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Mitratapide

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Mitratapide
Clinical data
Trade namesYarvitan
Other namesMitratapid; R103757
Routes of
administration
By mouth
ATCvet code
Legal status
Legal status
Pharmacokineticdata
Bioavailability55–69%
Protein binding>99.9%[1]
MetabolismExtensiveliver(sulfoxidation);first pass effect
Eliminationhalf-life6.3 hours (mitratapide), up to 44.7 hours (metabolites)
ExcretionFeces (80–90%)[2]
Identifiers
  • 2-[(2R)-Butan-2-yl]-4-[4-[4-[4-[[(2S,4R)-2-(4-chlorophenyl)-2-[(4-methyl-1,2,4-triazol-3-yl)sulfanylmethyl]-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC36H41ClN8O4S
Molar mass717.29g·mol−1
3D model (JSmol)
  • CC[C@@H](C)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OC[C@@H]5CO[C@@](O5)(CSC6=NN=CN6C)C7=CC=C(C=C7)Cl
  • InChI=1S/C36H41ClN8O4S/c1-4-26(2)45-35(46)44(25-39-45)31-11-9-29(10-12-31)42-17-19-43(20-18-42)30-13-15-32(16-14-30)47-21-33-22-48-36(49-33,27-5-7-28(37)8-6-27)23-50-34-40-38-24-41(34)3/h5-16,24-26,33H,4,17-23H2,1-3H3/t26-,33-,36-/m1/s1
  • Key:HQSRVYUCBOCBLY-XOOFNSLWSA-N

Mitratapideis aveterinary medicationused for the treatment of overweight and obese dogs sold under the brand nameYarvitan.Itsmechanism of actioninvolvesinhibitionofmicrosomal triglyceride transfer protein(MTP) which is responsible for the absorption of dietarylipids.[3]Clinical study also suggests that mitratapide may help to reverse insulin resistance in dogs.[4]

The drug was developed byJanssen Pharmaceuticaand is chemically related to theantifungaldrugs such asitraconazolewhich were also developed by Janssen.

Mitratapide (under the brand name Yarvitan) was authorized for use in the EU by theEuropean Medicines Agencyfor helping weight loss in dogs, but it has since been withdrawn from the market in the EU.[5]

References

[edit]
  1. ^"Yarvitan 5 mg/ml Oral Solution for Dogs. Summary of Product Characteristics"(PDF).ema.europa.eu.Retrieved27 August2016.
  2. ^"Yarvitan (mitratapide). Scientific Discussion"(PDF).ema.europa.eu.Retrieved27 August2016.
  3. ^MitratapideArchived2012-04-05 at theWayback Machine,vetstream
  4. ^Dobenecker B, De Bock M, Engelen M, Goossens L, Scholz A, Kienzle E (December 2009)."Effect of mitratapide on body composition, body measurements and glucose tolerance in obese Beagles".Veterinary Research Communications.33(8): 839–47.doi:10.1007/s11259-009-9232-5.PMC2776940.PMID19544001.
  5. ^German AJ (October 2016)."Weight management in obese pets: the tailoring concept and how it can improve results".Acta Veterinaria Scandinavica.58(Suppl 1): 57.doi:10.1186/s13028-016-0238-z.PMC5073926.PMID27766974.