Ipamorelin
Selective GH secretagogue with a cleaner side-effect profile than GHRP-6.
Evidence Score
Score Breakdown
Overview
Ipamorelin is a synthetic pentapeptide growth hormone secretagogue that selectively stimulates growth hormone (GH) release without significantly affecting cortisol, prolactin, or ACTH levels. It has undergone Phase II clinical trials for post-operative ileus but is primarily used off-label in anti-aging and performance contexts.
Mechanism of Action
Ipamorelin binds the growth hormone secretagogue receptor (GHS-R1a, the ghrelin receptor) in the pituitary, triggering pulsatile GH release. Its selectivity for GH over other pituitary hormones distinguishes it from earlier secretagogues like GHRP-6. GH then stimulates hepatic IGF-1 production, driving downstream anabolic effects.
Evidence Base
Phase II clinical trials were conducted for post-operative ileus recovery (Helsinn Healthcare). These trials demonstrated GH elevation and safety data in hospitalized patients. No FDA approval was obtained. Additional published pharmacokinetic studies exist. Off-label use in anti-aging clinics is widespread.
Gene Pathway Detail
GHS-R1a activation stimulates the GH/IGF-1 axis, driving hepatic IGF-1 gene expression and downstream anabolic gene programs including IGFBP-3, ALS, and tissue-specific IGF-1 receptor signaling. Biomeme could monitor IGF-1 axis gene expression to confirm GH secretagogue activity.
mRNA Monitoring Insight
IGF-1 and IGFBP gene expression changes are monitorable and provide functional readout of GH axis activation. This is valuable because serum GH levels are pulsatile and difficult to interpret from single blood draws, while mRNA changes reflect sustained pathway engagement.
Safety Considerations
Phase II trial data showed acceptable safety profile. Fewer off-target effects than earlier GH secretagogues (no significant cortisol/prolactin increase). Long-term safety data is limited. Theoretical concerns around sustained GH elevation include insulin resistance and potential tumor promotion.
FAQ
How is ipamorelin different from HGH?
Quick Facts
- Category
- Growth Hormone Secretagogue
- Score
- 52/100 (C+)
- Gene Pathways
- 4 characterized
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