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Dirlotapide

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Dirlotapide
Clinical data
Trade namesSlentrol
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral
ATCvet code
Legal status
Legal status
Pharmacokinetic data
Protein bindingHigh[1]
MetabolismHepatic
Elimination half-life5–18 hours (increased with repeated dosing)
ExcretionFeces, urine
Identifiers
  • 1-Methyl-N-[(1S)-2-(methyl-(phenylmethyl)amino)-2-oxo-1-phenylethyl]-5-[​[oxo-[2-[4-(trifluoromethyl)phenyl]phenyl]methyl]amino]-2-indolecarboxamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC40H33F3N4O3
Molar mass674.71 g/mol g·mol−1
3D model (JSmol)
  • FC(F)(F)c1ccc(cc1)c2ccccc2C(=O)Nc3cc4c(cc3)n(c(c4)C(=O)N[C@@H](c5ccccc5)C(=O)N(Cc6ccccc6)C)C
  • InChI=1S/C40H33F3N4O3/c1-46(25-26-11-5-3-6-12-26)39(50)36(28-13-7-4-8-14-28)45-38(49)35-24-29-23-31(21-22-34(29)47(35)2)44-37(48)33-16-10-9-15-32(33)27-17-19-30(20-18-27)40(41,42)43/h3-24,36H,25H2,1-2H3,(H,44,48)(H,45,49)/t36-/m0/s1 checkY
  • Key:TUOSYWCFRFNJBS-BHVANESWSA-N checkY
  (verify)

Dirlotapide is a drug used to treat obesity in dogs.[1] It is manufactured by Pfizer and Zoetis and marketed under the brand name Slentrol.

It works as a gut-selective microsomal triglyceride transfer protein (MTTP or MTP) inhibitor.[2] This blocks the assembly and release of lipoproteins into the bloodstream, thereby reducing fat absorption. It also elicits a satiety signal from lipid-filled cells lining the intestine.

Usage

It is supplied as an oral solution. It is not intended for use in humans, cats, birds, rodents, or other animals.

Dirlotapide is used to manage obesity in dogs and helps by reducing appetite. It is used as part of an overall weight control program that also includes proper diet and exercise, under the supervision of a veterinarian. Side effects may include vomiting, diarrhea, lethargy, drooling, or uncoordination. Allergic reaction to the medication may include, facial swelling, hives, scratching, sudden onset of diarrhea, vomiting, shock, seizures, pale gums, cold limbs, or coma.

Regulation and safety

On January 5, 2007, the U.S. Food and Drug Administration (FDA) approved Slentrol, the first time the FDA has approved a drug for obese dogs.[3][4]

However, concerns have since been raised, since 2010, about adverse effects[5] that might more strongly affect particular breeds.[6]

References

  1. ^ a b "Slentrol (dirlotapide) Oral Solution (5 mg/ml, 1%) for Use in Dogs Only. Full Prescribing Information" (PDF). zoetisUS.com. Pfizer Animal Health. Div. of Pfizer Inc. NY, NY 10017. Retrieved 28 November 2015.
  2. ^ http://www.freepatentsonline.com/y2016/0002264.html
  3. ^ http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2769592/
  4. ^ Bridges, Andrew. "FDA approves 1st drug for obese dogs". Associated Press. Archived from the original on January 8, 2007. Retrieved January 6, 2007 – via Yahoo! News.
  5. ^ http://www.cbsnews.com/news/why-pfizer-doesnt-want-the-fda-studying-its-diet-drug-for-dogs/
  6. ^ http://blogs.wsj.com/health/2010/10/14/fda-sniffing-around-pfizers-doggy-weight-loss-drug-slentrol/