Linaclotide

Irritable bowel syndrome and chronic constipation are common chronic functional diseases in the department of gastroenterology. Their recurrent symptoms severely affect patients' quality of life, and there has been an unmet clinical need for highly efficient and safe treatment regimens for a long time. Linaclotide is an active pharmaceutical ingredient (API) belonging to the guanylate cyclase C (GC-C) agonist class. By selectively activating GC-C receptors on the surface of intestinal epithelial cells, it increases the concentration of cyclic guanosine monophosphate (cGMP) inside and outside the cells. On the one hand, it promotes intestinal fluid secretion and accelerates intestinal peristalsis; on the other hand, it reduces the sensitivity of pain-sensing nerves and relieves abdominal pain symptoms. Clinically, it is indicated for the treatment of adult constipation-predominant irritable bowel syndrome (IBS-C), adult chronic idiopathic constipation (CIC) and functional constipation in children aged 6 to 17 years, and is a first-line treatment recommended by relevant guidelines.

The global market size related to linaclotide has maintained steady growth in recent years, exceeding 1.8 billion US dollars in 2024. The growth rate of the domestic market in recent years is significantly higher than the global average, with the compound annual growth rate remaining above 20%. At present, the original research product still dominates the domestic preparation market, and 3 domestic pharmaceutical companies have obtained approval for the marketing of generic drugs. As linaclotide capsules were included in the scope of the seventh batch of national centralized drug procurement, the price of winning bids has dropped by more than 70% compared with the highest price of the original research product, the market penetration rate continues to increase, which also drives the rapid growth of demand for upstream APIs.

The original research of linaclotide was jointly developed by AstraZeneca and Ironwood Pharmaceuticals, with the original brand name Linzess® (令泽舒®). Its core compound patent will expire in China in 2027, and patents in major overseas markets have expired successively. The main dosage form approved in China is capsule, with two specifications of 145μg and 290μg. Both the original research and domestic generic drug preparations have been included in the national reference preparation catalog. Up to now, linaclotide APIs from more than 10 domestic enterprises have completed registration with the Center for Drug Evaluation (CDE), and the preparation varieties approved for marketing include the original research product and 3 domestic generic drugs. (Data as of June 2025, please refer to the official CDE website for the latest information)

CATO can provide a full set of impurity reference standards for linaclotide API. Most of the products are in stock, and spot orders placed before 16:00 can be shipped on the same day. All products meet the compliance requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can provide stable and reliable reference standard support for the whole process of R&D, production and quality control of API and preparation enterprises.