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Mitratapide

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Mitratapide
Clinical data
Trade namesYarvitan
Other namesMitratapid; R103757
Routes of
administration
By mouth
ATCvet code
Legal status
Legal status
Pharmacokinetic data
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 mass717.29 g·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

Mitratapide is aveterinary medication used for the treatment of overweight and obese dogs sold under the brand nameYarvitan. Itsmechanism of action involvesinhibition ofmicrosomal 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 Pharmaceutica and is chemically related to theantifungal drugs such asitraconazole which were also developed by Janssen.

Mitratapide (under the brand name Yarvitan) was authorized for use in the EU by theEuropean Medicines Agency for helping weight loss in dogs, but it has since been withdrawn from the market in the EU.[5]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).www.ema.europa.eu. Retrieved27 August 2016.
  2. ^"Yarvitan (mitratapide). Scientific Discussion"(PDF).www.ema.europa.eu. Retrieved27 August 2016.
  3. ^MitratapideArchived 2012-04-05 at theWayback Machine, vetstream.com
  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.PMC 2776940.PMID 19544001.
  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.PMC 5073926.PMID 27766974.
Stimulants
Amphetamines and
phenethylamines
Adrenergic agonists
Other
Cannabinoid
antagonists
GLP-1,GIP,and / or
glucagon agonists
DACRAs
5-HT2C
receptor agonists
Absorption inhibitors
Uncouplers
Others
GI tract
Cholesterol absorption inhibitors,NPC1L1
Bile acid sequestrants/resins (LDL)
Liver
Statins (HMG-CoA reductase,LDL)
Niacin and derivatives (HDL andLDL)
MTTP inhibitors (VLDL)
ATP citrate lyase inhibitors (LDL)
Thyromimetics (VLDL)
Blood vessels
PPAR agonists (LDL)
Fibrates
Others
CETP inhibitors (HDL)
PCSK9 inhibitors (LDL)
ANGPTL3 inhibitors (LDL/HDL)
Combinations
Other


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