First IBS-C drug linaclotide approved in China

AstraZeneca in2019Year1Month15The State Drug Administration (NMPA) has officially approved the world's first (First in class) Guanylate cyclase agonistsLinzess(linaclotide,Linaclotide) is listed in China as a specialized treatment for adult constipation-predominant irritable bowel syndrome (IBS-C) of prescription drugs.

2012Year8Month, linaclotideFDAApprovedIBS-Cand treatment of patients with chronic idiopathic constipation, trade nameLinzessThe drug is the world's first approved guanylate cyclase for the treatment of constipation.Cagonists; in addition,2017Year2month,FDAApproved72Timogof linaclotide for chronic idiopathic constipation (CIC) Treatment of adult patients. In the Japanese market,LinzessIn2016Year12Approved in the month to become a treatmentIBS-CThe first prescription drug, and on2017Year3It is listed in Japan last month.

As of now, linaclotide has been30A number of countries have been approved for listing, becoming a globalIBS-CThe leading prescription drug in the field of treatment.

Constipation-irritable predominant bowel syndrome(Irritable Bowel Syndrome with Constipation, IBS-C)

Irritable bowel syndrome (IBS) is a common clinical functional bowel disease, constipation-predominant irritable bowel syndrome (IBS-C) is one of the subtypes. The main clinical symptoms are recurrent constipation, accompanied by abdominal pain, abdominal distension and abdominal discomfort related to defecation. Because of its recurrent attacks, the quality of life of patients is affected.

In China,IBSThe prevalence of up6.5%, in which15%ForIBS-CIt is estimated that the current domestic patient population of this type is about1400Ten thousand. However, prior to the domestic listing of linaclotide,IBS-CThe treatment of patients is mainly based on symptoms such as antispasmodic, osmotic laxatives and other types of drugs, China has been the lack of targeted and effective treatment drugs, the approval of linaclotide in China will bring new and effective treatment options for Chinese doctors and the majority of patients, to fill the adult population in China.IBS-CGaps in the field of treatment.

chronic idiopathic constipation(Chronic Idiopathic Constipation, CIC)

Chronic functional constipation is a group of multi-population onset, multi-factor existence, with difficulty in defecation, discomfort in defecation and prolonged defecation as the main symptoms of the syndrome, according to the etiology can be divided into primary (idiopathic) constipation and secondary constipation, of which idiopathic constipation is also known as "refractory" or "primary" because of its unclear etiology and difficult treatment ".CICwithIBS-CSimilarly, clinical symptoms often overlap between the two, distinguished primarily by abdominal symptoms,IBS-CAbdominal pain symptoms are not relieved by defecation.

According to statistics,IBSThe global incidence is approximately11%,CICAbout14%The pathogenesis of both are more complex, although it is generally not considered to be associated with certain serious diseases or higher mortality, but it seriously affects the quality of life of patients.

Drug Introduction

Chinese name: Linaclotide

English name:Linaclotide

Trade name: Ling Zeshu®(Linzess®)

linaclotide is a guanylate cyclase-C(GC-C) Agonist, the structure is containing.14An amino acid polypeptide that binds to and acts locally on intestinal epithelial cellsGC-Creceptor,GC-CThe activation of leads to the intracellular and extracellular loop guanosine phosphate (cGMP) The concentration is increased, and the intracellularcGMPElevation stimulates the secretion of chloride and bicarbonate ions into the intestinal lumen, resulting in increased and accelerated passage of intestinal secretions. In animal models, linaclotide has also been shown to reduce pain in the small intestine, which is thought to be extracellular.cGMPThe increase is mediated by a decrease in the activity of intestinal pain-sensing nerves thereby inducing a reduction in visceral pain.

Patent Information

Linaclotide is registered in the American Orange Book.10Related U.S. patents, there are7All patents in the United States have been granted, while two patents in China are still in the substantive examination stage.