endothelin receptor type A (ETA) antagonist** classified as a small molecule drug. It was developed by Bristol Myers Squibb for cardiovascular diseases, with primary investigation for conditions such as hypertension and hyperproliferative vascular diseases. The drug functions by blocking ETA receptors, thereby inhibiting endothelin-1-mediated vasoconstriction and smooth muscle cell proliferation, processes implicated in diseases like restenosis. Studies show it reduces intimal lesion formation following vascular injury and offers renoprotective effects in diabetic nephropathy models, possibly through inhibition of the renin-angiotensin-aldosterone system and reactivation of NO synthesis[1][3]. Preclinical data also indicate it may enhance analgesic effects via imidazoline I2 receptor-mediated mechanisms[1].

Other names
BMS182874BMS-182874BMS 182874
02

Targets

EDNRB (Endothelin receptor type B)EDNRA (Endothelin receptor type A)

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