Review
This narrative review examines the pharmacological mechanisms, safety profiles, and regulatory status of twelve peptides commonly marketed in sports medicine contexts, spanning both FDA-approved compounds (e.g., tesamorelin/Egrifta) and unapproved "gray market" substances (e.g., BPC-157, CJC-1295, TB-500, ipamorelin, and others). The authors note that while many unapproved peptides show promising tissue repair and metabolic effects in animal models, rigorous human safety and efficacy data are largely absent. The review highlights a growing direct-to-consumer gray market operating outside regulatory oversight and discusses the potential for serious patient harm. Notably, the authors address the placebo effect as a possible mediator of perceived peptide efficacy and examine how social media may amplify this effect. A clinician-oriented framework is proposed to guide evidence-based patient discussions about peptide use for musculoskeletal healing and athletic performance, including consideration of alternative treatments. Key limitations include the narrative (non-systematic) review methodology and the inherently limited and heterogeneous evidence base for most compounds discussed, particularly in human populations.
Sports medicine (Auckland, N.Z.) · Apr 2026DOI ↗ ReviewPreprint
This narrative review examines the pharmacological mechanisms, safety profiles, and regulatory status of twelve peptides commonly encountered in sports medicine and athletic performance contexts, including both approved agents (e.g., tesamorelin/Egrifta, sermorelin) and unapproved "gray market" compounds (e.g., BPC-157, CJC-1295, TB-500, ipamorelin, AOD-9604, FS-344, GHK-Cu, MOTS-C, SS-31, and thymosin beta-4). The authors note that while many unapproved peptides show promising tissue repair and metabolic outcomes in animal models, rigorous human safety and efficacy data remain scarce. The review highlights the emergence of a direct-to-consumer gray market operating outside regulatory oversight and the potential for serious patient harm. It further discusses the placebo effect as a potential mediator of perceived peptide efficacy, and how social media may amplify this effect. The authors provide a clinical framework to guide patient-provider discussions and promote evidence-based practice for musculoskeletal healing. Key limitations include the narrative (non-systematic) review design, reliance on preclinical literature for most unapproved compounds, and the absence of head-to-head human trials for the majority of agents discussed.
Unknown journal · Apr 2026DOI ↗ Review
This narrative review examines the potential role of therapeutic peptides in orthopaedic care, synthesizing preclinical and mechanistic literature across several peptide classes. The authors categorize peptides by their primary proposed function: wound-healing agents (BPC-157, TB-500, GHK-Cu), growth hormone secretagogues (ipamorelin, CJC-1295, tesamorelin, sermorelin, AOD-9604), recovery-enhancing peptides (epithalon, delta sleep-inducing peptide, pinealon), and neuroactive peptides (selank, semax, dihexa). The review describes how these compounds are theorized to interact with signaling pathways—including PI3K/Akt, mTOR, MAPK, TGF-β, and AMPK—to promote tissue regeneration, resolve inflammation, and support neuromuscular recovery. The authors acknowledge that, while preclinical evidence is promising, robust human clinical trial data are largely absent, representing a significant gap in the literature. Limitations include the review's reliance on animal and in vitro studies, the absence of a systematic search methodology, and the lack of direct clinical evidence supporting efficacy or safety in human orthopaedic populations. The authors call for future controlled trials to validate these mechanistic findings in clinical settings.
Journal of the American Academy of Orthopaedic Surgeons. Global research & reviews · Jan 2026DOI ↗ ReviewPreprint
This review paper examines the pharmacological mechanisms, safety profiles, and regulatory status of both approved and unapproved peptide therapies relevant to sports medicine, musculoskeletal injury recovery, and athletic performance enhancement. The compounds reviewed span a wide spectrum — from FDA-approved agents such as tesamorelin and sermorelin, to gray-market compounds including BPC-157, TB-500, CJC-1295, Ipamorelin, AOD-9604, FS-344, GHK-Cu, MOTS-C, and SS-31. The authors note that while many unapproved peptides show promising results in preclinical and animal models — including favorable tissue repair and metabolic effects — rigorous human safety and efficacy data remain scarce. The review highlights a growing direct-to-consumer gray market operating outside regulatory oversight and discusses how social media may amplify perceived benefits through placebo-related mechanisms. The paper also offers a clinical framework to guide patient conversations and support evidence-based decision-making. Key limitations include the inherent constraints of a narrative review design, reliance on heterogeneous preclinical data for unapproved compounds, and the absence of controlled human trials for most of the highlighted peptides.
Unknown journal · Dec 2025DOI ↗ Review
This review paper surveys the current landscape of analytical methods used in sports anti-doping laboratories to detect peptide-based drugs, drug candidates, and their analogs in biological specimens such as blood, serum, and urine. The authors describe the broad range of peptidic compounds subject to anti-doping scrutiny, spanning low-molecular-mass peptides (e.g., growth hormone-releasing peptides, ARA-290, TB-500, AOD-9604, CJC-1295, desmopressin) to intermediate-mass proteins (e.g., insulins, IGF-1, growth hormone, erythropoietin) and higher-molecular-mass biologics (e.g., stamulumab). The review outlines detection approaches including chromatographic-mass spectrometric, electrophoretic, immunological, and combined methodologies, emphasizing the challenge of proving exogenous origin at very low concentrations in limited sample volumes. A central finding is that a meaningful gap remains between what is technically achievable in detection and what is routinely practiced in day-to-day analytical workflows. Limitations of this paper include its nature as a narrative review rather than an original experimental study, meaning it synthesizes existing literature without generating new empirical data. It does not evaluate clinical outcomes or therapeutic efficacy of any compound discussed.
Expert review of proteomics · Nov 2014DOI ↗ Review
This review summarizes five years of published literature on the analytical detection of emerging and non-approved performance-enhancing substances in the context of sports anti-doping controls. The authors examine a broad range of compounds classified as doping agents by the World Anti-Doping Agency (WADA), spanning both peptidic substances—such as modified insulin-like growth factor-1 (IGF-1), TB-500 (thymosin beta-4 fragment), peginesatide/hematide, growth hormone releasing peptides, and AOD-9604—and non-peptidic substances, including selective androgen receptor modulators (SARMs), hypoxia-inducible factor (HIF) stabilizers, siRNA, S-107, and aladorian (ARM036). Inorganic substances such as cobalt are also discussed. The review focuses specifically on the analytical challenges posed by these compounds, including their physicochemical properties, low concentrations in biological matrices (blood and urine), metabolic transformation, and suitability for chromatographic–mass spectrometric or alternative detection methods. The study does not present original experimental data or human clinical outcomes, but rather synthesizes existing literature to guide development of detection strategies. A key limitation is that, as a review, it does not independently validate any analytical method and reflects the state of the field only up to its publication date.
Journal of pharmaceutical and biomedical analysis · May 2014DOI ↗