证据内容以英文维护。

GHRP-2 的理想化结构描述

由序列构建的理想化构象;并非实验结构或预测结构。

速览

ENTRY TYPE
approved diagnostic
IDENTITY
Sequence verified

No structure asset recorded

TOP EVIDENCE
Grade A — GHD diagnosis (adults and children)
MAJOR STATUS
Jurisdiction-specific — see status table
SPORT
Prohibited — as of 2026-08-06
VERIFIED
2026-08-06

Bottom line

GHRP-2 (pralmorelin) is a synthetic hexapeptide ghrelin-receptor agonist. It received regulatory approval in Japan in 2004 as a diagnostic agent for growth hormone deficiency. A separate 48-week, randomized intranasal-treatment trial in 126 children found no significant improvement in growth despite increasing GH secretion; that treatment study was not the basis for the diagnostic evidence summarized below. Human pharmacology studies report that GHRP-2 can also affect ACTH, cortisol, and prolactin.

Identity and composition

FieldVerified information
Preferred nameGHRP-2 (Pralmorelin)
Key aliasesKP-102, GPA-748, Growth Hormone Releasing Peptide-2, pralmorelin
Molecular/sequence identityHexapeptide: D-Ala-D-2-Nal-Ala-Trp-D-Phe-Lys-NH2
Modifications/formD-amino acids at positions 1, 2, and 5 confer metabolic stability; D-2-naphthylalanine (D-2-Nal) at position 2 enhances binding affinity
Stable identifiers: 6918245; CAS: 158861-67-7; MW ~818 Da
Identity caveatsNot to be confused with GHRP-6 (His-D-Trp-Ala-Trp-D-Phe-Lys-NH2, ~873 Da). Assay-specific potency comparisons should not be converted into human-dose equivalence.

Development and approval status

JurisdictionStatus and indicationProduct/sourceAs of
Japan (PMDA)Approved 2004 for diagnostic testing of GH deficiencyPralmorelin (Kaken Pharmaceutical)2026-08-06
US (FDA)No approved indication; development discontinued2026-08-06
EU (EMA)No marketing authorization2026-08-06
Status is multi-axis
GHRP-2 authorization and sport-status profileFour medicine-authorization axes reproduce only documented status rows; sport status is shown separately.UNITED STATESNo approved indication;development discontinuedSOURCE / AS OFROW 2 / 2026-08-06EU/EEANo marketing authorizationSOURCE / AS OFROW 3 / 2026-08-06UNITED KINGDOMSOURCE ROW OMITTEDSEE AUDIT REASONSOURCE / AS OFNOT PRESENT / NOT RECORDEDOTHER DOCUMENTEDApproved 2004 for diagnostictesting of GH deficiencySOURCE / AS OFROW 1 / 2026-08-06SPORT STATUS — SEPARATE FROM MEDICINE AUTHORIZATIONPralmorelin is a prescription diagnostic in Japan. The 2026 WADA Prohibited List explicitlynames GHRP-2 (pralmorelin) among GH-releasing peptides in section S2.2.4; it is prohibited
Authorization belongs to the named product, use, place, and date; sport status is independent.
文字说明
UNITED STATES
US (FDA): No approved indication; development discontinued
EU/EEA
EU (EMA): No marketing authorization
UNITED KINGDOM
No UNITED KINGDOM row is present in the source status table
OTHER DOCUMENTED
Japan (PMDA): Approved 2004 for diagnostic testing of GH deficiency

Sport status: Pralmorelin is a prescription diagnostic in Japan. The 2026 WADA Prohibited List explicitly names GHRP-2 (pralmorelin) among GH-releasing peptides in section S2.2.4; it is prohibited at all times. It has been detected in seized nutritional supplements (Thomas et al., Drug Test Anal 2010; PMID: 20878896).

Mechanism and pharmacology

GHRP-2 is an agonist at the ghrelin receptor (GHS-R1a) on pituitary somatotroph cells and can provoke an acute GH response. Human pharmacology studies also report effects on ACTH, cortisol, and prolactin. Route-specific observations from small studies should not be generalized to unapproved therapeutic use.

