Active Ingredient History

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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 epithelium. 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.   NCATS

  • SMILES: C[C@@H](O)[C@@H]1NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@H](CSSC[C@H](NC(=O)CNC1=O)C(=O)N[C@@H](Cc4ccc(O)cc4)C(=O)O)NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CCC(=O)O)NC3=O)C(=O)N[C@@H](CC(=O)N)C(=O)N6CCC[C@H]6C(=O)N[C@@H](C)C(=O)N2
  • InChIKey: KXGCNMMJRFDFNR-WDRJZQOASA-N
  • Mol. Mass: 1526.77
  • ALogP: Missing data
  • ChEMBL Molecules:
More Chemistry
  • Mechanisms of Action:
  • Multi-specific: No
  • Black Box: Yes
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$10.4133 - $14.9436
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

constella | cys cys glu tyr cys cys asn pro ala cys thr gly cys tyr (disulfide bridge: 1-6; 2-10; 5-13) | 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-l-tyrosine cyclic (1->6),(2->10),(5->13)-tris(disulfide) | linaclotide | linaclotide acetate | linzess | md-1100 | md-1100 acetate | mm-416775

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