Aliskiren

Overactivation of the renin-angiotensin-aldosterone system (RAAS) is one of the core pathological mechanisms underlying the onset and progression of hypertension. As the first non-peptide oral direct renin inhibitor, aliskiren has a mechanism of action different from that of traditional ACEI and ARB drugs. It can block the cleavage process of angiotensinogen catalyzed by renin from the initial link of RAAS activation, effectively lowering blood pressure while reducing target organ damage. It is clinically mainly used for the treatment of essential hypertension. It can be used as a single agent for patients intolerant to ACEI or ARB, and can also be used in combination with thiazide diuretics, calcium channel blockers, etc., to improve the control and compliance rate of refractory hypertension. The applicable population covers adult hypertensive patients and some groups with comorbidities who require intensive blood pressure lowering.

The global market size of antihypertensive drugs has maintained steady growth for a long time, among which RAAS inhibitors account for approximately 30%. As the only direct renin inhibitor antihypertensive drug, the global peak sales of aliskiren-related preparations once approached US$1.2 billion in 2010. Subsequently, the market size declined due to factors such as indication restrictions and iteration of competing products. At present, the global market is mainly supplied by generic drugs. In terms of the domestic market, aliskiren oral preparations were first approved for import in 2010. They have not yet been included in the national centralized volume-based procurement, and the number of applications for domestic generic preparations is small, so there is still certain market space on the API supply side.

The original research enterprise of aliskiren is Novartis, and the original brand name is "Rasilez". The expiration date of its core compound patent in the United States is 2017, and the core compound patent in China expired in 2017. The dosage form of the original marketed product is film-coated tablet, with specifications of 150mg and 300mg. The original preparation has been included in the Reference Listed Drug Catalogue published by NMPA, and is also included in the FDA Reference Listed Drug Catalogue. Up to now, no domestic enterprise has obtained the A-status registration number of aliskiren API. Only the original imported preparation has been approved for marketing, and no domestic aliskiren preparation has been approved. (Data as of June 2025, please refer to the official website of CDE for the latest information)

CATO can provide a full set of aliskiren impurity reference standards, most of which are available from stock. Stock orders placed before 16:00 can be shipped on the same day. All reference standards meet the requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can fully meet the full-process needs of API R&D, quality research and compliance declaration.