Ipamorelin 5mg/mL

Route: Subcutaneous injection. Administer into the abdomen, thigh, or upper arm subcutaneous tissue. Injection is typically performed once daily, often in the evening to coincide with the natural nocturnal GH pulse, or as directed by the prescriber. Use a new sterile insulin-type needle/syringe for each injection. Rotate injection sites. Reconstituted peptide solutions are time-sensitive; follow the prescribed reconstitution and administration instructions.

Dosing is entirely prescriber-determined. General published pharmacological context:

• Typical compounding practice doses have ranged from 100–300 mcg per injection, administered once to three times daily.
• Evening administration may align with physiologic nocturnal GH secretion peaks.
• Prescribers individualize dose based on patient clinical context, IGF-1 levels, and therapeutic goals.
• This is a 5 mg/mL preparation; exact draw volume is calculated by the prescriber.

Ipamorelin (Aib-His-D-2-Nal-D-Phe-Lys-NH₂) is a pentapeptide that selectively binds and activates the growth hormone secretagogue receptor 1a (GHS-R1a) — the same receptor activated by the endogenous hormone ghrelin — on somatotroph cells of the anterior pituitary. GHS-R1a is a Gq-protein-coupled receptor; its activation elevates intracellular cAMP (via protein kinase A) and mobilizes intracellular calcium, triggering pulsatile GH release. The resultant GH stimulates hepatic IGF-1 production (mediating anabolic effects on muscle, bone, and adipose tissue). Critically, ipamorelin's selectivity profile — demonstrated in swine models — shows no significant ACTH, cortisol, FSH, LH, prolactin, or TSH elevation even at doses far exceeding its GH-release ED₅₀, distinguishing it from earlier GHRPs (GHRP-2, GHRP-6) that also activate non-GHS-R1a pathways raising cortisol and prolactin.

Ipamorelin has been investigated in preclinical and limited human pharmacokinetic studies as a selective GH secretagogue. Prescriber-directed compounded use has focused on patient-specific contexts where increased endogenous GH pulsatility is a therapeutic goal — such as adult GH deficiency, age-related GH decline, body composition management, or recovery support. Prescribers should note ipamorelin is not FDA-approved and no large-scale human efficacy trials have been completed; clinical decisions should be based on available pharmacological evidence and patient-specific risk-benefit assessment.

Monitoring: IGF-1 levels at baseline and during therapy; fasting glucose (GH can induce insulin resistance); assess for signs of acromegaly (joint pain, coarsening of features) with prolonged use; injection site assessment.

Contraindications:

• Known hypersensitivity to ipamorelin or formulation components.
• Active malignancy: GH and IGF-1 elevation may potentially stimulate tumor growth; avoid in patients with active cancer.
• Pregnancy and lactation: insufficient safety data.

Warnings & Precautions:

• Insulin resistance: GH secretagogues may reduce insulin sensitivity; monitor fasting glucose in patients with diabetes or prediabetes.
• Fluid retention: mild, transient edema or water retention may occur.
• Pituitary tumors: GH secretagogues are contraindicated in patients with untreated pituitary pathology.
• Not FDA-approved; human clinical efficacy data are limited.

Drug Interactions:

• Glucocorticoids may blunt GH secretagogue response via somatostatin enhancement.
• Insulin and hypoglycemic agents: dose adjustment may be necessary due to GH-induced insulin resistance.

Common Side Effects: Injection site pain/redness; transient water retention; mild flushing; headache. Unlike GHRP-2/6, ipamorelin does not significantly elevate cortisol or prolactin at therapeutic doses.

Store lyophilized ipamorelin powder (pre-reconstitution) at 2°C–8°C; protect from light. After reconstitution with bacteriostatic water: refrigerate at 2°C–8°C and use within the beyond-use date assigned by Genesis Compounding (typically 30 days after reconstitution). Do not freeze reconstituted solution. Protect from light.

What distinguishes ipamorelin from other growth hormone-releasing peptides?

Ipamorelin is the first GHS-R1a agonist to selectively stimulate GH release without significantly elevating cortisol, ACTH, or prolactin — effects seen with older GHRPs (GHRP-2, GHRP-6). This selectivity makes its GH-stimulating effects more physiologically comparable to natural pulsatile GH secretion.

When should ipamorelin be injected?

Many prescribers direct evening (before sleep) subcutaneous injection to align with the natural nocturnal GH pulse. Your prescriber will specify the exact timing and frequency for your regimen.

How is IGF-1 related to ipamorelin therapy?

Ipamorelin stimulates GH release from the pituitary; GH then stimulates the liver to produce IGF-1 (insulin-like growth factor 1), which mediates many of GH's anabolic effects on muscle, bone, and adipose tissue. IGF-1 levels are monitored to assess the biological response to therapy.

Is ipamorelin FDA-approved?

No. Ipamorelin has no FDA-approved indication. This is a patient-specific, prescriber-directed 503A compounded preparation from Genesis Compounding, prepared based on prescriber clinical judgment.

Can ipamorelin be used with CJC-1295 or sermorelin?

Some prescribers combine GHS-R1a agonists (ipamorelin) with GHRH-receptor agonists (CJC-1295, sermorelin) to stimulate GH release through complementary receptor pathways. Any such combination is a prescriber-directed, patient-specific clinical decision.