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Amitiza (LUBIPROSTONE)

Sucampo Pharma Llc · FDA-approved approved Small molecule Quality 65/100

Amitiza works by activating chloride channels in the intestines, increasing fluid secretion and promoting bowel movements.

Amitiza (Lubiprostone) is a small molecule chloride channel activator developed by Sucampo Pharma LLC, targeting the chloride channel protein 2. It was FDA-approved in 2006 for the treatment of chronic idiopathic constipation and irritable bowel syndrome characterized by constipation. Amitiza is commercially available, with multiple generic manufacturers. Key safety considerations include its potential to cause gastrointestinal side effects. The commercial status of Amitiza is not off-patent.

At a glance

Generic nameLUBIPROSTONE
SponsorSucampo Pharma Llc
Drug classChloride Channel Activator [EPC]
TargetChloride channel protein 2
ModalitySmall molecule
Therapeutic areaMetabolic
PhaseFDA-approved
First approval2006

Mechanism of action

Lubiprostone is locally acting chloride channel activator that enhances chloride-rich intestinal fluid secretion without altering sodium and potassium concentrations in the serum. Lubiprostone acts by specifically activating ClC-2, which is normal constituent of the apical membrane of the human intestine, in protein kinase A-independent fashion.Patch clamp cell studies in human cell lines have indicated that the majority of the beneficial biological activity of lubiprostone and its metabolites is observed only on the apical (luminal) portion of the gastrointestinal epithelium. Lubiprostone, via activation of apical ClC-2 channels in intestinal epithelial cells, bypasses the antisecretory action of opiates that results from suppression of secretomotor neuron excitability. Activation of ClC-2 by lubiprostone has also been shown to stimulate recovery of mucosal barrier function and reduce intestinal permeability via the restoration of tight junction protein compl

Approved indications

Common side effects

Key clinical trials

Patents

PatentExpiryType

Primary sources

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SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results
FDA Orange BookPatents + exclusivity

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