Abstract
BPC-157 (pentadecapeptide BPC-157; sequence: Gly–Glu–Pro–Pro–Pro–Gly–Lys–Pro–Ala–Asp–Asp–Ala–Gly–Leu–Val) is a gastric-derived 15-mer peptide that has attracted preclinical interest for cytoprotective, angiogenic, anti-inflammatory, and tissue-repair activities. Unlike many short peptides, BPC-157 shows remarkable stability in gastric juice and has demonstrated efficacy when given orally in multiple animal models (gastrointestinal injury, colitis, tendon and muscle healing, and others). This paper summarizes its chemistry, evidence for oral activity, mechanisms proposed, pharmacokinetics data, formulation considerations for oral delivery, safety/handling notes, key references (PubMed/PMC) and ten FAQs. All content is framed for research use only. PubChem+2PMC+2
Chemical identity & identifiers
- Name (common): BPC-157 (Body Protection Compound-157; pentadecapeptide BPC-157)
- Amino-acid sequence: Gly-Glu-Pro-Pro-Pro-Gly-Lys-Pro-Ala-Asp-Asp-Ala-Gly-Leu-Val
- Molecular formula / mass (typical listing): C₆₂H₉₈N₁₆O₂₂ (free base approx. MW 1419.5, see supplier specs). PubChem+1
- CAS number (commonly cited): 137525-51-0 (trifluoroacetate salt and other commercial forms are listed under this CAS in supplier databases). MilliporeSigma+1
- PubChem CID: 9941957. PubChem
Historical background & overview
BPC-157 was identified from gastric juice and studied in multiple laboratories (primarily preclinical) for its apparent role in promoting mucosal protection, angiogenesis, and healing of wounds and soft-tissue injuries. Interest in oral dosing stems from early observations that the peptide is remarkably stable in human gastric juice, enabling potential efficacy via the oral route in animal models of gastrointestinal and systemic injury. PMC+1
Evidence for oral efficacy — selected preclinical studies & reviews
- Gastrointestinal protection & colitis: Multiple animal studies and reviews document BPC-157’s protective effects in models of gastric lesions, colitis, and intestinal anastomosis healing when administered orally. Systematic and narrative reviews summarize these findings across models. PMC+1
- Soft-tissue, tendon, and muscle healing: Preclinical models (oral and parenteral dosing) describe accelerated tendon and muscle recovery, angiogenesis at injury sites, and improved functional outcomes. Recent orthopedic medicine reviews highlight increasing interest in BPC-157 for musculoskeletal healing, though clinical trial data are limited. PubMed+1
- Central nervous system & systemic effects: Animal studies and reviews report neuroprotective and systemic cytoprotective effects after oral dosing in some models. PMC
These studies are predominantly preclinical (rodent/animal models) and often utilize multiple routes (oral, intramuscular, subcutaneous, intraperitoneal); however, the oral route has repeatedly produced positive outcomes in peer-reviewed animal studies and is emphasized in several reviews. PMC+1
Mechanisms of action (proposed / evidence-based)
- Angiogenesis and growth-factor modulation: BPC-157 modulates angiogenic signaling (VEGF and others) and can promote vessel formation in injured tissues. PMC
- Cytoprotection and mucosal maintenance: Demonstrated protection of gastric and intestinal mucosa against diverse noxious agents; maintains epithelial integrity and accelerates re-epithelialization. PMC
- Modulation of inflammatory cascades: Reported downregulation of some pro-inflammatory mediators and reduction of leukocyte infiltration in injured tissue models. PMC
- Interaction with NO and other systems: Some literature suggests BPC-157 interacts with nitric oxide signaling and other endogenous protective systems, contributing to its pleiotropic effects. PMC
Pharmacokinetics & oral bioavailability notes
- Stability: BPC-157 has been reported to be stable in human gastric juice for >24 hours, which likely underpins its oral activity in animal models. PMC
- PK after parenteral dosing: Pharmacokinetic studies after IV/IM dosing report short plasma half-life but measurable distribution; absolute bioavailability after IM was estimated in animal studies (note: these values are for parenteral routes; dedicated oral PK in multiple species is less comprehensively characterized). PMC+1
- Oral route — functional bioavailability: Many animal studies demonstrate functional bioavailability (therapeutic effects) after oral dosing, even if detailed human oral PK data are lacking. This functional effect is likely due to gastric stability and local plus systemic absorption in preclinical species. PMC+1
Formulation & delivery considerations for oral use
- Liquid vs. solid oral forms: Preclinical studies have used solutions administered by gavage; oral stability suggests multiple oral formulation options may be feasible.
- Enteric strategies: Although BPC-157 is stable in gastric juice, enteric approaches or mucoadhesive formulations may be considered when targeting distal intestinal segments.