Evidence by claim

Claim/indicationStageGradeBest human evidenceMain resultImportant limitations
GHD diagnosis (adults and children)Approved (Japan)APMDA product record and 2014 re-examination report; 503 postmarketing cases from 19 institutions, with 502 in the effectiveness analysisAgainst clinician diagnosis based on at least two other GH-stimulation agents, the 9 ng/mL criterion for severe GHD had sensitivity 0.853 and specificity 0.885; ROC AUC 0.939Japan-specific product and indication; postmarketing comparison was retrospective and does not establish therapeutic use
Short stature treatmentPhase II (discontinued) [1]XTanaka et al., 2014; intranasal GHRP-2 in short GHD childrenIncreased GH secretion but no clinically significant growth promotionIntranasal route; therapeutic program discontinued
GH release (acute pharmacology)Phase I [1]CPihoker et al., J Clin Endocrinol Metab 1998; ten prepubertal short childrenAcute GH response and PK/PD parameters characterized after one exposurePharmacology endpoints only; small, selected pediatric population
Food intake/metabolismHuman studyCLaferrère et al., J Clin Endocrinol Metab 2005; seven lean healthy menA 270-minute infusion increased buffet-meal energy intake by 35.9% versus salineAcute crossover experiment; small N
证据等级
  • AA级:已确定特定标签用途
  • BB级:中等人体证据
  • CC级:初步人体证据
  • DD级:仅临床前
  • EE级:轶事/营销声明
  • XX级:证据与该声明相矛盾或不支持该声明
了解有关证据分级的更多信息
Claim-evidence profile
GHRP-2 claim-evidence profileA: 1 claim; B: 0 claims; C: 2 claims; D: 0 claims; E: 0 claims; X: 1 claimCONTRADICTORY / NON-SUPPORTIVEA — Established for a specific labeled useGrade A: Established for a specific labeled use — current approval plus adequate controlled trials and post-market context.1 claimGHD diagnosis (adults and children)B — Moderate human evidenceGrade B: Moderate human evidence — multiple controlled studies or a strong pivotal study, but no current approval for the claim.0 claimsC — Preliminary human evidenceGrade C: Preliminary human evidence — small, uncontrolled, surrogate-endpoint, or early-phase studies.2 claimsGH release (acute pharmacology)Food intake/metabolismD — Preclinical onlyGrade D: Preclinical only — in vitro or animal evidence with no adequate human efficacy evidence.0 claimsE — Anecdotal/marketing claimGrade E: Anecdotal/marketing claim — testimonials, extrapolation, or vendor claims without adequate scientific support.0 claimsX — Evidence contradicts or does not support the claimGrade X: Evidence contradicts or does not support the claim — adequate negative evidence, failed program, or claim inconsistent with the studied material.1 claimShort stature treatment
This counts the page's claim rows; it does not average them into a score.
文字说明

Text alternative for the claim-evidence diagram. Each grade is defined below:

AEstablished for a specific labeled use
1 claim: GHD diagnosis (adults and children)
BModerate human evidence
0 claims
CPreliminary human evidence
2 claims: GH release (acute pharmacology); Food intake/metabolism
DPreclinical only
0 claims
EAnecdotal/marketing claim
0 claims
XEvidence contradicts or does not support the claim
1 claim: Short stature treatment
United StatesNo approved indication; development discontinued
EU/EEANo marketing authorization
OtherApproved 2004 for diagnostic testing of GH deficiency

