Emerging Use of BPC-157 in Orthopaedic Sports Medicine: A Systematic Review

This systematic review conducted by the Case Western Reserve University group critically evaluated the state of evidence on BPC-157 (Body Protection Compound-157) in orthopaedic sports medicine, a context in which the peptide has gained popularity among athletes despite lacking regulatory approval. 36 studies published between 1993 and 2024 were analyzed, of which 35 were preclinical and only 1 was clinical (retrospective, in humans).

The mechanisms identified as the basis for BPC-157's therapeutic effects include:

• VEGFR2 pathway activation and nitric oxide synthesis via Akt-eNOS, promoting angiogenesis
• ERK1/2 signaling, facilitating cell proliferation and endothelial repair
• Increased growth hormone receptor expression in fibroblasts
• Reduction of inflammatory cytokines and modulation of the healing response
• Neuromuscular stabilization and protection against demyelination

In preclinical models, BPC-157 demonstrated beneficial effects on muscle, tendon, ligament, and bone injuries, with accelerated healing and better organization of repaired tissue. A single retrospective human clinical study (n=12 with chronic knee pain) reported sustained relief over >6 months following injection, but with significant methodological limitations. BPC-157's plasma half-life is less than 30 minutes, with hepatic metabolism and apparently benign safety profile in animal models.

The authors concluded that despite the robust preclinical base, "no clinical safety data were found in humans" and BPC-157 should be considered investigational. The review warns about use outside clinical trials and emphasizes the need for randomized human trials before incorporation into medical practice. The article also recalls that BPC-157 is classified by WADA as a prohibited substance (S0), requiring caution with competitive athletes.