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Glyset (MIGLITOL)

Pfizer · FDA-approved approved Small molecule

Glyset works by delaying the breakdown of carbohydrates in the gut, allowing less glucose to enter the bloodstream.

Glyset (Miglitol) is a small molecule alpha-glucosidase inhibitor developed by Pharmacia and Upjohn, now owned by Pfizer. It targets lysosomal alpha-glucosidase to delay carbohydrate absorption, making it a treatment for type 2 diabetes mellitus. Glyset was FDA-approved in 1996 and is now off-patent, with a generic version available. The drug has a half-life of 2.3 hours and 60% bioavailability. Key safety considerations include gastrointestinal side effects.

At a glance

Generic nameMIGLITOL
SponsorPfizer
Drug classalpha-Glucosidase Inhibitor
TargetLysosomal alpha-glucosidase
ModalitySmall molecule
Therapeutic areaMetabolic
PhaseFDA-approved
First approval1996

Mechanism of action

Mechanism of Action. In contrast to sulfonylureas, miglitol tablets do not enhance insulin secretion. The antihyperglycemic action of miglitol results from reversible inhibition of membrane-bound intestinal -glucoside hydrolase enzymes. Membrane-bound intestinal -glucosidases hydrolyze oligosaccharides and disaccharides to glucose and other monosaccharides in the brush border of the small intestine. In diabetic patients, this enzyme inhibition results in delayed glucose absorption and lowering of postprandial hyperglycemia.Because its mechanism of action is different, the effect of miglitol tablets to enhance glycemic control is additive to that of sulfonylureas when used in combination. In addition, miglitol tablets diminish the insulinotropic and weight-increasing effects of sulfonylureas.Miglitol has minor inhibitory activity against lactase and consequently, at the recommended doses, would not be expected to induce lactose intolerance.

Approved indications

Common side effects

Drug interactions

Key clinical trials

Primary sources

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

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