Linaclotide

Classification

Guanylate cyclase-C agonist (14-amino-acid peptide)

Approval status

Approved medicine

Research status

Labelled indications are defined in product information.

Molecular formula

Insufficient reliable evidence identified.

Molecular weight

Insufficient reliable evidence identified.

Sequence

Oral peptide that acts locally in the intestine with minimal systemic absorption as labelled.

Primary biological target

Guanylate cyclase-C

Half-life

Insufficient reliable evidence identified.

Routes investigated

Oral

Human evidence level

A — Approved clinical use / strong human evidence

An approved oral peptide medicine for irritable bowel syndrome with constipation and chronic idiopathic constipation, as labelled.

Established (labelled / textbook receptor pharmacology)

Binds guanylate cyclase-C on intestinal epithelium, increasing cGMP, chloride/bicarbonate secretion (CFTR) and reducing visceral pain signalling in labelled pharmacology.

Increases intestinal fluid and accelerates transit in labelled CIC/IBS-C populations.

• IBS-C
• Chronic idiopathic constipation

Investigational findings are not proven clinical benefits unless an authority has labelled that indication.

Overall human evidence grade: A · Approved clinical use / strong human evidence

Phase 3 programmes support labelled GI indications.

Animal, cell and in-vitro findings are listed separately from human effects.

GC-C / cGMP pathway characterised in intestinal models.

This section does not provide personalised medical dosing. Values are those reported in papers or protocols. Animal mg/kg doses are not converted to human doses.

Doses reported in human studies

Insufficient reliable evidence identified.

Preclinical / animal study dosing

Insufficient reliable evidence identified.

Reliable human pharmacokinetic data were not identified for this encyclopaedia entry, or are limited to product information for approved presentations.

Diarrhoea is the principal labelled adverse effect; dehydration risk.

Unknowns. Absence of a published harm signal is not evidence of safety.

Contraindications. Paediatric boxed warning in USPI for children under 6; see PI.

Approved (FDA/EMA) for specified constipation disorders.

Verify ARTG for linaclotide. Not sold here.

1. [1] Linaclotide prescribing information

   Linaclotide prescribing information

   Open source