*** Welcome to piglix ***

Orlistat

Orlistat
Orlistat structure.svg
Orlistat ball-and-stick model.png
Clinical data
Trade names Xenical, Alli
AHFS/Drugs.com Monograph
MedlinePlus a601244
License data
Pregnancy
category
  • AU: B1
  • US: X (Contraindicated)
Routes of
administration
Oral
ATC code A08AB01 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability Negligible
Protein binding >99%
Metabolism In the GI tract
Biological half-life 1 to 2 hours
Excretion Fecal
Identifiers
Synonyms tetrahydrolipstatin
CAS Number 96829-58-2 YesY
PubChem (CID) 3034010
IUPHAR/BPS 5277
DrugBank DB01083 N
ChemSpider 2298564 YesY
UNII 95M8R751W8 N
KEGG D04028 YesY
ChEMBL CHEMBL175247 YesY
ECHA InfoCard 100.167.400
Chemical and physical data
Formula C29H53NO5
Molar mass 495.735 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  

Orlistat is a drug designed to treat obesity. It is marketed as a prescription drug under the trade name Xenical by Roche in most countries, and is sold over-the-counter as Alli by GlaxoSmithKline in the United Kingdom and the United States. Its primary function is preventing the absorption of fats from the human diet by acting as a lipase inhibitor, thereby reducing caloric intake. It is intended for use in conjunction with a healthcare provider-supervised reduced-calorie diet.

Orlistat is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. However, due to its relative simplicity and stability, orlistat was chosen over lipstatin for development as an anti-obesity drug.

The effectiveness of orlistat in promoting weight loss is definite but modest. Pooled data from clinical trials suggest that people given orlistat in addition to lifestyle modifications, such as diet and exercise, lose about 2–3 kilograms (4.4–6.6 lb) more than those not taking the drug over the course of a year. Orlistat also modestly reduces blood pressure and appears to prevent the onset of type 2 diabetes, whether from the weight loss itself or to other effects. In a large randomized controlled trial, orlistat was found to reduce the incidence of diabetes by nearly 40% in obese people.


...
Wikipedia

...