Linaclotide

Category: pharmacological

Aliases: Linzess

Pharmacological Mechanism

GC-C (guanylate cyclase-C) agonist — raises intestinal cGMP → CFTR-mediated chloride / bicarbonate / water secretion into lumen. Approved for chronic idiopathic constipation + IBS-C. Minimal systemic absorption → DDI-light. Diarrhea is the main dose-limiting side effect.

Half-Life (t½)

PO: 1h

Dosing Guidelines

• PO: Typical 0.145 mg (Range: 0.072–0.29 mg)

Target Organ Systems

• digestive

Pathways It Modulates

• GI motility + secretion (activator) — guanylate cyclase-C (GC-C)

Chemical Identifiers

• PubChem CID: 16158208
• Formula: C59H79N15O21S6
• Molecular weight: 1526.74 g/mol
• InChIKey: KXGCNMMJRFDFNR-WDRJZQOASA-N
• 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](CC4=CC=C(C=C4)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)CC6=CC=C(C=C6)O)CCC(=O)O

References

• PMID 20863829