Investigation of pharmacotherapeutic agents with the goal of enhancing mitochondrial function, ATP production, and exercise performance in athletes. The agents reviewed include Urolithin A, CoQ10, MitoQ, NMN, Creatine, NR, Elamipretide, Mitochondrial-derived peptides, exercise mimetics, and classical doping agents. The agents Urolithin A, MitoQ, NMN, and Creatine had the clearest human and/or athlete related evidence, although most studies are small and short term. CoQ10 and MitoQ may support oxidative stress reduction and recovery biomarkers, but evidence for direct performance enhancement remains limited. Elamipretide and mitochondrial-derived peptides are not yet practical athlete therapies, although they are promising mechanistic and disease based concept. Overall, mitochondrial-targeted therapy is promising for athletic use, but larger and longer term studies are required, especially with long term safety data and responder analysis.