Key studies

StudyDesign/populationExposure studiedEndpoints and resultLimitations
PMDA re-examination report (2014)Official regulatory reassessment; 503 postmarketing cases from 19 Japanese institutions, 502 in effectiveness analysisJapan-labeled single diagnostic administrationAt the 9 ng/mL severe-GHD criterion, sensitivity was 0.853, specificity 0.885, and ROC AUC 0.939 versus clinician diagnosis using at least two other stimulation agentsRetrospective postmarketing comparison; not a randomized trial or therapeutic study
Drugs R&D drug profile (2004); PMID: 15230633Secondary, unsigned development-profile article summarizing pralmorelin's pharmacology and then-current development status [1]Not a primary trial reportDescribed the diagnostic rationale and reported a 15 mcg/L peak-GH threshold from the development recordSecondary source; published before Japanese approval and should not be cited as the primary multicenter diagnostic trial
Pihoker et al., J Clin Endocrinol Metab 1998; PMID: 9543135Phase I PK/PD; ten prepubertal short children (nine boys and one girl; mean age 7.7 years) [1]One 1 mcg/kg exposure over 1 minuteTerminal 0.55 hours; GH reached maximum concentration at 0.42 hoursPharmacology study only; small, selected pediatric population
Tanaka et al., Clin Pediatr Endocrinol 2014; PMID: 25148835Phase II; short children with GHD [1]Intranasal GHRP-2 sprayIncreased GH but no significant height velocity improvementTherapeutic program discontinued
Laferrère et al., J Clin Endocrinol Metab 2005; PMID: 15699539Randomized within-subject comparison; seven lean healthy men [1] infusion at 1 mcg/kg/hour for 270 minutesFood intake increased 35.9% versus saline; serum GH also increasedAcute setting only; small N; not a therapeutic dose-finding study

Dose and administration evidence

Approved labeled regimen

The label summary below is product-, indication-, and jurisdiction-specific; consult the full current label and a licensed clinician/pharmacist.

Japan-approved diagnostic exposure (PMDA): 2 mcg/kg by slow injection for ages 4–17 years, capped at 100 mcg; 100 mcg by slow IV injection for adults, administered fasting. A peak GH cutoff of 16 ng/mL is used for children; 9 ng/mL for adults. This is a single-administration diagnostic test for GH deficiency — not a therapeutic regimen and not guidance for self-administration.

Studied regimens (not recommendations)

No established or recommended human dose. This sentence concerns therapeutic and other unapproved use; it does not erase the separate Japan-specific, single-administration diagnostic label above. Published nontherapeutic pharmacology studies used protocol-specific exposures under research oversight; they do not establish a therapeutic regimen.

What is not established

  • Effective therapeutic dose for any non-diagnostic indication

  • Safety or efficacy of chronic daily administration

  • Dose finding for body composition or performance claims

Safety

Established label risks

The PMDA re-examination report recorded no adverse drug reactions among 503 postmarketing cases, while the preapproval Japanese trials recorded adverse drug reactions in 86 of 227 participants (37.9%), most commonly borborygmi, feeling hot, sweating, and increased white-blood-cell count. These product-specific diagnostic data do not establish chronic-use safety.

Human-study signals

At higher or repeated doses, GHRP-2 can elevate cortisol and prolactin. Mild injection-site reactions, transient flushing, and increased appetite have been reported.

Unknowns and product-quality risks

Long-term safety (beyond single/diagnostic administration) is not established. No Phase III therapeutic safety data exist. Research-grade material is unregulated.

Interactions and special populations

No formal drug-interaction studies. Diagnostic use should avoid concomitant GH-suppressing medications.

Regulatory, compounding, and sport notes

Pralmorelin is a prescription diagnostic in Japan. The 2026 Prohibited List explicitly names GHRP-2 (pralmorelin) among GH-releasing peptides in section S2.2.4; it is prohibited at all times. It has been detected in seized nutritional supplements (Thomas et al., Drug Test Anal 2010; PMID: 20878896).

Evidence gaps

  • No Phase III therapeutic efficacy trial

  • No long-term safety data beyond diagnostic single-dose use

  • No adequate human body-composition data

  • No studies in women for most endpoints

  • No approved therapeutic indication outside Japan

Search notes

  • Databases and registries: PubMed, ClinicalTrials.gov, PMDA (Japan), FDA Drugs@FDA

  • Search terms: "GHRP-2", "pralmorelin", "KP-102", "growth hormone releasing peptide 2"

  • Last searched: 2026-08-06

  • Inclusion emphasis: Human studies; regulatory documents; primary peer-reviewed data

Sources

  1. Drugs R&D. Pralmorelin: GHRP 2, GPA 748, growth hormone-releasing peptide 2, KP-102 D, KP-102 LN. 2004;5(4):236-239. PMID: 15230633. PubMed classifies this unsigned article as a review; it is a development profile, not the primary multicenter diagnostic trial report. https://pubmed.ncbi.nlm.nih.gov/15230633/

