National Cancer Institute Thesaurus

Last uploaded: February 23, 2024
Preferred Name

Linaclotide
Synonyms

Linaclotide

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)

LINACLOTIDE

[9-L-tyrosine]heat-stable enterotoxin (Escherichia coli)-(6-19)-peptide

Linzess

MD-1100

Definitions

A synthetic, fourteen amino acid peptide and agonist of intestinal guanylate cyclase type C (GC-C), which is structurally related to the guanylin peptide family, with secretagogue, analgesic and laxative activities. Upon oral administration, linaclotide binds to and activates GC-C receptors located on the luminal surface of the intestinal epithelium. This increases the concentration of intracellular cyclic guanosine monophosphate (cGMP), which is derived from guanosine triphosphate (GTP). cGMP activates the cystic fibrosis transmembrane conductance regulator (CFTR) and stimulates the secretion of chloride and bicarbonate into the intestinal lumen. This promotes sodium excretion into the lumen and results in increased intestinal fluid secretion. This ultimately accelerates GI transit of intestinal contents, improves bowel movement and relieves constipation. Increased extracellular cGMP levels may also exert an antinociceptive effect, through an as of yet not fully elucidated mechanism, that may involve modulation of nociceptors found on colonic afferent pain fibers. Linaclotide is minimally absorbed from the GI tract.

ID

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C81001

Accepted_Therapeutic_Use_For

Treatment of irritable bowel syndrome with constipation (IBS-C), chronic constipation and other gastrointestinal disorders

CAS_Registry

851199-59-2

Chemical_Formula

C59H79N15O21S6

code

C81001

Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C63923

Contributing_Source

CTRP

FDA

DEFINITION

A synthetic, fourteen amino acid peptide and agonist of intestinal guanylate cyclase type C (GC-C), which is structurally related to the guanylin peptide family, with secretagogue, analgesic and laxative activities. Upon oral administration, linaclotide binds to and activates GC-C receptors located on the luminal surface of the intestinal epithelium. This increases the concentration of intracellular cyclic guanosine monophosphate (cGMP), which is derived from guanosine triphosphate (GTP). cGMP activates the cystic fibrosis transmembrane conductance regulator (CFTR) and stimulates the secretion of chloride and bicarbonate into the intestinal lumen. This promotes sodium excretion into the lumen and results in increased intestinal fluid secretion. This ultimately accelerates GI transit of intestinal contents, improves bowel movement and relieves constipation. Increased extracellular cGMP levels may also exert an antinociceptive effect, through an as of yet not fully elucidated mechanism, that may involve modulation of nociceptors found on colonic afferent pain fibers. Linaclotide is minimally absorbed from the GI tract.

Display_Name

Linaclotide

FDA_UNII_Code

N0TXR0XR5X

FULL_SYN

Linaclotide

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)

LINACLOTIDE

[9-L-tyrosine]heat-stable enterotoxin (Escherichia coli)-(6-19)-peptide

Linzess

MD-1100

Has_Salt_Form

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C77223

label

Linaclotide

Legacy Concept Name

Linaclotide

Preferred_Name

Linaclotide

prefixIRI

Thesaurus:C81001

PubMedID_Primary_Reference

19098860

Semantic_Type

Pharmacologic Substance

UMLS_CUI

C2000261

subClassOf

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C548

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