- Dosing frequency: Animal studies use a wide range of doses and schedules; standardized translational human dosing has not been established. Always refer to protocol-specific literature when designing preclinical studies. PMC+1
Safety, regulatory context & limitations
- Preclinical safety: Animal studies frequently report tolerability at experimental doses; however, systematic GLP toxicology packages suitable for regulatory approval are limited in public literature. PMC
- Regulatory status: BPC-157 is not an FDA-approved therapeutic. It appears in research/compendia listings and is sold by research chemical suppliers, but it is also included on lists and warnings by regulatory bodies regarding unapproved peptide products. WADA lists BPC-157 under prohibited substances for sport. PubMed+1
- Cancer/angiogenesis caution: Because BPC-157 promotes angiogenesis in some settings, theoretical concerns exist about effects on tumor growth; the clinical relevance of this risk is not well defined and requires dedicated safety studies. PMC
Practical lab handling & storage (research context)
- Typical supply form: lyophilized peptide (free base or TFA/acetate salts). Suppliers list CAS 137525-51-0 for common preparations. MilliporeSigma+1
- Storage: store lyophilized product as recommended by vendor (often −20 °C, desiccated); reconstitute per protocol and follow short storage life for aqueous solutions.
- Use statement: For research use only — not for human or veterinary use outside of approved clinical trials.
Key references (PubMed / PMC) — selected high-value sources
- Seiwerth S, et al. Stable Gastric Pentadecapeptide BPC 157 and Wound Healing / Tissue Protection. (Review) PMC. 2021. PMC
- Vukojević J, et al. Pentadecapeptide BPC-157 and the central nervous system. Neural Regeneration Research. 2021. (PMC review discussing gastric stability and CNS effects). PMC
- Duzel A, et al. Stable gastric pentadecapeptide BPC 157 in the treatment of soft tissue injury and GI models. (Review / overview). 2017. PMC. PMC
- He L, et al. Pharmacokinetics, distribution, metabolism, and excretion of BPC-157 in rats and dogs. Frontiers in Pharmacology. 2022. (PK parenteral data). PMC+1
- Vasireddi N. Emerging Use of BPC-157 in Orthopaedic Sports Medicine. (Recent review highlighting rising clinical/athlete interest and regulatory notes). PubMed. 2024–2025. PubMed+1
10 Frequently Asked Questions (FAQ)
1. What is “oral BPC-157”?
“Oral BPC-157” refers to administration of the pentadecapeptide by mouth. Preclinical models demonstrate measurable and reproducible therapeutic effects after oral dosing, attributed in part to the peptide’s stability in gastric juice. PMC+1
2. What is the CAS number for BPC-157?
The commonly cited CAS number for commercial BPC-157 preparations (trifluoroacetate salt, etc.) is 137525-51-0. Verify the CAS on the supplier’s Certificate of Analysis for a specific lot. MilliporeSigma+1
3. Is BPC-157 stable when taken orally?
Yes — studies have reported that BPC-157 remains stable in human gastric juice for extended periods (reported >24 hours in vitro), which supports its oral activity in animal models. PMC
4. What kinds of conditions has oral BPC-157 been tested for (preclinically)?
Animal models include gastric and intestinal lesions, colitis/IBD models, anastomosis healing, tendon and muscle injury models, and various systemic injury paradigms. Most data are preclinical. PMC+1
5. How does oral BPC-157 work (mechanistically)?
Proposed mechanisms include promotion of angiogenesis and growth-factor signaling, cytoprotection of mucosal tissues, modulation of inflammatory pathways, and interaction with nitric-oxide signaling — with diverse downstream effects depending on the injury model. PMC+1
6. Are there human clinical trials proving oral efficacy?
Robust, large-scale, peer-reviewed human clinical trials for BPC-157 (oral or other routes) are very limited or absent in public literature. Most evidence remains preclinical. PMC+1
7. What is known about oral pharmacokinetics in humans?
Detailed human oral PK data are sparse. Parenteral PK in animals has been characterized; functional oral efficacy has been demonstrated in animals but translational human PK/PD studies are needed. PMC+1
8. Is oral BPC-157 safe?
In preclinical models it is frequently well tolerated at experimental doses, but formal human toxicology and long-term safety data are limited. Because BPC-157 affects angiogenesis, theoretical safety issues (e.g., tumor-related angiogenesis) warrant careful evaluation. PMC
9. Is BPC-157 legal and regulated?
BPC-157 is not an FDA-approved medicine. It is sold by some research suppliers for laboratory use. Regulatory posture varies by jurisdiction, and WADA classifies it as prohibited in sport. Clinical use outside approved trials is not recommended. PubMed+1
10. How should research labs handle and store BPC-157?
Follow supplier SDS/CoA guidance. Typical practice: store lyophilized peptide desiccated at −20 °C, reconstitute just prior to use, and handle using standard lab PPE. Use only in institutional, approved research settings. MilliporeSigma+1
Conclusions & research gaps
Oral BPC-157 is a compelling preclinical candidate because of its gastric stability and repeated demonstration of therapeutic effects in animal models after oral dosing. However, significant gaps remain: standardized human PK/PD for oral administration, comprehensive GLP toxicology, and well-designed randomized clinical trials to evaluate safety and efficacy in humans. Until such data exist, use should remain confined to controlled research settings. PMC+1
