Nisoldipine

In response to the long-term antihypertensive needs of patients with hypertension complicated by coronary artery disease, dihydropyridine calcium channel blockers have always been the first-line clinical choice due to their advantages of high vascular selectivity and mild adverse reactions. As a second-generation drug of this category, nisoldipine highly specifically blocks L-type calcium channels on the membrane of vascular smooth muscle cells, reduces calcium ion influx, and effectively dilates peripheral arteries and coronary arteries. It has a long-lasting antihypertensive effect and exerts minimal impact on heart rate and myocardial contractility. It is mainly used clinically for the treatment of essential hypertension and ischemic heart disease, especially suitable for elderly hypertensive patients with concomitant coronary heart disease, and can simultaneously reduce the risk of cardiovascular events.

The market size of antihypertensive drugs in China has exceeded RMB 110 billion, with calcium channel blockers accounting for nearly 30%, among which the annual growth rate of second-generation long-acting preparations remains above 7%. Nisoldipine has the dual benefits of both antihypertensive effect and coronary protection, so its market demand continues to be stable. At present, the domestic preparation market is dominated by generic drugs, and more than 20 enterprises have obtained preparation approval documents. The supply of active pharmaceutical ingredients (APIs) has been basically localized, and the winning bid price has dropped by about 82% compared with that in the initial stage of the original drug's launch, greatly improving the accessibility of medication for patients.

The original developer of nisoldipine is Bayer, with the original brand name Nisoldipine Sular. The core compound patent expired globally in 2007, and the patent for the sustained-release dosage form in the US market also expired in 2018. The main dosage form approved for the original drug is sustained-release tablets, with specifications including 10mg, 20mg, 30mg and 40mg, which has been included in the FDA Reference Listed Drug Catalogue. The original preparation has not been imported into China yet. At present, the nisoldipine APIs of 8 domestic enterprises have obtained Class A status through CDE registration, and the APIs of another 3 enterprises are under the review stage. A number of domestic preparations such as nisoldipine tablets and nisoldipine sustained-release capsules have been approved for marketing. (Data as of July 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for nisoldipine API, covering all types of reference standards including starting material impurities, degradation impurities, enantiomers and others involved in the synthetic route. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All reference standards comply with the regulatory requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and can directly support the API registration declaration and quality research work.