molecules of the month


oral Renin Inhibitor

Ph. III candidate in essential hypertension

SBDD and PK profile opt

J. Med. Chem.

Mitsubishi Tanabe, Yokohama, JPShanghai Pharmaceuticals, Shanghai, CN

SPH3127 chemical structure oral Renin Inhibitor - Mitsubishi Tanabe, Yokohama, JP Shanghai Pharmaceuticals, Shanghai, CN
5 mins read

Context. SPH3127 (Mitsubishi Tanabe and Shanghai Pharmaceuticals) is an oral direct renin inhibitor (DRI) being developed for hypertension. The renin-angiotensin-aldosterone system is responsible for regulating blood pressure. Existing drugs treat hypertension by targeting angiotensin-converting enzyme (ACE) and the angiotensin II receptor. However, these drugs can lead to a feedback effect whereby plasma serum levels become elevated. Renin, the pathway’s first and rate-limiting enzyme, has been an attractive therapeutic target for decades since the identification of peptide-like renin inhibitors and renin’s structural determination. First and second-generation renin inhibitors were peptide analogues and transition state peptidomimetics, while third-generation compounds, guided by structure-based design, yielded non-peptidomimetic synthetic compounds such as aliskiren, which was approved in 2007. Aliskiren suffered from low oral bioavailability, and…

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