Dirlotapide

Dirlotapide
Systematic (IUPAC) name


1-Methyl-N-[(1S)-2-(methyl-(phenylmethyl)amino)-2-oxo-1-phenylethyl]-5-[[oxo-[2-[4-(trifluoromethyl)phenyl]phenyl]methyl]amino]-2-indolecarboxamide
Clinical data
Trade names	Slentrol
AHFS/Drugs.com	International Drug Names
Routes of administration	Oral
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Protein binding	High^[1]
Metabolism	Hepatic
Biological half-life	5–18 hours (increased with repeated dosing)
Excretion	Feces, urine
Identifiers
CAS Number	481658-94-0^Y
ATCvet code	QA08AB91(WHO)
PubChem	CID 9917862
ChemSpider	8093509^Y
UNII	578H0RMP25^Y
KEGG	D03867^Y
ChEMBL	CHEMBL410414^Y
Chemical data
Formula	C₄₀H₃₃F₃N₄O₃
Molar mass	674.71 g/mol
SMILES 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 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^Y Key:TUOSYWCFRFNJBS-BHVANESWSA-N^Y
(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.

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. It also elicits a satiety signal from lipid-filled cells lining the intestine.

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]

References

1 2 "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. Retrieved 28 November 2015.
↑ http://www.freepatentsonline.com/y2016/0002264.html
↑ http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2769592/
↑ Bridges, Andrew. "FDA approves 1st drug for obese dogs". Associated Press. Archived from the original on January 8, 2007. Retrieved January 6, 2007 – via Yahoo! News.
↑ http://www.cbsnews.com/news/why-pfizer-doesnt-want-the-fda-studying-its-diet-drug-for-dogs/
↑ http://blogs.wsj.com/health/2010/10/14/fda-sniffing-around-pfizers-doggy-weight-loss-drug-slentrol/

Antiobesity agents/Anorectics (A08)

Central

Stimulants	4-Methylamphetamine^‡ Amfecloral Amfepentorex Amfepramone Aminorex^‡ Amphetamine Amphetaminil Atomoxetine Benfluorex^‡ Benzphetamine Bupropion (+naltrexone; +zonisamide^†) Cathine Cathinone Chlorphentermine Ciclazindol Clobenzorex Cloforex Clominorex Clortermine Dexfenfluramine^‡ Dextroamphetamine Dexmethylphenidate Difemetorex^‡ Dimethylcathinone Diphemethoxidine Ephedrine Ephedra^‡ Etilamfetamine Etolorex Fenbutrazate Fencamfamine Fenethylline Fenfluramine^‡ (+phentermine^‡) Fenproporex Fludorex Fluminorex Furfenorex^‡ Indanorex Khat Levopropylhexedrine Lisdexamfetamine Manifaxine Mazindol Mefenorex Methamphetamine Methylphenidate Norfenfluramine Pemoline Pentorex Phendimetrazine Phenethylamine Phenmetrazine Phentermine (+topiramate) Phenylpropanolamine Picilorex Pipradrol Prolintane Propylhexedrine Pseudoephedrine Pyrovalerone Radafaxine Reboxetine Setazindol Sibutramine^‡ Synephrine Tesofensine Viloxazine Xylopropamine Zylofuramine

Cannabinoid receptor antagonists	Drinabant^§ Ibipinabant^§ Otenabant^§ Rimonabant^‡ Rosonabant^§ Surinabant^§ Taranabant^§

Others	5-HTP Galactomannan Guar gum Glucomannan L-DOPA L-Phenylalanine L-Tryptophan L-Tyrosine Lorcaserin Lu AA-33810 Metformin Naltrexone Naloxone Oxyntomodulin P57 Peptide YY Topiramate Yohimbine (Yohimbe) Zonisamide water

Peripheral

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

Lipid modifying agents (C10)

GI tract

Cholesterol absorption inhibitors, NPC1L1	Ezetimibe SCH-48461

Bile acid sequestrants/resins (LDL)	Cholestyramine Colestipol Colestilan Colextran Colesevelam

Liver

Statins (HMG-CoA reductase, LDL)	Simvastatin^# Atorvastatin Fluvastatin Lovastatin Mevastatin Pitavastatin Pravastatin Rosuvastatin Cerivastatin^‡

Niacin and derivatives (HDL and LDL)	Niceritrol Niacin Nicofuranose Aluminium nicotinate Nicotinyl alcohol Acipimox

MTTP inhibitors (VLDL)	Dirlotapide Lomitapide Mitratapide

Blood vessels

Fibrates (PPAR)	Clofibrate^‡ Bezafibrate Aluminium clofibrate Gemfibrozil Fenofibrate Simfibrate Ronifibrate Ciprofibrate Etofibrate Clofibride Clinofibrate

CETP inhibitors (HDL)	Anacetrapib^† Dalcetrapib^§ Evacetrapib^§ Torcetrapib^§

Combinations

Other

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

This article is issued from Wikipedia - version of the Friday, March 18, 2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.