Chemistry:Capromorelin
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| Trade names | Entyce, Elura |
| Other names | CP-424,391 |
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| Routes of administration | By mouth |
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| Elimination half-life | 2.4 hours[2] |
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| Formula | C28H35N5O4 |
| Molar mass | 505.619 g·mol−1 |
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Capromorelin, sold under the brand names, Entyce and Elura, is a medication used for the management of weight loss in cats and dogs.[3][4] Capromorelin is a ghrelin receptor agonist known to increase appetite and weight gain.[1]
Capromorelin was developed by Pfizer.[5][6]
Capromorelin was approved for veterinary use in the United States in May 2016.[7] It is the second drug approved for the management of weight loss in cats and the first drug approved specifically for the management of weight loss in cats with chronic kidney disease.[1]
Research
Capromorelin functions to stimulate the secretion of growth hormone and as a ghrelin mimetic which causes the body to secrete human growth hormone in a way usually seen at puberty and in young adulthood. Studies have shown the drug to directly raise insulin growth factor 1 (IGF-1) and growth hormone levels.[8]
In a one-year treatment trial (starting 1999) with 395 seniors between 65 and 84 years old, patients who received the drug gained an average of 3 lb (1.4 kg) in lean body mass in the first six months and also were better able to walk in a straight line in a test of balance, strength and coordination. After 12 months, patients receiving capromorelin also had an improved ability to climb stairs, however the results were not good enough to continue the trial for the 2nd planned year.[9]
As of 2017, capromorelin studies in humans had been discontinued.[10]
Veterinary uses
Capromorelin is indicated for the management of weight loss in cats and dogs.[1]
References
- ↑ 1.0 1.1 1.2 1.3 "FDA Approves Elura for Weight Loss in Cats with Chronic Kidney Disease". 19 October 2020. https://www.fda.gov/animal-veterinary/cvm-updates/fda-approves-elura-capromorelin-oral-solution-managing-weight-loss-cats-chronic-kidney-disease.
This article incorporates text from this source, which is in the public domain.
- ↑ "Metabolism, pharmacokinetics, tissue distribution, and excretion of [14C]CP-424391 in rats". Drug Metabolism and Disposition 33 (1): 190–9. January 2005. doi:10.1124/dmd.104.001065. PMID 15486077.
- ↑ "Entyce". https://animaldrugsatfda.fda.gov/adafda/views/#/home/previewsearch/141-457.
- ↑ "Elura". https://animaldrugsatfda.fda.gov/adafda/views/#/home/previewsearch/141-536.
- ↑ "Discovery and biological characterization of capromorelin analogues with extended half-lives". Bioorganic & Medicinal Chemistry Letters 12 (22): 3279–82. November 2002. doi:10.1016/s0960-894x(02)00734-5. PMID 12392732.
- ↑ "Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin". Bioorganic & Medicinal Chemistry 11 (4): 581–90. February 2003. doi:10.1016/s0968-0896(02)00433-9. PMID 12538023.
- ↑ "Aratana Therapeutics Granted FDA Approval of Entyce (capromorelin oral solution)". Aratana Therapeutics. 17 May 2016. https://www.prnewswire.com/news-releases/aratana-therapeutics-granted-fda-approval-of-entyce-capromorelin-oral-solution-300270460.html.
- ↑ "Preclinical pharmacology of CP-424,391, an orally active pyrazolinone-piperidine [correction of pyrazolidinone-piperidine] growth hormone secretagogue". Endocrine 14 (1): 121–32. February 2001. doi:10.1385/ENDO:14:1:121. PMID 11322494.
- ↑ "Effects of an oral growth hormone secretagogue in older adults". The Journal of Clinical Endocrinology and Metabolism 94 (4): 1198–206. April 2009. doi:10.1210/jc.2008-0632. PMID 19174493.
- ↑ "Capromorelin: a ghrelin receptor agonist and novel therapy for stimulation of appetite in dogs". Veterinary Medicine and Science 4 (1): 3–16. February 2018. doi:10.1002/vms3.83. PMID 29468076.
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