Peptides›GH secretagogue›Capromorelin

Capromorelin

/ Non-peptide ghrelin receptor (GHS-R1a) agonist (spiroindoline class)

TIER 1 · ClinicalN = 0 · TESTING PENDINGMW 506.65 g·mol⁻¹

ALIAS · Entyce (trade — canine) · Elura (trade — feline) · CP-424,391 · Pfizer ghrelin agonist

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Research use onlyAny dose figures below describe what specific cited studies used, reported factually. Nothing on this page is guidance for human use.READ FIRST →

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§ A · Identity

Primary sequenceNon-peptide small molecule (spiroindoline scaffold)

MW · 506.65CLASS · Non-peptide ghrelin receptor (GHS-R1a) agonist (spiroindoline class)CATEGORY · GH secretagogue

FDA-approved as a veterinary therapeutic (Entyce 2016 for canine appetite stimulation; Elura 2020 for feline weight management in chronic kidney disease). The 'tier-1' rating reflects pivotal RCT-grade evidence; the indication is veterinary, not human. Originally developed by Pfizer for human sarcopenia/cachexia indications but discontinued human clinical development.

§ B · Mechanism of action

Capromorelin is a non-peptide selective agonist at the growth-hormone secretagogue receptor 1a (GHS-R1a), the endogenous receptor for ghrelin. Receptor occupancy in the hypothalamus and pituitary stimulates GH release and centrally drives appetite via NPY/AgRP neurons in the arcuate nucleus. In contrast to MK-677 (ibutamoren), capromorelin has been clinically developed primarily for the appetite-stimulation arm of GHS-R1a pharmacology rather than the GH/IGF-1 arm.

§ C · Human clinical evidence

Tier 1 in veterinary medicine. In humans, Phase 1 and Phase 2 trials in older adults demonstrated dose-dependent GH and IGF-1 elevation and increases in lean body mass, but the human program (originally targeting hip-fracture recovery and frailty) was not advanced to Phase 3. No FDA-approved human indication.

§ D · Primary literature

PubMed28056951Zollers B et al. — Capromorelin oral solution (ENTYCE®) increases food consumption and body weight when administered for 4 consecutive days to healthy adult Beagle dogs in a randomized, masked, placebo controlled study · BMC Veterinary Research · human-phase-3-rctOral capromorelin (3 mg/kg) significantly increased food consumption and body weight in healthy dogs over a 4-day dosing window; data supported FDA approval of Entyce.Limitations: Healthy-dog model rather than the clinical inappetence population; short dosing window; veterinary indication only — does not transfer to human use.2017

PubMed29468076Rhodes L et al. — Capromorelin: a ghrelin receptor agonist and novel therapy for stimulation of appetite in dogs · Veterinary Medicine and Science · reviewReviews mechanism (selective MK-0677-class non-peptide ghrelin agonist), pharmacokinetics, and the body of canine + feline pivotal data underlying FDA approval as Entyce/Elura.Limitations: Review article authored partly by sponsor (Aratana/Elanco) employees; primary outcome is mechanistic narrative, not original data.2018

§ F · Safety signal

In the veterinary RCT data, the most common adverse events were hypersalivation, vomiting, and lethargy at therapeutic doses. The class concern with sustained GHS-R1a agonism — insulin resistance and glucose intolerance — was noted in the discontinued human Phase 2 program but did not preclude approval at the lower doses used in companion animals.

§ H · Regulatory status

Regulatory status

FDA status:: FDA-approved

§ I · Notable gaps and controversies

Capromorelin is FDA-approved only in companion animals. Marketing or use in humans for appetite stimulation, weight gain, or GH/IGF-1 elevation lacks Phase 3 validation and falls outside any approved labelling. The veterinary product (oral solution) is not the same chemical material as research-grade powder sold by peptide vendors; lot purity and identity are not interchangeable.