Impact of Tesamorelin, a Growth Hormone-Releasing Factor (GRF) Analogue, on the Pharmacokinetics of Simvastatin and Ritonavir in Healthy Volunteers.
Teng. Shirley S; Potvin. Diane D; Mamputu. Jean-Claude JC; Vincent. Geneviève G; Zoltowska. Monika M; Morin. Josée J; Hatimi. Saida S; Michaud. Sophie-Elise SE; High. Kim K; Ducharme. Murray P MP
Key Findings
- Tesamorelin had no significant effect on the overall exposure (AUC) of simvastatin or ritonavir.
- Cmax (peak level) of ritonavir dropped slightly, but the change was small and not clinically important.
- Both drugs can be safely co‑administered with tesamorelin without dose adjustments.
Practical Outcomes
- If you’re using tesamorelin for anti‑aging or body composition goals, you can keep your usual simvastatin or ritonavir regimen. No special timing or dose changes are needed, making it easier to stack these compounds safely.
Summary
Tesamorelin doesn't meaningfully change how the liver enzyme CYP3A processes common drugs like simvastatin (a cholesterol pill) and ritonavir (an antiviral). In healthy volunteers, the drug levels stayed within the normal range, so you don't need to adjust the doses of these meds when you take tesamorelin.
Abstract
The potential impact of tesamorelin on CYP3A activity was investigated by examining its effect on the pharmacokinetics of simvastatin and ritonavir. In two randomized, two-way crossover studies, subjects were administered 2 mg tesamorelin on Days 1-7 with 80 mg simvastatin or 100 mg ritonavir co-administered on Day 6 (Treatment A), and a single dose of simvastatin or ritonavir alone on Day 6 (Treatment B). Pharmacokinetic samples were collected on Day 6 to measure simvastatin, ritonavir and tesamorelin plasma concentrations. For simvastatin, A/B ratios of least squares geometric means and corresponding 90% confidence intervals (CIs) for AUC0-t , AUC0-inf and Cmax were contained within the usual no effect range of 80-125%. For ritonavir, ratios and 90% CIs for AUCs were within this acceptance range, but the lower CI for Cmax was 74.8%, suggesting a decreased rate of exposure. However, since the A/B ratios for AUCs and Cmax parameters were approximately 90%, these were minor decreases and no dose adjustment of ritonavir is required in the presence of tesamorelin. These studies showed that the impact of tesamorelin on CYP3A activity appears to be minimal, if any. Either medication may be co-administered with tesamorelin in patients without changing their original dosing regimen.
Study Information
pubmed
2013
2013-05-15T00:00:00.000Z
10.1002/cpdd.27
2
22