Mechanism of Action
Binds GHS-R1a for GH release AND CD36 receptors in cardiac tissue for direct cardioprotection. Anti-apoptotic effects in cardiomyocytes independent of GH axis.
Clinical Use
GH optimization, cardiac protection (off-label), body composition. Typically used in cycles to manage tachyphylaxis. Compounding.
Contraindications
Tachyphylaxis with continuous use requires cycling. Active malignancy.
Evidence Summary
Phase I/II human trials confirming GH release and cardiac effects. EU Phase II data for cardiac failure. Tachyphylaxis limits long-term use.
Key Studies
- 1.Broglio et al., JCEM 1999 — cardioprotection in heart failure patients demonstrated
- 2.Mao et al., Endocrinology 2007 — CD36 cardiac receptor identification and binding confirmed
- 3.Tivesten et al., J Cardiovasc Pharmacol 2000 — cardiac function improvement in human study
Evidence Gaps
Not FDA-approved. Tachyphylaxis limits long-term use. EU Phase II data limited.
Emerging Research
CD36-mediated cardiac receptor effects remain an area of active research interest.