CAPROMORELIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C28H35N5O4
Molecular Weight	505.6086
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1N=C2CCN(C[C@@]2(CC3=CC=CC=C3)C1=O)C(=O)[C@@H](COCC4=CC=CC=C4)NC(=O)C(C)(C)N

InChI

InChIKey=KVLLHLWBPNCVNR-SKCUWOTOSA-N

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

HIDE SMILES / InChI

Molecular Formula	C28H35N5O4
Molecular Weight	505.6086
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.aratana.com/wp-content/uploads/2016/12/ENTYCE-Pkg_Insert-8_5x11-FINAL.pdf
Curator's Comment: description was created based on several sources, including: https://www.ncbi.nlm.nih.gov/pubmed/19174493 | http://adisinsight.springer.com/drugs/800011628

Capromorelin is a potent ghrelin receptor agonist. Capromorelin is indicated for appetite stimulation in dogs. Plasma insulin-like growth factor-I (IGF-I) was elevated progressively over a 5-d course of daily oral dosing in dogs. In healthy older adults at risk for functional decline, administration of the capromorelin may improve body composition and physical function. Adverse events included fatigue, insomnia, and small increases in fasting glucose, glycosylated hemoglobin, and indices of insulin resistance.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Ghrelin receptor 15 Target ID: CHEMBL4616 Sources: DOI: 10.2174/2212796807999131128125920 \| https://www.ncbi.nlm.nih.gov/pubmed/24670149	Agonist 2752		7.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Inappetence 2 Sources: http://www.aratana.com/wp-content/uploads/2016/12/ENTYCE-Pkg_Insert-8_5x11-FINAL.pdf	Palliative		Approved 8583	ENTYCE Approved Use ENTYCE is indicated for appetite stimulation in dogs Launch Date 2016
Aging 4 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19174493	Palliative		Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
28.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
90.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
187.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
33.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
71.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
206.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
97.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
254.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
527.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
135.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
346 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
798.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
2.75 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.54 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.56 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.02 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.91 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25448190/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	CAPROMORELIN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
100 mg single, oral Highest studied dose Dose: 100 mg Route: oral Route: single Dose: 100 mg Sources: https://pubmed.ncbi.nlm.nih.gov/25448190/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/25448190/	Sources: https://pubmed.ncbi.nlm.nih.gov/25448190/

PubMed

Title	Date	PubMed
Smaller cardiac cell size and reduced extra-cellular collagen might be beneficial for hearts of Ames dwarf mice.	2010-09-01	20827400
Evidence for functional ghrelin receptors on parasympathetic preganglionic neurons of micturition control pathways in the rat.	2010-09	20497419
The prokinetic face of ghrelin.	2010	20721347
Effects of an oral growth hormone secretagogue in older adults.	2009-04	19174493
Growth hormone (GH)-releasing hormone and GH secretagogues in normal aging: Fountain of Youth or Pool of Tantalus?	2008	18488883
Gateways to clinical trials.	2007-04	17520107
Gastric motor effects of peptide and non-peptide ghrelin agonists in mice in vivo and in vitro.	2005-08	15843418
Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin.	2003-02-20	12538023
Discovery and biological characterization of capromorelin analogues with extended half-lives.	2002-11-18	12392732

Patents

Sample Use Guides

In Vivo Use Guide

Dog: 3 mg/kg body weight once daily

Route of Administration: Oral

In Vitro Use Guide

In rat pituitary cell cultures, Capromorelin stimulated growth hormone release with an EC50 = 3 nM.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:50:44 GMT 2025` Edited by `admin` on `Mon Mar 31 18:50:44 GMT 2025`
Record UNII	0MQ44VUN84
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CP-424,391

Preferred Name

English

CAPROMORELIN

Official Name

English

CAPIMORELIN

Common Name

English

PROPANAMIDE, 2-AMINO-N-(2-(2,3,3A,4,6,7-HEXAHYDRO-2-METHYL-3-OXO-3A-(PHENYLMETHYL)-5H-PYRAZOLO(4,3-C)PYRIDIN-5-YL)-2-OXO-1-((PHENYLMETHOXY)METHYL)ETHYL)-2-METHYL-, (R-(R*,R*))-

Common Name

English

CP-424391

Code

English

capromorelin [INN]

Common Name

English

2-AMINO-N-((1R)-1-(((3AR)-3A-BENZYL-2,3,3A,4,6,7-HEXAHYDRO-2-METHYL-3-OXO-5H-PYRAZOLO(4,3-C)PYRIDIN-5-YL)CARBONYL)-2-(BENZYLOXY)ETHYL)-2-METHYLPROPIONAMIDE

Common Name

English

CAPROMORELIN [MI]

Common Name

English

CAPROMORELIN [GREEN BOOK]

Common Name

English

Classification Tree Code System Code

CFR

21 CFR 520.292