Capromorelin Explained

Capromorelin, sold under the brand names, Entyce and Elura, is a medication used for the management of weight loss in cats and dogs.^{[1] [2]} Capromorelin is a ghrelin receptor agonist known to increase appetite and weight gain.

Capromorelin was developed by Pfizer.^{[3] [4]}

Capromorelin was approved for veterinary use in the United States in May 2016.^[5] 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.

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.^[6]

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.^[7]

As of 2017, capromorelin studies in humans had been discontinued.^[8]

Veterinary uses

Capromorelin is indicated for the management of weight loss in cats and dogs.

Notes and References

1. Web site: Entyce . U.S. Food and Drug Administration (FDA) . 12 December 2022.
2. Web site: Elura . U.S. Food and Drug Administration (FDA) . 12 December 2022.
3. Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Murray MC, Cook ER, DiBrino JN, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Lewis SK, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, Pettersen JC, DaSilva-Jardine PA, Wilson TC, Thompson DD . 6 . Discovery and biological characterization of capromorelin analogues with extended half-lives . Bioorganic & Medicinal Chemistry Letters . 12 . 22 . 3279–82 . November 2002 . 12392732 . 10.1016/s0960-894x(02)00734-5 .
4. Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Cook ER, DiBrino JN, Campeta AM, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, DaSilva-Jardine PA, Wilson TC, Thompson DD . 6 . Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin . Bioorganic & Medicinal Chemistry . 11 . 4 . 581–90 . February 2003 . 12538023 . 10.1016/s0968-0896(02)00433-9 .
5. Web site: Aratana Therapeutics Granted FDA Approval of Entyce (capromorelin oral solution) . Aratana Therapeutics . PR Newswire . 17 May 2016 . 12 December 2022.
6. Pan LC, Carpino PA, Lefker BA, Ragan JA, Toler SM, Pettersen JC, Nettleton DO, Ng O, Pirie CM, Chidsey-Frink K, Lu B, Nickerson DF, Tess DA, Mullins MA, MacLean DB, DaSilva-Jardine PA, Thompson DD . 6 . 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 . 11322494 . 10.1385/ENDO:14:1:121 . 46978604 .
7. White HK, Petrie CD, Landschulz W, MacLean D, Taylor A, Lyles K, Wei JY, Hoffman AR, Salvatori R, Ettinger MP, Morey MC, Blackman MR, Merriam GR . 6 . Effects of an oral growth hormone secretagogue in older adults . The Journal of Clinical Endocrinology and Metabolism . 94 . 4 . 1198–206 . April 2009 . 19174493 . 10.1210/jc.2008-0632 . free .
8. Rhodes L, Zollers B, Wofford JA, Heinen E . Capromorelin: a ghrelin receptor agonist and novel therapy for stimulation of appetite in dogs . Veterinary Medicine and Science . 4 . 1 . 3–16 . February 2018 . 29468076 . 5813110 . 10.1002/vms3.83 .