Talk:Aliskiren
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Chemistry
editThe hydroxyl group of aliskiren forms hydrogen bonds with both oxygen atoms of Asp32. The amine group forms hydrogen bonds with Gly217's carboxylic acid group and Asp32's oxygen atom. The aromatic ring's methoxy group fills the S3 pocket, potentially forming a hydrogen bond with Tyr14's secondary amine. Aliskiren’s amide group forms a hydrogen bond with Ser76's secondary amine. Additionally, aliskiren selectively binds to the S3sp sub-pocket, contributing to its specificity as a renin inhibitor. The binding is stabilized by these hydrogen bonds, showcasing the specificity and potency of aliskiren as a renin inhibitor. Angeliki Giorgalli (talk) 16:06, 25 February 2024 (UTC)
Basic Pharmacokinetics
editAliskiren, a hydrophilic renin inhibitor (logP= 2.45), displays exceptional selectivity and high aqueous solubility(>350 mg/ml), with favourable pharmacokinetics supporting once-daily dosing. Metabolism occurs via CYP3A4, and despite low oral bioavailability (2.5%), its extensive tissue uptake and limited interactions make it a promising antihypertensive drug. (Vd= 135 L) Aliskiren’s main route of elimination is via faeces, supported by a study which detected radio-labeled aliskiren showing more than 80% was found in faeces. Angeliki Giorgalli (talk) 16:08, 25 February 2024 (UTC)