Capromorelin

Capromorelin
Clinical data
Trade names	Entyce, Elura, Eluracat
Other names	CP-424,391
License data	US DailyMed: Capromorelin;
Routes of; administration	By mouth
ATCvet code	QH01AX90 (WHO) ;
Legal status
Legal status	CA: ℞-only; US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Elimination half-life	2.4 hours
Identifiers
	IUPAC name N-[(2R)-1-[(3aR)-2-methyl-3-oxo-3a-(phenylmethyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-1-oxo-3-(phenylmethoxy)propan-2-yl]-2-amino-2-methylpropanamide;
CAS Number	193273-66-4 ;
PubChem CID	216208;
DrugBank	DB15205 ;
ChemSpider	187411 ;
UNII	0MQ44VUN84;
KEGG	D03373;
ChEMBL	ChEMBL113313 ;
CompTox Dashboard (EPA)	DTXSID5057886 ;
Chemical and physical data
Formula	C28H35N5O4
Molar mass	505.619 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)(C(=O)N[C@H](COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)[C@@]3(C2)CC4=CC=CC=C4)C)N;
	InChI InChI=1S/C28H35N5O4/c1-27(2,29)25(35)30-22(18-37-17-21-12-8-5-9-13-21)24(34)33-15-14-23-28(19-33,26(36)32(3)31-23)16-20-10-6-4-7-11-20/h4-13,22H,14-19,29H2,1-3H3,(H,30,35)/t22-,28-/m1/s1 ; Key:KVLLHLWBPNCVNR-SKCUWOTOSA-N ;
	(what is this?) (verify)

Capromorelin, sold under the brand names, Entyce and Elura, is a medication used for the management of weight loss in cats and dogs.^[5]^[6] Capromorelin is a ghrelin receptor agonist known to increase appetite and weight gain.^[2]

Capromorelin was developed by Pfizer.^[7]^[8]

Capromorelin was approved for veterinary use in the United States in May 2016.^[9] 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.^[2]

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.^[10]

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.^[11]

As of 2017, capromorelin studies in humans had been discontinued.^[12]

Veterinary uses

Capromorelin is indicated for the management of weight loss in cats and dogs.^[2]

References

^ "Notice: Multiple additions to the Prescription Drug List (PDL) [2024-08-13]". Health Canada. 13 August 2024. Retrieved 15 August 2024.
^ ^a ^b ^c ^d "FDA Approves Elura for Weight Loss in Cats with Chronic Kidney Disease". U.S. Food and Drug Administration. 19 October 2020. Retrieved 12 December 2022. This article incorporates text from this source, which is in the public domain.
^ "Eluracat EPAR". European Medicines Agency. 22 May 2023. Retrieved 24 May 2024.
^ Khojasteh-Bakht SC, O'donnell JP, Fouda HG, Potchoiba MJ (January 2005). "Metabolism, pharmacokinetics, tissue distribution, and excretion of [14C]CP-424391 in rats". Drug Metabolism and Disposition. 33 (1): 190–9. doi:10.1124/dmd.104.001065. PMID 15486077. S2CID 20760627.
^ "Entyce". U.S. Food and Drug Administration (FDA). Retrieved 12 December 2022.
^ "Elura". U.S. Food and Drug Administration (FDA). Retrieved 12 December 2022.
^ Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Murray MC, et al. (November 2002). "Discovery and biological characterization of capromorelin analogues with extended half-lives". Bioorganic & Medicinal Chemistry Letters. 12 (22): 3279–82. doi:10.1016/s0960-894x(02)00734-5. PMID 12392732.
^ Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Cook ER, et al. (February 2003). "Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin". Bioorganic & Medicinal Chemistry. 11 (4): 581–90. 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. Retrieved 12 December 2022 – via PR Newswire.
^ Pan LC, Carpino PA, Lefker BA, Ragan JA, Toler SM, Pettersen JC, et al. (February 2001). "Preclinical pharmacology of CP-424,391, an orally active pyrazolinone-piperidine [correction of pyrazolidinone-piperidine] growth hormone secretagogue". Endocrine. 14 (1): 121–32. doi:10.1385/ENDO:14:1:121. PMID 11322494. S2CID 46978604.
^ White HK, Petrie CD, Landschulz W, MacLean D, Taylor A, Lyles K, et al. (April 2009). "Effects of an oral growth hormone secretagogue in older adults". The Journal of Clinical Endocrinology and Metabolism. 94 (4): 1198–206. doi:10.1210/jc.2008-0632. PMID 19174493.
^ Rhodes L, Zollers B, Wofford JA, Heinen E (February 2018). "Capromorelin: a ghrelin receptor agonist and novel therapy for stimulation of appetite in dogs". Veterinary Medicine and Science. 4 (1): 3–16. doi:10.1002/vms3.83. PMC 5813110. PMID 29468076.

