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 ;
CompTox Dashboard (EPA)	DTXSID90182506 ;
Chemical and physical data
Formula	C25H39NO3
Molar mass	401.591 g·mol−1
3D model (JSmol)	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 and was better tolerated than orlistat.[6]

References

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.
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. 31 (3): 494–9. doi:10.1038/sj.ijo.0803446. PMID 16953261.
Padwal, R (2008). "Cetilistat, a new lipase inhibitor for the treatment of obesity". Current Opinion in Investigational Drugs. 9 (4): 414–21. PMID 18393108.
http://www.alizyme.com/alizyme/products/cetilistat/ Archived January 7, 2009, at the Wayback Machine
"Norgine acquires cetilistat" (PDF). Archived from the original (PDF) on 2011-01-24. Retrieved 2010-02-10.
Kopelman, P.; Groot Gde, H.; Rissanen, A.; Rossner, S.; Toubro, S.; Palmer, R.; Hallam, R.; Bryson, A.; Hickling, R. I. (Jan 2010). "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 (1): 108–15. doi:10.1038/oby.2009.155. PMID 19461584.

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[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. 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. 9 (4): 414–21. PMID 18393108.

[4] ttp://www.alizyme.com/alizyme/products/cetilistat/ Archived January 7, 2009, at the Wayback Machine

[5] "Norgine acquires cetilistat" (PDF). Archived from the original (PDF) on 2011-01-24. Retrieved 2010-02-10.

[6] Kopelman, P.; Groot Gde, H.; Rissanen, A.; Rossner, S.; Toubro, S.; Palmer, R.; Hallam, R.; Bryson, A.; Hickling, R. I. (Jan 2010). "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 (1): 108–15. doi:10.1038/oby.2009.155. PMID 19461584.

Cetilistat

See also

References