Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C40H33F3N4O3 |
Molecular Weight | 674.7117 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(Cc1ccccc1)C(=O)[C@]([H])(c2ccccc2)N=C(c3cc4cc(ccc4n3C)NC(=O)c5ccccc5-c6ccc(cc6)C(F)(F)F)O
InChI
InChIKey=TUOSYWCFRFNJBS-BHVANESWSA-N
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
DescriptionCurator's Comment:: description was created based on several sources, including:
https://www.vetdepot.com/product-labels/slentrol.pdf | https://www.ncbi.nlm.nih.gov/pubmed/17276061 | https://www.ncbi.nlm.nih.gov/pubmed/17567511
Curator's Comment:: description was created based on several sources, including:
https://www.vetdepot.com/product-labels/slentrol.pdf | https://www.ncbi.nlm.nih.gov/pubmed/17276061 | https://www.ncbi.nlm.nih.gov/pubmed/17567511
Dirlotapide is indicated for the management of obesity in dogs. Dirlotapide is a microsomal triglyceride transfer protein (MTP) inhibitor. It mainly acts locally in the gut to reduce appetite, increase fecal fat and produce weight loss in dogs. The adverse reactions associated with treatment with Dirlotapide include vomiting, loose stools/diarrhea, lethargy, and anorexia.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17567511
Curator's Comment:: <0.01%
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17276061
Curator's Comment:: https://www.google.com/patents/WO2003002533A1 # Pfizer Inc.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2364681 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17276061 |
1.5 nM [IC50] | ||
Target ID: CHEMBL3356 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17276061 |
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Target ID: CHEMBL3397 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17276061 |
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Target ID: CHEMBL3622 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17276061 |
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Target ID: CHEMBL289 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17276061 |
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Target ID: CHEMBL2364675 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17276061 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | SLENTROL Approved UseSLENTROL (dirlotapide) Oral Solution is indicated for the management of obesity in dogs. Launch Date1.16786882E12 |
PubMed
Title | Date | PubMed |
---|---|---|
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity. | 2007 Apr 1 |
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Efficacy and safety of dirlotapide in the management of obese dogs evaluated in two placebo-controlled, masked clinical studies in North America. | 2007 Aug |
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Influence of dirlotapide, a microsomal triglyceride transfer protein inhibitor, on the digestibility of a dry expanded diet in adult dogs. | 2007 Aug |
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Canine obesity: an overview. | 2007 Aug |
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The use of 18O-exchange and base-catalyzed N-dealkylation with liquid chromatography/tandem mass spectrometry to identify carbinolamide metabolites. | 2010 Jul 30 |
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Low-energy nanoemulsification to design veterinary controlled drug delivery devices. | 2010 Oct 21 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.vetdepot.com/product-labels/slentrol.pdf
The initial dosage of SLENTROL is 0.01 mL/kg (0.0045 mL/lb) body weight, administered once daily, for the first 14 days. After the first 14 days of treatment, the dose volume of SLENTROL should be doubled to 0.02 mL/kg (0.009 mL/lb) of body weight, administered once daily for the next 14 days (days 15 to 28 of treatment). Dogs should be weighed monthly and the dose volume adjusted every month, as necessary, to maintain a target percent weight loss of ≥0.7% per week.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17276061
In a murine model investigating intestinal triglyceride transfer protein (MTP) inhibition, dirlotapide demonstrated potent inhibition of intestinal fat absorption with an ED25 of 0.16 mg/kg. In contrast, it was a poor inhibitor of hepatic MTP as demonstrated in a murine model of triglyceride lowering, where it had an ED25 of 6 mg/kg.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29728
Created by
admin on Sat Jun 26 02:52:08 UTC 2021 , Edited by admin on Sat Jun 26 02:52:08 UTC 2021
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WHO-VATC |
QA08AB91
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CFR |
21 CFR 520.666
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EMA VETERINARY ASSESSMENT REPORTS |
SLENTROL [WITHDRAWN]
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Code System | Code | Type | Description | ||
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C77329
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C521290
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578H0RMP25
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DIRLOTAPIDE
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9917862
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M4665
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DB11399
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481658-94-0
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CHEMBL410414
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8468
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1592684
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PRIMARY | RxNorm |
ACTIVE MOIETY