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Primary Target

Heat-stable enterotoxin receptor

3

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

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Serotonin 2a (5-HT2a) receptor

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Callisto Pharmaceuticals

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Other drugs for constipation

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Showing 1 - 3 of 3 results

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PLECANATIDE

7IK8Z952OK

Subunit 1 (16) Similarity Search

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Subunit 1 (16) Similarity Search

Status:

US Approved Rx (2017)

First approved in 2017

Class:

PROTEIN

Targets:

Heat-stable enterotoxin receptor

Conditions:

Chronic idiopathic constipation

Plecanatide (SP-304) is a synthetic, 16-amino acid peptide with 2 disulfide bonds that is a secondin-class guanylate cyclase-C (GC-C) receptor agonist. Plecanatide (brand name Trulance) was approved in January 2017 by the FDA for the treatment of chr...

onic idiopathic constipation (CIC). Plecanatide stimulates intestinal fluid secretions in the gastrointestinal tract to support regular bowel function. Plecanatide, taken orally once daily, works locally in the upper GI tract to stimulate secretion of intestinal fluid and support regular bowel function. Plecanatide is structurally related to human uroguanylin, and similar to uroguanylin, plecanatide functions as a guanylate cyclase-C (GC-C) agonist. Both plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation of intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit. In animal models, plecanatide has been shown to increase fluid secretion into the gastrointestinal (GI) tract, accelerate intestinal transit, and cause changes in stool consistency.

LINACLOTIDE

N0TXR0XR5X

Subunit 1 (14) Similarity Search

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Subunit 1 (14) Similarity Search

Status:

US Approved Rx (2012)

First approved in 2012

Class:

PROTEIN

Targets:

Heat-stable enterotoxin receptor

Conditions:

Irritable bowel syndrome

Linaclotide (marketed under the trade name Linzess and Constella) is a peptide agonist of the guanylate cyclase 2C (GC-C). Once linaclotide and its active metabolite binds to GC-C, it has local effect on the luminal surface of the intestinal epitheli...

um. Activation of GC-C by linaclotide results in the intra- and extracellular increase of cyclic guanosine monophosphate concentrations (cGMP). This elevation of cGMP levels stimulates the secretion of chloride and bicarbonate into the intestinal lumen via activation of cystic fibrosis transmembrane conductance regulator (CFTR) ion channel. The metabolite of linaclotide MM-419447 (CCEYCCNPACTGC) contributes to the pharmacologic effects of linaclotide. Ultimately, linaclotide helps patients with IBS (especially with constipation) as GI transit is accelerated and the release of intestinal fluid is increased. In animal models, a decrease in visceral pain after administration of linaclotide may be observed. A decrease in the activity of pain-sensing nerves occurs as a result of an increase in extracellular cGMP. It was approved by the FDA in August 2012 for the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation (IBS-C) in adults.

LINACLOTIDE ACETATE

NSF067KU1M

Subunit 1 (14) Similarity Search

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Subunit 1 (14) Similarity Search

Status:

US Approved Rx (2012)

First approved in 2012

Class:

PROTEIN

Targets:

Heat-stable enterotoxin receptor

Conditions:

Irritable bowel syndrome

Linaclotide (marketed under the trade name Linzess and Constella) is a peptide agonist of the guanylate cyclase 2C (GC-C). Once linaclotide and its active metabolite binds to GC-C, it has local effect on the luminal surface of the intestinal epitheli...

um. Activation of GC-C by linaclotide results in the intra- and extracellular increase of cyclic guanosine monophosphate concentrations (cGMP). This elevation of cGMP levels stimulates the secretion of chloride and bicarbonate into the intestinal lumen via activation of cystic fibrosis transmembrane conductance regulator (CFTR) ion channel. The metabolite of linaclotide MM-419447 (CCEYCCNPACTGC) contributes to the pharmacologic effects of linaclotide. Ultimately, linaclotide helps patients with IBS (especially with constipation) as GI transit is accelerated and the release of intestinal fluid is increased. In animal models, a decrease in visceral pain after administration of linaclotide may be observed. A decrease in the activity of pain-sensing nerves occurs as a result of an increase in extracellular cGMP. It was approved by the FDA in August 2012 for the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation (IBS-C) in adults.

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