Tesamorelin
(07)
Overview
Tesamorelin is a growth hormone–releasing factor (GHRF) analog approved to reduce excess abdominal fat (visceral adipose tissue, VAT) in adults with HIV-associated lipodystrophy. It is not a weight-loss drug and long-term cardiovascular safety hasn’t been established.
Category
(GHRH) Analog
Challenge
Developing tesamorelin required ensuring peptide stability, bioactivity, and purity under physiological conditions while maintaining selective stimulation of growth hormone–releasing hormone receptors. The formulation had to preserve tertiary structure and prevent enzymatic degradation during storage and systemic administration. Optimizing the lyophilized powder and reconstitution medium was essential to maintain peptide integrity and bioavailability after injection.
Impact
CJC-1295 enhances endogenous GH pulsatility via GHRH-receptor activation, raising IGF-1 and downstream pathways involved in lipolysis, protein synthesis, and metabolic regulation. Early studies showed sustained GH/IGF-1 increases and occasional modest reductions in fat mass or waist measures, but durable, long-term clinical benefits remain unproven.