Intestinal mucosal repair service

Linaclotide

Overview

Description A medication used to treat different types of constipation and conditions related to constipation.

DrugBank ID DB08890

Modality Small Molecule

Patents 12

Indicated Conditions 3

Clinical Trials

Phase 0 0

Phase 1 6

Phase 2 21

Phase 3 19

Phase 4 9

Therapeutic Categories

• Guanylate Cyclase-C Agonist

Mechanism of Action

• Guanylyl cyclase C Agonist

Identification

Summary

Linaclotide is a guanylate cyclase-C agonist used to treat different types of constipation, such as irritable bowel syndrome-related constipation, idiopathic constipation, and functional constipation.

Brand Names

Constella, Linzess

Generic Name Linaclotide

DrugBank Accession Number DB08890

Background

Linaclotide is a synthetic 14-amino acid cyclic peptide and first-in-class guanylate cyclase-C (G-CC) agonist. Linaclotide is structurally related to human guanylin and uroguanylin, paracrine peptide hormones that are endogenous activators of GC-C. It is also a homolog of a heat-stable enterotoxin derived from Escherichia coli, the first natural ligand that activates GC-C.

Linaclotide is used for the treatment of various types of constipation, including irritable bowel syndrome with constipation. Linaclotide was first approved by the FDA on August 30, 2012. It gained EMA and Health Canada approval on November 26, 2012 and December 3, 2013, respectively. Linaclotide works to improve the symptoms of constipation and gastrointestinal symptoms of conditions involving constipation.

Modality Small Molecule

Groups Approved, Investigational

Weight

Average: 1526.736

Monoisotopic: 1525.389918805

Chemical Formula

C 59 H 79 N 15 O 21 S 6

Synonyms

• (9-L-TYROSINE)HEAT-STABLE ENTEROTOXIN (ESCHERICHIA COLI)-(6-19)-PEPTIDE
• L-TYROSINE, L-CYSTEINYL-L-CYSTEINYL-L-.ALPHA.-GLUTAMYL-L-TYROSYL-L-CYSTEINYL-L-CYSTEINYL-L-ASPARAGINYL-L-PROLYL-L-ALANYL-L-CYSTEINYL-L-THREONYLGLYCYL-L-CYSTEINYL-, CYCLIC (1->6),(2->10),(5->13)-TRIS(DISULFIDE)
• Linaclotida
• Linaclotide

External IDs

• ASP-0456
• ASP0456
• MD-1100

Pharmacology

Indication

Linaclotide is indicated for the treatment of irritable bowel syndrome with constipation in adults. This indication is approved in the US, Canada, and Europe. In the US, linaclotide's indication has been updated to include treatment of irritable bowel syndrome with constipation (IBS-C) in both adults and pediatric patients 7 years of age and older.

In the US and Canada, it is also indicated for the treatment of chronic idiopathic constipation in adults.

In the US, it is also indicated for the treatment of functional constipation in pediatric patients 6 to 17 years of age.