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1g
Linaclotide API | 1g
Produced in China | COA | GMP certified $ 1,290
2g
Linaclotide API | 2g
Produced in China | COA | GMP certified $ 2,581
5g
Linaclotide API | 5g
Produced in China | COA | GMP certified $ 6,453
Custom
Linaclotide API | Custom
Produced in China | COA | GMP certified On Request
Distributor
CDMO
Produced in Asia
Employees: 50+
Audit Report: Currently Eurofins has no report for this supplier. Contact them to let them know you are interested!
Certifications: CoA
CEP
See all 6 certificates
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Producer
Employees: 1500+
GMP
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Employees: 373
See all 8 certificates
Produced in North America
Produced in Europe
Employees: 200+
Employees: 250+
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Employees: 25
Employees: 1000+
Employees: 10+
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Produced in South America
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Procaps
Pfizer
Reckitt
Sanofi
Blau
Abbvie
A medication that treats irritable bowel syndrome with constipation and other persistent constipation conditions, helping improve bowel regularity across key therapeutic markets.
Alimentary Tract and Metabolism Amino Acids, Peptides, and Proteins Drugs for Constipation Enzyme Activators Gastrointestinal Agents Guanylate Cyclase Activators
Linaclotide
small molecule
851199-59-2
DB08890
Approved drug
A06AX04
Linaclotide (CAS 851199-59-2) is a synthetic 14‑amino acid cyclic polypeptide and first‑in‑class guanylate cyclase‑C agonist structurally related to the endogenous peptides guanylin and uroguanylin. It is approved for the treatment of irritable bowel syndrome with constipation in adults across the US, Canada, and Europe. In the US and Canada, it is also indicated for chronic idiopathic constipation in adults, and in the US it is approved for functional constipation in pediatric patients 6 to 17 years of age.
The drug acts locally in the intestinal lumen and is minimally absorbed. Its pharmacodynamic profile reflects both secretory and visceral analgesic effects. Binding to membrane‑bound guanylate cyclase‑C on intestinal epithelial cells increases intracellular and extracellular cyclic GMP. Activation of intracellular cyclic GMP stimulates protein kinase II, which phosphorylates and activates the CFTR chloride channel. Resulting chloride and bicarbonate secretion, together with reduced sodium absorption, enhances luminal fluid content and accelerates gastrointestinal transit. Elevated extracellular cyclic GMP in the submucosa contributes to reduced visceral hypersensitivity by dampening nociceptor activity.
Key ADME characteristics include negligible systemic bioavailability, local metabolism to an active metabolite in the gastrointestinal tract, and degradation into small peptides and amino acids. Because systemic exposure is minimal, classical plasma pharmacokinetic parameters are not informative. Food intake with high fat content can increase stool looseness and frequency.
Safety considerations mainly relate to its pharmacological activity, with diarrhea being the most common adverse effect and a potential cause of dehydration. Use is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction. Pediatric safety is age dependent, with approved use limited to defined populations.
Linaclotide is marketed under brands such as Linzess and Constella. For API procurement, sourcing should prioritize peptide integrity, control of cyclic structure, and robust analytical verification of identity, purity, and potency, given its susceptibility to degradation and the need for consistent biological activity.
