Comparative analysis reveals distinct metabolic and vascular profiles between everolimus and sirolimus, highlighting the need for head-to-head trials in organ transplantation.
In comparison to sirolimus, everolimus has higher bioavailability, a shorter terminal half-life, different blood metabolite patterns, the potential to antagonize the negative effects of CNIs on neuronal and kidney cell metabolism (which sirolimus enhances), the ability to stimulate mitochondrial oxidation (which sirolimus inhibits) and to reduce vascular inflammation to a greater extent. A head-to-head, randomized trial comparing the safety and tolerability of these two mTOR inhibitors in solid organ transplant recipients is merited.
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Klawitter et al. (2015) studied this question.
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