Dirlotapide

Source: Wikipedia, the free encyclopedia.
Dirlotapide
By mouth
ATCvet code
Legal status
Legal status
Pharmacokinetic data
Protein bindingHigh[1]
MetabolismLiver
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
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.[citation needed]

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.[medical citation needed] It also elicits a satiety signal from lipid-filled cells lining the intestine.[medical citation needed]

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]

Dirlotapide (under the brand name Slentrol) was authorized for use in the EU by the European Medicines Agency for helping weight loss in dogs, but has since been withdrawn from the market in the EU.[7]

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. Archived from the original (PDF) on 8 December 2015. Retrieved 28 November 2015.
  2. ^ US 20160002264, "Carbocyclic- and Heterocyclic-Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds", assigned to Pfizer, Inc. 
  3. PMID 19885086
    .
  4. ^ Bridges A. "FDA approves 1st drug for obese dogs". Associated Press. Archived from the original on 2007-01-08. Retrieved January 6, 2007 – via Yahoo! News.
  5. ^ Edwards J (15 October 2010). "Why Pfizer Doesn't Want the FDA Studying Its Diet Drug for Dogs". CBS News. Retrieved 2018-07-05.
  6. ^ Hobson K (14 October 2010). "FDA Sniffing Around Pfizer's Doggy Weight-Loss Drug Slentrol". WSJ. Retrieved 2018-07-05.
  7. PMID 27766974
    .
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