[1] "Notice: Multiple additions to the Prescription Drug List (PDL) [2024-08-13]". Health Canada. 13 August 2024. Retrieved 15 August 2024.

[FDA_capromorelin-2] "FDA Approves Elura for Weight Loss in Cats with Chronic Kidney Disease". U.S. Food and Drug Administration. 19 October 2020. Retrieved 12 December 2022. This article incorporates text from this source, which is in the public domain.

[3] "Eluracat EPAR". European Medicines Agency. 22 May 2023. Retrieved 24 May 2024.

[4] Khojasteh-Bakht SC, O'donnell JP, Fouda HG, Potchoiba MJ (January 2005). "Metabolism, pharmacokinetics, tissue distribution, and excretion of [14C]CP-424391 in rats". Drug Metabolism and Disposition. 33 (1): 190–9. doi:10.1124/dmd.104.001065. PMID 15486077. S2CID 20760627.

[5] "Entyce". U.S. Food and Drug Administration (FDA). Retrieved 12 December 2022.

[6] "Elura". U.S. Food and Drug Administration (FDA). Retrieved 12 December 2022.

[7] Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Murray MC, et al. (November 2002). "Discovery and biological characterization of capromorelin analogues with extended half-lives". Bioorganic & Medicinal Chemistry Letters. 12 (22): 3279–82. doi:10.1016/s0960-894x(02)00734-5. PMID 12392732.

[8] Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Cook ER, et al. (February 2003). "Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin". Bioorganic & Medicinal Chemistry. 11 (4): 581–90. doi:10.1016/s0968-0896(02)00433-9. PMID 12538023.

[9] "Aratana Therapeutics Granted FDA Approval of Entyce (capromorelin oral solution)". Aratana Therapeutics. 17 May 2016. Retrieved 12 December 2022 – via PR Newswire.

[10] Pan LC, Carpino PA, Lefker BA, Ragan JA, Toler SM, Pettersen JC, et al. (February 2001). "Preclinical pharmacology of CP-424,391, an orally active pyrazolinone-piperidine [correction of pyrazolidinone-piperidine] growth hormone secretagogue". Endocrine. 14 (1): 121–32. doi:10.1385/ENDO:14:1:121. PMID 11322494. S2CID 46978604.

[11] White HK, Petrie CD, Landschulz W, MacLean D, Taylor A, Lyles K, et al. (April 2009). "Effects of an oral growth hormone secretagogue in older adults". The Journal of Clinical Endocrinology and Metabolism. 94 (4): 1198–206. doi:10.1210/jc.2008-0632. PMID 19174493.

[capromorelin-12] Rhodes L, Zollers B, Wofford JA, Heinen E (February 2018). "Capromorelin: a ghrelin receptor agonist and novel therapy for stimulation of appetite in dogs". Veterinary Medicine and Science. 4 (1): 3–16. doi:10.1002/vms3.83. PMC 5813110. PMID 29468076.

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