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词条 Mitratapide
释义

  1. See also

  2. References

{{Drugbox
| IUPAC_name = 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
| image = Mitratapide.svg
| width = 315
| alt =
| caption =
| tradename = Yarvitan
| Drugs.com =
| MedlinePlus =
| pregnancy_AU =
| pregnancy_US =
| pregnancy_category =
| legal_AU =
| legal_CA =
| legal_UK =
| legal_US =
| legal_status =
| routes_of_administration = By mouth (0.5% solution)
| bioavailability = 55–69%
| protein_bound = >99.9%[1]
| metabolism = Extensive liver (sulfoxidation); first pass effect
| elimination_half-life = 6.3 hours (mitratapide), up to 44.7 hours (metabolites)
| excretion = Feces (80–90%)[2]
| synonyms = Mitratapid; R103757
| CAS_number = 179602-65-4
| ATCvet = yes
| ATC_prefix = A08
| ATC_suffix = AB90
| UNII = FVW7T75XP4
| PubChem = 213047
| DrugBank =
| ChemSpiderID = 184740
| KEGG = D05060
| C=36 | H=41 | Cl=1 | N=8 | O=4 | S=1
| molecular_weight = 717.28 g/mol
| smiles = 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
| StdInChI = 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
| StdInChIKey = HQSRVYUCBOCBLY-XOOFNSLWSA-N
}}Mitratapide is a veterinary drug for the treatment of overweight and obese dogs sold under the brand name Yarvitan. Its mechanism of action involves inhibition of microsomal triglyceride transfer protein (MTP) which is responsible for the absorption of dietary lipids.[3] Clinical study also suggests that mitratapide may help to reverse insulin resistance in dogs.[4]

The drug was developed by Janssen Pharmaceutica and is chemically related to the antifungal drugs such as itraconazole which were also developed by Janssen.

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authorized for use in the EU by the European Medicines Agency for helping weight loss in dogs, but it has since been withdrawn from the market in the EU.[5]

See also

  • Dirlotapide

References

1. ^{{cite web|title=Yarvitan 5 mg/ml Oral Solution for Dogs. Summary of Product Characteristics|url=http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/veterinary/000113/WC500069449.pdf|website=www.ema.europa.eu|accessdate=27 August 2016}}
2. ^{{cite web|title=Yarvitan (mitratapide). Scientific Discussion|url=http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Scientific_Discussion/veterinary/000113/WC500069446.pdf|website=www.ema.europa.eu|accessdate=27 August 2016}}
3. ^Mitratapide {{webarchive|url=https://web.archive.org/web/20120405061345/http://www.vetstream.com/canis/Content/Generic/gen00870.asp |date=2012-04-05 }}, vetstream.com
4. ^{{cite journal | pmid = 19544001 | year = 2009 | last1 = Dobenecker | first1 = B | last2 = De Bock | first2 = M | last3 = Engelen | first3 = M | last4 = Goossens | first4 = L | last5 = Scholz | first5 = A | last6 = Kienzle | first6 = E | title = Effect of mitratapide on body composition, body measurements and glucose tolerance in obese Beagles | volume = 33 | issue = 8 | pages = 839–47 | doi = 10.1007/s11259-009-9232-5 | pmc = 2776940 | journal = Veterinary Research Communications}}
5. ^{{cite journal|last1=German|first1=AJ|title=Weight management in obese pets: the tailoring concept and how it can improve results|journal=Acta veterinaria Scandinavica|date=20 October 2016|volume=58|issue=Suppl 1|pages=57|doi=10.1186/s13028-016-0238-z|pmid=27766974|pmc=5073926}}
{{Antiobesity preparations}}{{Lipid modifying agents}}{{gastrointestinal-drug-stub}}{{veterinary-med-stub}}

6 : Veterinary drugs|Antiobesity drugs|Piperazines|Triazoles|Phenol ethers|Ketals

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