Linaclotide
Generic Name: linaclotide
Brand Names:
Linzess
11 DESCRIPTION LINZESS (linaclotide) is a guanylate cyclase-C (GC-C) agonist. Linaclotide is a 14-amino acid peptide with the following chemical name: L-cysteinyl-L-cysteinyl-L-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonyl-glycyl-L-cysteinyl-L-tyrosine, cyclic (1-6), (2-10), (5-13)-tris (disulfide). The molecular formula of linaclotide is C 59 H 79 N 15 O 21 S 6 and its molecular weight is 1526.8.
Overview
11 DESCRIPTION LINZESS (linaclotide) is a guanylate cyclase-C (GC-C) agonist. Linaclotide is a 14-amino acid peptide with the following chemical name: L-cysteinyl-L-cysteinyl-L-glutamyl-L-tyrosyl-L-cysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonyl-glycyl-L-cysteinyl-L-tyrosine, cyclic (1-6), (2-10), (5-13)-tris (disulfide). The molecular formula of linaclotide is C 59 H 79 N 15 O 21 S 6 and its molecular weight is 1526.8.
Uses
1 INDICATIONS AND USAGE LINZESS is indicated for the treatment of: • irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older • chronic idiopathic constipation (CIC) in adults • functional constipation (FC) in pediatric patients 6 years of age and older LINZESS is a guanylate cyclase-C agonist indicated for treatment of: Irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older. ( 1 ) Chronic idiopathic constipation (CIC) in adults. ( 1 ) Functional constipation (FC) in pediatric patients 6 years of age and older. ( 1 )
Dosage
2 DOSAGE AND ADMINISTRATION The recommended dosage in adults is: IBS-C : 290 mcg orally once daily. ( 2.1 ) CIC : 145 mcg orally once daily or 72 mcg orally once daily based on individual presentation or tolerability. ( 2.1 ) The recommended dosage in pediatric patients: 7 years of age and older with IBS-C : 145 mcg orally once daily. ( 2.1 ) 6 years of age and older with FC : 72 mcg orally once daily. ( 2.1 ) Administration Instructions ( 2.2 ): Take on empty stomach at least 30 minutes prior to a meal at approximately the same time each day. Do not crush or chew LINZESS capsule or capsule contents.
Side Effects
6 ADVERSE REACTIONS Most common adverse reactions (≥2%) reported in adult patients with IBS-C or CIC are: diarrhea, abdominal pain, flatulence and abdominal distension. ( 6.1 ) Most common adverse reaction (≥2%) reported in pediatric patients with FC or IBS-C is diarrhea. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact AbbVie, Inc. at 1-800-678-1605 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Warnings
WARNING: RISK OF SERIOUS DEHYDRATION IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE LINZESS is contraindicated in patients less than 2 years of age; in nonclinical studies in neonatal mice, administration of a single, clinically relevant adult oral dose of linaclotide caused deaths due to dehydration [see Contraindications ( 4 ), Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.4 )]. 5 WARNINGS AND PRECAUTIONS Diarrhea: Patients may experience severe diarrhea. If severe diarrhea occurs, suspend dosing and rehydrate the patient. ( 5.2 ) 5.1 Risk of Serious Dehydration in Pediatric Patients Less Than 2 Years of Age LINZESS is contraindicated in patients less than 2 years of age. In neonatal mice (human age equivalent of approximately 0 to 28 days), linaclotide increased fluid secretion as a consequence of age-dependent elevated GC-C agonism which was associated with increased mortality within the first 24 hours due to dehydration. 4 CONTRAINDICATIONS LINZESS is contraindicated in: Patients less than 2 years of age due to the risk of serious dehydration [see Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.4 )] . Patients with known or suspected mechanical gastrointestinal obstruction. Patients less than 2 years of age.
Pregnancy
8. 1 Pregnancy Risk Summary Linaclotide and its active metabolite are negligibly absorbed systemically following oral administration [see Clinical Pharmacology ( 12.3 )] , and maternal use is not expected to result in fetal exposure to the drug. The available data on LINZESS use in pregnant women are not sufficient to inform any drug-associated risk for major birth defects and miscarriage.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied LINZESS Capsule Strength Description Packaging NDC number 72 mcg White to off-white opaque hard gelatin capsules with gray imprint “FL 72” Bottle of 30 0456-1203-30 145 mcg White to off-white opaque hard gelatin capsules with gray imprint "FL 145" Bottle of 30 0456-1201-30 290 mcg White to off-white opaque hard gelatin capsules with gray imprint "F...
Frequently Asked Questions
What is Linaclotide used for?▼
1 INDICATIONS AND USAGE LINZESS is indicated for the treatment of: • irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older • chronic idiopathic constipation (CIC) in adults • functional constipation (FC) in pediatric patients 6 years of age and older LINZESS is a guanylate cyclase-C agonist indicated for treatment of: Irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older. ( 1 ) Chronic idiopathic constipation (CIC) in adults. ( 1 ) Functional constipation (FC) in pediatric patients 6 years of age and older. ( 1 )
What are the side effects of Linaclotide?▼
6 ADVERSE REACTIONS Most common adverse reactions (≥2%) reported in adult patients with IBS-C or CIC are: diarrhea, abdominal pain, flatulence and abdominal distension. ( 6.1 ) Most common adverse reaction (≥2%) reported in pediatric patients with FC or IBS-C is diarrhea. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact AbbVie, Inc. at 1-800-678-1605 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Can I take Linaclotide during pregnancy?▼
8. 1 Pregnancy Risk Summary Linaclotide and its active metabolite are negligibly absorbed systemically following oral administration [see Clinical Pharmacology ( 12.3 )] , and maternal use is not expected to result in fetal exposure to the drug. The available data on LINZESS use in pregnant women are not sufficient to inform any drug-associated risk for major birth defects and miscarriage.
What are the important warnings for Linaclotide?▼
WARNING: RISK OF SERIOUS DEHYDRATION IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE LINZESS is contraindicated in patients less than 2 years of age; in nonclinical studies in neonatal mice, administration of a single, clinically relevant adult oral dose of linaclotide caused deaths due to dehydration [see Contraindications ( 4 ), Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.4 )]. 5 WARNINGS AND PRECAUTIONS Diarrhea: Patients may experience severe diarrhea. If severe diarrhea occurs, suspend dosing and rehydrate the patient. ( 5.2 ) 5.1 Risk of Serious Dehydration in Pediatric Patients Less Than 2 Years of Age LINZESS is contraindicated in patients less than 2 years of age. In neonatal mice (human age equivalent of approximately 0 to 28 days), linaclotide increased fluid secretion as a consequence of age-dependent elevated GC-C agonism which was associated with increased mortality within the first 24 hours due to dehydration. 4 CONTRAINDICATIONS LINZESS is contraindicated in: Patients less than 2 years of age due to the risk of serious dehydration [see Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.4 )] . Patients with known or suspected mechanical gastrointestinal obstruction. Patients less than 2 years of age.
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.