Product Name

Linaclotide

Name: Linaclotide - LGM Pharma
SKU: 851199-59-2

CAS Number

851199-59-2

LGM Pharma is an API distributor. LGM Pharma supplies APIs as per CGMP with DMF support, subject to availability and manufacturer requirements. LGM Pharma does not sell or supply APIs or finished dosage products to individual patients, doctors, or pharmacies.

Questions? Call our customer API support number 1-(800)-881-8210

Product Name:

Linaclotide

CAS Number:

851199-59-2

Indication:

Treatment of irritable bowel syndrome (IBS) with constipation and chronic idiopathic constipation.

Mode of Action:

Linaclotide is an agonist of guanylate cyclase-C (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. 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.

Pharmacodynamics:

Changes in the appearance and consistency of stools as measured by the Bristol Stool Form Scale (BSFS) have been noted after taking linaclotide.

Metabolism:

Linaclotide is metabolized within the gastrointestinal tract to its principal, active metabolite, MM-419447, by loss of the terminal tyrosine moiety. Both linaclotide and the metabolite are proteolytically degraded within the intestinal lumen to smaller peptides and naturally occurring amino acids.

Toxicity:

Most common adverse reactions (incidence of at least 2%) reported in IBS-C or CIC patients are diarrhea, abdominal pain, flatulence and abdominal distension.

PubChem:

16158208

Formula:

C59-H79-N15-O23-S6

Molecular Mass:

1526.7531

Synonyms:

Linaclotide, Linzess, UNII-N0TXR0XR5X

SMILES:

C[C@H]1C(=O)N[C@H]2CSSC[C@H]3C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@H](NC(=O)CNC(=O)[C@@H](NC2=O)[C@@H](C)O)C(=O)N[C@@H](Cc4ccc(cc4)O)C(=O)O)C(=O)N[C@@H](CSSC[C@@H](C(=O)N3)N)C(=O)N[C@H](C(=O)N5CCC[C@H]5C(=O)N1)CC(=O)N)Cc6ccc(cc6)O)CCC(=O)O

General Reference:

Busby RW, Kessler MM, Bartolini WP, Bryant AP, Hannig G, Higgins CS, Solinga RM, Tobin JV, Wakefield JD, Kurtz CB, Currie MG: Pharmacologic properties, metabolism, and disposition of linaclotide, a novel therapeutic peptide approved for the treatment of irritable bowel syndrome with constipation and chronic idiopathic constipation. J Pharmacol Exp Ther. 2013 Jan;344(1):196-206. doi: 10.1124/jpet.112.199430. Epub 2012 Oct 22. Pubmed

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

LGM currently offers Monoclonal Antibodies (mAbs) for non-GMP/R&D use. Please inquire about Monoclonal Antibodies produced under GMP conditions.

Questions? Call our customer API support number 1-(800)-881-8210.

Ask us about this product

API’s From Quality Manufacturers:

Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
Premium quality GMP certified and fully accredited API manufacturing plants
Technical packages as well as access to filed DMF, ASMF or CEP (subject to availability)
Regulatory and technical assistance towards any submission type based on specific customer requirements

Linaclotide

851199-59-2

Ask us about this product

API’s From Quality Manufacturers:

Find an API Product