Cetilistat

Cetilistat

Clinical data
ATC code	none
Identifiers
IUPAC name 2-(Hexadecyloxy)-6-methyl-4H-3,1-benzoxazin-4-one
CAS Number	282526-98-1
PubChem (CID)	9952916
ChemSpider	8128526
UNII	LC5G1JUA39
KEGG	D09208
ChEMBL	CHEMBL2103825
Chemical and physical data
Formula	C25H39NO3
Molar mass	401.582 g/mol
3D model (Jmol)	Interactive image
SMILES CCCCCCCCCCCCCCCCOc2oc(=O)c1cc(C)ccc1n2
InChI InChI=1S/C25H39NO3/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-19-28-25-26-23-18-17-21(2)20-22(23)24(27)29-25/h17-18,20H,3-16,19H2,1-2H3 Key:MVCQKIKWYUURMU-UHFFFAOYSA-N
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Cetilistat is a drug designed to treat obesity. It acts in the same way as the older drug orlistat (Xenical) by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested.^[1]

In human trials, cetilistat was shown to produce similar weight loss to orlistat, but also produced similar side effects such as oily, loose stools, fecal incontinence, frequent bowel movements, and flatulence.^[2][3] It is likely that the same precautions would apply in that absorption of fat-soluble vitamins and other fat-soluble nutrients may be inhibited, requiring vitamin supplements to be used to avoid deficiencies.

Cetilistat has completed Phase 1 and 2 trials in the West and is currently in Phase 3 trials in Japan where it is partnered with Takeda.^[4] Norgina BV has now acquired the full global rights to cetilistat from Alizyme after the latter went into administration.^[5]

A published phase 2 trial found cetilistat significantly reduced weight with and was better tolerated than orlistat.^[6]

See also

• Anti-obesity medication

References

1. Yamada Y, Kato T, Ogino H, Ashina S, Kato K (2008). "Cetilistat (ATL-962), a novel pancreatic lipase inhibitor, ameliorates body weight gain and improves lipid profiles in rats". Hormone and Metabolic Research. 40 (8): 539–43. doi:10.1055/s-2008-1076699. PMID 18500680.
2. Kopelman, P; Bryson, A; Hickling, R; Rissanen, A; Rossner, S; Toubro, S; Valensi, P (2007). "Cetilistat (ATL-962), a novel lipase inhibitor: A 12-week randomized, placebo-controlled study of weight reduction in obese patients". International journal of obesity (2005). 31 (3): 494–9. doi:10.1038/sj.ijo.0803446. PMID 16953261.
3. Padwal, R (2008). "Cetilistat, a new lipase inhibitor for the treatment of obesity". Current opinion in investigational drugs (London, England : 2000). 9 (4): 414–21. PMID 18393108.
4. http://www.alizyme.com/alizyme/products/cetilistat/ Archived January 7, 2009, at the Wayback Machine.
5. Norgine acquires cetilistat
6. "Weight loss, HbA1c reduction, and tolerability of cetilistat in a randomized, placebo-controlled phase 2 trial in obese diabetics: comparison with orlistat (Xenical).". Obesity. 18: 108–15. Jan 2010. doi:10.1038/oby.2009.155. PMID 19461584.