PEL-007

PEL-007 is a novel, potent REV-ERB agonist designed to improve upon the pharmacokinetic profile and efficacy of first-generation REV-ERB agonists like SR9009. It acts as a nuclear receptor agonist, specifically targeting REV-ERBα and REV-ERBβ, which are essential for regulating circadian rhythms and cardiac mitochondrial function. In preclinical studies, PEL-007 has demonstrated significant cardioprotective effects against doxorubicin-induced cardiotoxicity by enhancing mitochondrial respiration, increasing ATP production, and suppressing pro-inflammatory gene expression. It effectively maintains cardiac ejection fraction in mouse models of chemotherapy-induced heart failure, suggesting potential as an adjuvant therapy to safeguard the heart during cancer treatment.