"THE GREY ZONE" OF PHARMACOLOGY: A REVIEW OF PEPTIDE BIOREGULATORS FOR POST-SPORTS INJURY RECOVERY (BPC-157, TB-500)
DOI:
https://doi.org/10.31891/pcs.2025.4.2Keywords:
peptide bioregulators, BPC-157, TB-500, Thymosin Beta-4, sports injury, regeneration, tendon healing, , WADA, pre-clinical studiesAbstract
The management of musculoskeletal injuries, particularly tendinopathies and ligament damage, remains a significant challenge in sports medicine. This is primarily due to the limited vascularization and low endogenous regenerative potential of connective tissue. The low efficacy of traditional therapeutic methods (NSAIDs, physiotherapy) in accelerating biological healing stimulates athletes and medical staff to search for alternative pharmacological agents. This has led to the emergence of a "grey zone" market - unregulated substances sold under the "research chemicals only" label. The most popular substances in this niche are the peptide bioregulators BPC-157 and TB-500. Their widespread anecdotal use starkly contrasts with their official status: both substances are banned by the World Anti-Doping Agency (WADA) and included in the Prohibited List under Class S0 "Unapproved Substances," as they lack approval for human therapeutic use.
Objective. To conduct a systematic analysis and critical review of the available pre-clinical (in vitro, animal) and clinical scientific literature regarding the biochemical basis, pharmacological mechanisms of action, evidence base for therapeutic potential, and safety risks associated with the use of BPC-157 and TB-500 for post-injury recovery.
Results. The analysis reveals a fundamental chasm between pre-clinical data and clinical reality. BPC-157 (a pentadecapeptide, a stable fragment of human gastric protein) demonstrates potent regenerative properties in numerous animal models (notably, rat Achilles tendon transection models). Its primary mechanism is linked to stimulating angiogenesis (via the VEGF pathway) and enhancing fibroblast migration (via FAK-Paxillin signaling modulation). However, at the time of this review, no published peer-reviewed randomized controlled trials (RCTs) in humans exist that confirm its efficacy and safety for treating musculoskeletal injuries. TB-500 is the synthetic version of Thymosin Beta-4 (TB4), a natural peptide that is a key regulator of actin polymerization in the cytoskeleton. Its mechanism of action is more fundamental, involving the stimulation of cell migration (fibroblasts, endothelial cells), inflammation modulation, and anti-fibrotic effects. While TB4 has undergone some clinical trials in other fields (e.g., chronic wound healing), its efficacy in sports injuries is unproven. Moreover, its ability to stimulate cell migration and angiogenesis carries theoretical oncogenic risks (potential stimulation of undiagnosed tumors). Both peptides are distributed via the "grey market," posing additional risks of bacterial contamination (endotoxins), impurities, and incorrect dosages.
Conclusion. The available data confirm that the use of BPC-157 and TB-500 for treating sports injuries in humans is currently a form of unregulated self-experimentation. A critical gap exists between promising pre-clinical data and the complete absence of an evidence base for their efficacy and safety in humans. There is an urgent need for high-quality, well-designed RCTs to move these substances out of the dangerous "grey zone" and either into the arsenal of evidence-based medicine or into the category of scientifically unfounded agents.
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