molecules of the month


ROMK potassium channel blocker

oral eff. in hypertension model (1 mpk QD)

backup candidate to MK-7145 (Ph. Ib)

J. Med. Chem., May 26, 2021

Merck & Co., Kenilworth, NJ

1 min read

The Merck ROMK potassium channel blocker, MK-8153, is a backup development candidate to MK-7145, whose development as a diuretic was terminated after a Ph. Ib study due to lack of efficacy. Traditional loop diuretic drugs such as furosemide inhibit the Na-K-Cl co-transporter, but carry the risk of life-threatening urinary potassium loss. ROMK is a K channel that feeds K ions to NKCC, facilitating Na absorption, and ROMK inhibitors act as diuretics in animal models without the same levels of potassium loss. Objectives for the backup molecule included a longer half-life and better permeability to enable an extended release formulation. A lower peak-to-trough ratio was thought to be desirable since high peak-to-trough ratios lead to rebound sodium retention and reduced PD over…

request a trial

Drug Hunter is commited to helping industry innovators make informed decisions. Premium members have access to our library of the latest stories in science, written by scientists.

Request a trial to access insights powering the pros in our industry.

already a member? log in: