Key result
SPH3127 demonstrated higher bioavailability and a more potent antihypertensive effect in preclinical models than aliskiren, and has completed a phase II trial for essential hypertension.
Why the study?
Developing direct renin inhibitors with favorable oral bioavailability has been a longstanding challenge because most reported agents had peptide-like structures or molecular weights > 600.
Population
Preclinical models
Comparison
Compound 18 (SPH3127) vs aliskiren
Design
Preclinical drug discovery study
Authors
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SPH3127 merits further DRI development; animal data leave open translation to human hypertension.
SPH3127 is a novel, orally active direct renin inhibitor with improved bioavailability and antihypertensive efficacy compared to aliskiren in preclinical models.
Iijima et al. (2022) studied essential hypertension. SPH3127 vs. aliskiren was evaluated. SPH3127 demonstrated higher bioavailability and a more potent antihypertensive effect in preclinical models than aliskiren, and has completed a phase II trial for essential hypertension.
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