Talk:Aliskiren

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Chemistry
The 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
Aliskiren, 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)