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

You don’t have time to read everything, but you can’t afford to fall behind.

Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples.

Get ahead now by requesting a trial.

already a member? log in: