molecules of the month


oral aldosterone synthase (CYP11B2) inhibitor

Ph. I/II for HTN, CKD, primary aldosteronism

from in-house screen of aldosterone synthase inhibitors

Press release, January 9, 2023

Roche, Basel, CH (AstraZeneca)

baxdrostat chemical structure oral aldosterone synthase (CYP11B2) inhibitor - Roche, Basel, CH (AstraZeneca)
6 mins read

What is it? Baxdrostat (RO6836191, CIN-107) is an oral aldosterone synthase (CYP11B2) inhibitor in several Ph. II trials (0.5-2 mg QD) for hypertension, CKD, and primary aldosteronism. The molecule is highly selective (>100x) against a cortisol synthesis enzyme, CYP11B1, allowing it to avoid negative effects due to cortisol reduction in the clinic, a longstanding challenge for clinical application of aldosterone synthase inhibitors. The molecule demonstrated dose-dependent PK/PD and overwhelming, trial-stopping efficacy in terms of reductions in systolic and diastolic blood pressure in hypertensive patients, contributing to the value of its recent $1.8B acquisition by AstraZeneca via CinCor. Originally discovered by Roche, it was out-licensed to a Cincinnati company with a 2022 IPO, CinCor, after Roche exited CV drug development, and…

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