Cetilistat

Cetilistat

Systematic (IUPAC) name
2-(Hexadecyloxy)-6-methyl-4H-3,1-benzoxazin-4-one
Clinical data
Identifiers
CAS Registry Number	282526-98-1 Y
ATC code	None
PubChem	CID 9952916
ChemSpider	8128526 N
UNII	LC5G1JUA39 Y
KEGG	D09208 Y
ChEMBL	CHEMBL2103825 N
Chemical data
Formula	C25H39NO3
Molecular mass	401.582 g/mol
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  N Key:MVCQKIKWYUURMU-UHFFFAOYSA-N  N
N (what is this?)  (verify)

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/
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.