Linaclotide

Guanylate Cyclase-C Agonist — ALIMENTARY TRACT AND METABOLISM

Key facts

Linaclotide is a drug in the Guanylate Cyclase-C Agonist class catalogued in DrugCentral. It was first approved by the FDA in 2012. Its mechanism of action is classified as Guanylate Cyclase Activators. DrugCentral lists 2 molecular targets, including GUCY2C and Gucy2c. Recorded indications include Chronic idiopathic constipation, Irritable bowel syndrome and Irritable bowel syndrome characterized by constipation.

• Drug class: Guanylate Cyclase-C Agonist.
• Mechanism of action: Guanylate Cyclase Activators.
• Molecular targets: GUCY2C and Gucy2c (2 listed in DrugCentral).
• Indications: Chronic idiopathic constipation, Irritable bowel syndrome and Irritable bowel syndrome characterized by constipation.
• ATC code: A06AX04 (Other drugs for constipation).
• Molecular formula: C59H79N15O21S6; molecular weight 1526.73 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Chronic idiopathic constipation
• Irritable bowel syndrome
• Irritable bowel syndrome characterized by constipation

Mechanism & targets

• Mechanism of action (MoA): Guanylate Cyclase Activators
• Established pharmacologic class: Guanylate Cyclase-C Agonist

Molecular targets (2)

Target	Gene	Action	Activity
Heat-stable enterotoxin receptor	GUCY2C	agonist	Ki 8.91
Heat-stable enterotoxin receptor	Gucy2c	agonist	Ki 8.38

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2016-12-19	PMDA	—	ASTELLAS PHARMA INC.
2012-08-30	FDA	—	FOREST LABS LLC

ATC classification

ATC code	Therapeutic hierarchy
A06AX04	ALIMENTARY TRACT AND METABOLISM › DRUGS FOR CONSTIPATION › DRUGS FOR CONSTIPATION › Other drugs for constipation

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Product dispensing error	614.5
Product storage error	567.7
Diarrhoea	191.9
Constipation	152.6
Product dose omission issue	122.2
Abdominal distension	94.5
Product packaging issue	67.3
Inappropriate schedule of product administration	60.5
Surgery	56.0
Incorrect dose administered	55.5
Pemphigus	53.2
Illness	53.1

Chemical structure

• Molecular formula: C₅₉H₇₉N₁₅O₂₁S₆
• Molecular weight: 1526.73 g/mol
• CAS number: 851199-59-2
• InChIKey: KXGCNMMJRFDFNR-WDRJZQOASA-N
• PubChem CID: 16158208

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](CC1=CC=C(O)C=C1)C(O)=O)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CCC(O)=O)NC3=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Linaclotide used for?

DrugCentral lists the following indications for Linaclotide: Chronic idiopathic constipation, Irritable bowel syndrome and Irritable bowel syndrome characterized by constipation.

How does Linaclotide work?

Linaclotide is classified as Guanylate Cyclase Activators; its molecular targets in DrugCentral include GUCY2C (agonist) and Gucy2c (agonist).

When was Linaclotide first approved?

Linaclotide was first approved by the FDA in 2012.

What drug class does Linaclotide belong to?

Linaclotide is in the Guanylate Cyclase-C Agonist class.

What is the chemical formula of Linaclotide?

Linaclotide has the molecular formula C59H79N15O21S6 and a molecular weight of 1526.73 g/mol.

Sources

• DrugCentral drug card 4622 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3301675 — compound record and bioactivity
• PubChem CID 16158208 — chemical identifiers
• DrugBank DB08890 — drug record
• FDA UNII N0TXR0XR5X — substance identity
• DailyMed: FDA labels for Linaclotide — current prescribing information (label search)
• UniProt P25092 (GUCY2C) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.