TESAMORELIN
Tesamorelin (Egrifta) is a 44-amino-acid GHRH (1-44) analog with trans-3-hexenoyl modification at His1 + Ala8 → half-life 26–38 minutes (vs. native 7min). FDA-approved 2010 for HIV-associated lipodystrophy (visceral fat reduction); stimulates pituitary GH/IGF-1 without direct GH risks. Research expands to Alzheimer’s cachexia, NAFLD.
Approval Edge: Only GHRH with NDA; clean compliance data.
Mechanism
- GHRH-R: ↑cAMP → pulsatile GH release.
- IGF-1 Mediation: Liver production ↑1.5–2x.
- Lipolytic: Visceral fat β3-AR activation.
- No Desensitization: Native sequence preserved.
Clinical Evidence
| Indication | Trials/Outcomes |
|---|---|
| HIV Lipodystrophy | VAT -15% (26w), triglycerides ↓ (Phase 3, NEJM 2010; n=400). |
| IGF-1 | +23–40% sustained (52w). |
| Cachexia | Lean mass +1.5kg (Alzheimer’s pilot). |
| Safety | No glucose worsening, cancer signals. |
RECOMBINE Trial: Confirmed durability.
Protocols
| Goal | Dose (mg/day) | Route/Frequency | Cycle |
|---|---|---|---|
| Lipodystrophy | 2mg | SubQ daily PM | Continuous (monitored) |
| IGF-1 Research | 1–2mg | Once daily | 12–26 weeks |
| Cachexia | 1mg | BID | 12 weeks |
- Egrifta Vial: 2mg recon w/ sterile water.
- Stack: Ipamorelin (pulse amp).
Benefits
- Visceral Fat: Gold standard HIV.
- IGF-1 Restore: GH-deficient proxy.
- Muscle Preservation: Anabolic signaling.
- Metabolic: Lipids, no hypo risk.
- Neuro: Alzheimer’s Phase 2.
Side Effects
| Common (25%) | Serious (Manageable) | Mitigation |
|---|---|---|
| Inj site rxn, arthralgia | IGFD (monitor) | Rotate sites |
| Paresthesia | Glucose ↑ (mild) | Baseline labs |
Comparisons
| GHRH | Half-Life | Approved? | HIV VAT? |
|---|---|---|---|
| Tesamorelin | 30min | Yes | Yes |
| CJC-1295 DAC | 7 days | No | No |
| Sermorelin | 10min | Yes (old) | No |
| Alexamorelin | Short | No | No |
Status & Access
- FDA: Egrifta Rx (HIV only).
- UK: Private/import; research chemical.
Disclaimer: Prescription/research; IGF-1 monitoring required.
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