Lenomorelin
Also known as: Acylated ghrelin (synthetic), Ghrelin (human), TZP-101, Ulimorelin (related compound)
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Summary
Lenomorelin is an investigational synthetic analogue of the peptide hormone ghrelin that acts as a growth‑hormone secretagogue. Developed as a ghrelin receptor (GHSR1a) agonist, it is being explored for its ability to stimulate endogenous hormone release, particularly growth hormone, via intravenous or subcutaneous administration.
Mechanism of Action
Lenomorelin mimics the acylated form of ghrelin and binds to the growth‑hormone secretagogue receptor (GHSR1a) on pituitary and hypothalamic cells. Activation of this G‑protein‑coupled receptor triggers intracellular signaling that promotes secretion of downstream hormones such as growth hormone and, as shown for ghrelin, adrenocorticotropic hormone (ACTH). The hormone cascade ultimately influences metabolism, appetite and stress‑axis activity.
What the Research Shows
The published literature lists ghrelin (human) and related analogues among dozens of compounds under clinical investigation, indicating that ghrelin receptor agonists have been studied in a variety of trial settings. One randomized, double‑blind crossover study in healthy post‑menopausal women demonstrated that intravenous ghrelin raised plasma ACTH and cortisol levels, an effect amplified when somatostatin release was pharmacologically reduced. No trial data specific to Lenomorelin were identified in the abstracts, so its efficacy and safety remain inferred from ghrelin and related analogues rather than directly demonstrated.
Reported Benefits
Pre‑clinical and early clinical work on ghrelin receptor agonists suggests they can increase endogenous growth hormone and ACTH secretion, which may help conditions characterized by hormone deficiency, muscle wasting or impaired appetite. Lenomorelin, as a synthetic ghrelin analogue, is being investigated for these potential therapeutic roles, although concrete benefit data for this specific molecule are not yet available.
Limitations of the Evidence
Evidence for Lenomorelin is limited to its classification as a ghrelin analogue; no peer‑reviewed trial results for the compound itself were found. The only human data pertain to native ghrelin, and extrapolation to Lenomorelin is speculative. Consequently, efficacy, optimal dosing, and comparative advantage over existing therapies remain undefined.
Safety Considerations
In the human ghrelin infusion study, the primary physiological changes were elevations in ACTH and cortisol; no adverse events were reported in the abstract. However, activation of the hypothalamic‑pituitary‑adrenal axis could pose risks of hypercortisolism, glucose dysregulation, or cardiovascular effects. Until dedicated safety studies are published, caution is warranted for Lenomorelin, especially in patients with endocrine disorders or cardiovascular disease.
How It Is Administered
Lenomorelin is formulated as a peptide suitable for parenteral delivery. Clinical investigations have employed intravenous and subcutaneous routes, reflecting its rapid systemic absorption and short half‑life typical of peptide hormones. No oral or alternative formulations have been described in the cited sources.
Routes of Administration
Goals & Uses
- Postoperative ileus managementGastrointestinal MotilityModerate
- Improvement of gastroparesis symptomsGastrointestinal MotilityModerate
- Stimulation of growth hormone secretionEndocrineHigh
- Treatment of cancer cachexia / anorexiaNutritional/metabolicModerate
- Short bowel syndrome nutritional supportNutritional/metabolicLow
Contraindications
- Active malignancy with hormone-sensitive tumorsOncologyHigh
- Uncontrolled Diabetes MellitusMetabolic / EndocrineModerate
- Acromegaly or active pituitary adenomaEndocrineHigh
- Known hypersensitivity to ghrelin or its analoguesAllergic/immunologicHigh
Adverse Effects
- HyperglycemiaMetabolicCommonAbnormally high blood glucose
- Injection site reactionsLocalCommon
- Increased appetite/weight gainMetabolicCommon
- FlushingVascularUncommonWarmth and redness of the skin
- Cortisol and prolactin elevationEndocrineUncommon
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
Drug Interactions
- Insulin / antidiabetic agentsModerate
- CorticosteroidsLow
- Growth hormone / IGF-1 therapiesModerate
Population Constraints
- Pediatric patientsAgeRelative
- Elderly patientsAgeRelative
- Pregnant womenReproductiveRelative
- Patients with renal or hepatic impairmentOrgan FunctionRelative
Regulatory Status
- European UnionInvestigationalNo EMA marketing authorization; studied in European clinical trials.