  2. Pihoker C et al. Pharmacokinetics and pharmacodynamics of GHRP-2: a phase I study in children. J Clin Endocrinol Metab. 1998;83(4):1168-1172. https://pubmed.ncbi.nlm.nih.gov/9543135/

  3. Tanaka T et al. Intranasal GHRP-2 in short children with GH deficiency. Clin Pediatr Endocrinol. 2014;23(4). https://pubmed.ncbi.nlm.nih.gov/25148835/

  4. Laferrère B et al. Growth hormone-releasing peptide-2 (GHRP-2), like ghrelin, increases food intake in healthy men. J Clin Endocrinol Metab. 2005;90(2):611-614. PMID 15699539. https://pubmed.ncbi.nlm.nih.gov/15699539/

  5. Thomas A et al. Identification of GHRP-2 in a nutritional supplement. Drug Test Anal. 2010;2(3):144-148. https://pubmed.ncbi.nlm.nih.gov/20878896/

  6. WADA. 2026 Prohibited List, section S2.2.4. https://www.wada-ama.org/sites/default/files/2025-09/2026list_en_final_clean_september_2025.pdf

  7. PubChem CID 6918245. https://pubchem.ncbi.nlm.nih.gov/compound/6918245

  8. Pharmaceuticals and Medical Devices Agency. GHRP Kaken 100 (pralmorelin hydrochloride), current product information. https://www.pmda.go.jp/PmdaSearch/rdDetail/iyaku/7223407D2023_1?user=1

  9. Pharmaceuticals and Medical Devices Agency. Re-examination report for GHRP Kaken 100 (approved indication and labeled diagnostic administration). https://www.pmda.go.jp/drugs_reexam/2014/P201400051/20002200_21600AMZ00573_A100_1.pdf

专家观点

专家怎么说

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视频

问题

What is GHRP-2 and what is its relationship to pralmorelin?

GHRP-2 (pralmorelin) is a synthetic hexapeptide ghrelin-receptor agonist. It received regulatory approval in Japan in 2004 as a diagnostic agent for GH deficiency under the name Pralmorelin (Kaken Pharmaceutical). It is not to be confused with GHRP-6, which has a different sequence and molecular weight.

Is GHRP-2 approved by the FDA or EMA?

No. The monograph documents approval in Japan as a single-administration diagnostic test for GH deficiency, no FDA-approved indication in the US, and no EMA marketing authorization in the EU. Status in other jurisdictions is not established here. Therapeutic development for short stature was discontinued after a Phase II trial of a nasal formulation found no clinically significant growth promotion.

What human evidence supports GHRP-2 for therapeutic use?

A phase 2 trial in children with growth hormone deficiency found increased GH secretion but no clinically significant growth promotion, and the therapeutic program was discontinued. A small acute study in seven men reported increased food intake versus saline. These nontherapeutic pharmacology findings do not establish a therapeutic regimen. No phase 3 therapeutic efficacy trial exists. No established or recommended human dose.

What are the main safety signals for GHRP-2?

Preapproval Japanese trials recorded adverse drug reactions in 86 of 227 participants (37.9%), most commonly borborygmi, feeling hot, sweating, and increased white-blood-cell count. Human pharmacology studies also report effects on cortisol and prolactin. Long-term safety beyond single diagnostic use is not established.

Is GHRP-2 prohibited by WADA?

Yes. The 2026 WADA Prohibited List explicitly names GHRP-2 (pralmorelin) among GH-releasing peptides in section S2.2.4; it is prohibited at all times. It has been detected in seized nutritional supplements.

What evidence supports the Japan-approved diagnostic use of GHRP-2?

A 2014 PMDA re-examination included 503 postmarketing cases, with 502 in the effectiveness analysis. Against clinician diagnosis based on at least two other GH-stimulation agents, the reported severe-GHD criterion had sensitivity 0.853, specificity 0.885, and ROC AUC 0.939. The comparison was retrospective and does not establish therapeutic use.

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