Linaclotide

Product Introduction

Linaclotide, also known as linaclotide acetate, trade name Linzess, is a synthetic peptide structure containing 14 amino acids related to the endogenous guanosine peptide family, and is the only FDA-approved clinically available intestinal locally-activated GC-C (guanylate cyclase-C) agonist analogue of a class of drugs that can be used to treat constipated irritable bowel syndrome (IBS-C) and chronic idiopathic constipation ( CIC) adult patients.

 

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Product Specification 

 

Clinical Studies
In a clinically conducted randomised, double-blind trial, patients with IBS-C were randomised into a treatment group (given linaclotide 290 μg/d) and a placebo group and treated for at least 12 weeks, and the results showed that linaclotide was more effective in terms of abdominal pain and increasing the number of completely spontaneous bowel movements (CSBMs) in the patients compared to the placebo group. The safety and efficacy of linaclotide in patients with chronic idiopathic constipation was confirmed in two further double-blind, multicentre clinical trials, in which patients were randomised to a placebo group, a linaclotide 145 μg/d group or a linaclotide 290 μg/d group.

After 12 weeks of treatment, patients in the 145 μg/d linaclotide group had a significantly higher number of completely spontaneous bowel movements than those in the placebo group. The 290 μg/d treatment group did not show much improvement in clinical outcomes, so the FDA approved only the 145 μg/d dose for the treatment of chronic idiopathic constipation (CIC). The recommended dose of linaclotide is 290 μg/d (for IBS-C) and 145 μg/d (for CIC), taken at least 30 minutes before the first meal of the day. Adverse reactions to linaclotide include diarrhoea, abdominal pain and vomiting. Caution should be exercised in patients 16 years of age and younger.

 

Pharmacological Actions
Linaclotide is a guanylate cyclase C agonist that binds to intestinal GC-C, resulting in elevated intracellular and extracellular cyclic guanosine monophosphate (cGMP) concentrations. Elevated intracellular cGMP can stimulate intestinal fluid secretion and accelerate gastrointestinal transit, thereby increasing the frequency of bowel movements. Elevated extracellular cGMP concentration can reduce the sensitivity of nociceptive nerves and decrease intestinal pain.

 

Pharmacokinetics
Absorption: LINZESS is poorly absorbed and bioavailable after oral administration. Concentrations of linaclotide and its active metabolite in plasma were below the low limit of quantification (LLOQ) after oral administration of doses of 145 μg or 290 μg. Therefore, standard pharmacokinetic parameters such as area under the curve (AUC), maximum concentration (Cmax), and half-life (t½) cannot be calculated.
DISTRIBUTION: Given that blood concentrations of oral doses of linaclotide therapy are not measurable, it is expected that linaclotide distributes to few tissues.
Metabolism: Linaclotide is metabolised in the gastrointestinal tract by loss of the terminal tyrosine portion to its major, active metabolite. Linaclotide and its metabolites are proteolytically degraded to smaller peptides and naturally occurring amino acids in the lumen of the small intestine.
Elimination: After administration of 290 μg of LINZESS per day to fed and fasted subjects for a total of 7 days, active peptides were recovered in faecal samples averaging approximately 5% (fasted) and approximately 3% (fed) and virtually all were active metabolites.

 

Usage and dosage
The drug comes in capsule form and is administered orally once daily. It relieves symptoms of pain and constipation caused by IBS-C, as well as constipation and difficult bowel movements manifested in patients with CIC. The recommended therapeutic dose of the drug is 290 mcg for patients with constipated irritable bowel syndrome; 145 mcg for patients with chronic idiopathic constipation. Take 30 minutes before the first meal of the day.

Precautions
Linzess is contraindicated in paediatric patients 6 years of age and younger.Treatment with this drug need not be contraindicated in paediatric patients 6-17 years of age. Animal studies have shown that adult rat doses of linaclotide treatment can cause death in young rats. To date, no pilot studies have been conducted in paediatric patients. The most commonly reported treatment-related side effect of Linzess is diarrhoea.

 

Product Application 

It can be used to treat adult patients with constipated irritable bowel syndrome (IBS-C) and chronic idiopathic constipation (CIC).

 

Delivery & Packaging

We usual packaging the PS with foil bag powder 1kg/bag, export drum 25kg/drum.

Also accept customization service according your inquire.

As delivery,we can delivery product by courier,by sea, by air, ect.

The more details please check follow picture for reference:

 

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