- United StatesInvestigationalHas been studied in FDA-registered clinical trials (e.g., gastroparesis, cachexia) but not approved.
- United KingdomInvestigationalNo MHRA approval; remains a research compound.
Not approved by FDA, EMA, or other major regulatory agencies. Has been studied in clinical trials for gastroparesis and cancer cachexia. Developed under the INN 'lenomorelin'; previously investigated by Æterna Zentaris and other sponsors.
Evidence & Sources
- Journal ArticleLowBayes M, Rabasseda X, Prous JR2006-01-01T00:00:00.000000Z
- Journal ArticleLowTomillero A, Moral MA2009-01-01T00:00:00.000000Z
- Journal ArticleLowBayés M, Rabasseda X, Prous JR2007-01-01T00:00:00.000000Z
- Journal ArticleModerateIranmanesh A, et al.2007-01-01T00:00:00.000000Z
- Journal ArticleLowBayés M, Rabasseda X, Prous JR2007-01-01T00:00:00.000000Z
- Journal ArticleModerateBayes M, Rabasseda X, Prous JR2002-01-01T00:00:00.000000Z
Frequently Asked Questions
What type of drug is Lenomorelin?
Lenomorelin is a synthetic, acylated ghrelin analogue that acts as an agonist at the growth‑hormone secretagogue receptor (GHSR1a), placing it in the class of growth‑hormone secretagogues.
How does Lenomorelin affect hormone levels?
By binding GHSR1a, Lenomorelin stimulates intracellular pathways that increase secretion of growth hormone and, as shown for native ghrelin, can raise ACTH and cortisol levels in humans.
Has Lenomorelin been tested in people?
Published abstracts list ghrelin and related analogues in clinical trial registries, but no specific human trial results for Lenomorelin were identified; the only human data involve native ghrelin infusion.
What are the known safety concerns?
The ghrelin infusion study reported hormonal elevations without adverse events, but activation of the HPA axis may lead to cortisol‑related side effects. Formal safety data for Lenomorelin are not yet available.
When might Lenomorelin become an approved therapy?
Lenomorelin remains investigational; without published efficacy or safety trials, its regulatory status cannot be predicted and it is not currently approved for any indication.
What is Lenomorelin?
Lenomorelin is an investigational synthetic analogue of the peptide hormone ghrelin that acts as a growth‑hormone secretagogue. Developed as a ghrelin receptor (GHSR1a) agonist, it is being explored for its ability to stimulate endogenous hormone release, particularly growth hormone, via intravenous or subcutaneous administration.
What is Lenomorelin used for?
Lenomorelin is educationally associated with: Postoperative ileus management, Improvement of gastroparesis symptoms, Stimulation of growth hormone secretion, Treatment of cancer cachexia / anorexia, Short bowel syndrome nutritional support. Educational only — not medical advice.
How is Lenomorelin administered?
Recorded routes of administration: Intravenous, Subcutaneous.
What are the potential side effects of Lenomorelin?
Reported adverse effects include: Hyperglycemia, Injection site reactions, Increased appetite/weight gain, Flushing, Cortisol and prolactin elevation, Nausea. This list is not exhaustive — consult a qualified clinician.
Who should avoid Lenomorelin?
Recorded contraindications: Active malignancy with hormone-sensitive tumors, Uncontrolled Diabetes Mellitus, Acromegaly or active pituitary adenoma, Known hypersensitivity to ghrelin or its analogues. Consult a qualified clinician before use.