BPC-157

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BPC-157
BPC-157.svg
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
DrugBank
PubChem CID
UNII
  • InChI=1S/C62H98N16O22/c1-31(2)25-37(55(92)74-50(32(3)4)62(99)100)71-46(81)29-65-51(88)33(5)67-53(90)38(26-48(84)85)73-54(91)39(27-49(86)87)72-52(89)34(6)68-57(94)41-15-10-21-75(41)58(95)35(13-7-8-20-63)70-45(80)30-66-56(93)40-14-9-22-76(40)60(97)43-17-12-24-78(43)61(98)42-16-11-23-77(42)59(96)36(18-19-47(82)83)69-44(79)28-64/h31-43,50H,7-30,63-64H2,1-6H3,(H,65,88)(H,66,93)(H,67,90)(H,68,94)(H,69,79)(H,70,80)(H,71,81)(H,72,89)(H,73,91)(H,74,92)(H,82,83)(H,84,85)(H,86,87)(H,99,100)/t33-,34-,35-,36-,37-,38-,39-,40-,41-,42-,43-,50-/m0/s1
    Key: HEEWEZGQMLZMFE-RKGINYAYSA-N
  • C[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]3CCCN3C(=O)[C@@H]4CCCN4C(=O)[C@H](CCC(=O)O)NC(=O)CN
Properties
C62H98N16O22
Molar mass 1419.556 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Gastric Pentadecapeptide BPC-157 (also known as Body Protection Compound 157, bepecin, or PL 14736) is a synthetic fifteen amino acid oligopeptide derived from a protein found in human gastric juice. BPC-157 has been studied primarily in laboratory animals for its potential healing properties. Research suggests it may help repair damaged tissues by promoting new blood vessel growth and activating various cellular repair pathways. In animal studies, the compound has shown promise for healing injuries to tendons, ligaments, muscles, and bones, as well as protecting organs and blood vessels from damage. It may also have neuroprotective effects on the brain and nervous system. Despite these findings in preclinical research, BPC-157 is not approved by any drug regulatory agency for human use, and there is limited data regarding it effectiveness on humans, although it has been used for many years. The peptide has gained popularity among athletes and the general public for injury recovery, leading the World Anti-Doping Agency to ban it in 2022. Health authorities discourage its use due to insufficient human safety data, and some jurisdictions have restricted it as a prescription-only medicine despite it not being available through legitimate prescriptions. Additionally, because the compound promotes blood vessel formation (angiogenesis), there are theoretical concerns about potential cancer promotion that require further investigation.

The peptide was discovered during research on human gastric juice​. [1] The amino acid sequence is Gly-Glu-Pro-Pro-Pro-Gly-Lys-Pro-Ala-Asp-Asp-Ala-Gly-Leu-Val. [2] BPC-157 is stable at room temperature and bioavailable in rodent models when administered IM or IV​. [3] The peptide demonstrates remarkable stability in human gastric juice, remaining intact for more than 24 hours, which supports its therapeutic effectiveness when administered orally​. [4]

Pharmacology

Mechanism of Action

BPC-157 works through several interconnected biological pathways that promote healing and tissue repair. To understand how it functions, it is helpful to think of the peptide as a chemical messenger that activates various repair mechanisms in the body.

Blood Vessel Formation and Repair

The primary way BPC-157 promotes healing is by activating the VEGF receptor 2 (VEGFR2) pathway​. [5] VEGF (Vascular Endothelial Growth Factor) is a protein that signals the body to create new blood vessels—a process called angiogenesis. Blood vessels function as the transportation network that delivers oxygen, nutrients, and repair materials to damaged tissues. Without adequate blood supply, injured tissues cannot heal properly.

When BPC-157 binds to VEGFR2 receptors on the surface of endothelial cells (the cells that line blood vessels), it triggers a cascade of events. The receptor becomes phosphorylated—meaning phosphate molecules attach to it, activating it like flipping a switch. This activation then triggers the Akt-eNOS pathway, which increases production of nitric oxide (NO) in the blood vessel walls​. [6] Nitric oxide causes blood vessels to dilate (widen), improving blood flow to injured areas and allowing more oxygen and healing nutrients to reach damaged tissues.

Cellular Signaling and Repair Pathways

BPC-157 activates several other molecular pathways that work together to promote tissue repair​. [7]

Focal adhesion kinase (FAK)-paxillin complexes are activated, which help cells migrate and attach to surfaces. This is crucial for wound healing because cells need to move into damaged areas and anchor themselves to begin rebuilding tissue. The peptide stimulates JAK-2 (Janus kinase 2), a protein that relays signals from outside the cell to the nucleus where genes are activated. This signaling pathway is involved in cell survival, growth, and immune responses—all essential for healing.

Early Growth Response gene 1 (Egr-1) is also activated. This gene acts like a master switch that turns on many other genes involved in cell growth, survival, and blood vessel formation. When Egr-1 is upregulated, it signals cells to grow and repair. The extracellular signal-regulated kinases (ERK1/2) pathway becomes activated as well. This pathway controls cell division and survival. When tissues are damaged, new cells must divide to replace dead or injured ones, and ERK1/2 activation promotes this cell multiplication.

Gene Expression Changes

BPC-157 changes which genes are expressed in cells, particularly in brain tissue after injury​. [8] When genes are upregulated (increased), specific biological effects occur:

Vegfr2 upregulation produces more VEGF receptors, making cells more sensitive to growth signals and better able to form new blood vessels. Nos3 and Nos1 genes produce enzymes that make nitric oxide, which dilates blood vessels and improves blood flow. Akt1 promotes cell survival and prevents damaged cells from dying prematurely, giving them time to repair. Src helps cells communicate with each other and respond to growth signals. Kras is involved in cell growth and division—essential for replacing damaged cells. Foxo and Srf are transcription factors that regulate many genes involved in stress resistance, metabolism, and cell survival.

BPC-157 downregulates (decreases) certain genes that can be harmful during healing. Nos2 produces large amounts of nitric oxide during inflammation, which can damage tissues if overproduced. By reducing Nos2, BPC-157 may help control excessive inflammation. Nfkb (Nuclear Factor kappa B) is a major inflammation-promoting factor. While some inflammation is necessary for healing, excessive amounts can cause additional tissue damage. By downregulating Nfkb, BPC-157 may reduce harmful inflammatory responses.

Endothelial Function

BPC-157 modulates Src and caveolin-1 (Cav-1) phosphorylation​. [6] Caveolin-1 is a protein found in small pockets (caveolae) on the cell membrane. When BPC-157 affects these proteins, it changes how VEGFR2 receptors are internalized into cells and how endothelial nitric oxide synthase (eNOS) is activated. The result is sustained production of nitric oxide, which keeps blood vessels dilated and ensures continuous blood flow to healing tissues.

Overall Effect

These mechanisms work together to create an optimal environment for tissue repair. BPC-157 increases blood flow to damaged areas, promotes new blood vessel formation, encourages cell survival and growth, facilitates cell migration to injury sites, and balances inflammatory responses to prevent excessive tissue damage while still allowing necessary healing inflammation.

Dosage and Administration

In research settings, typical dosages of BPC-157 range from 200 to 500 micrograms (mcg) daily. Preclinical studies commonly employ doses of 10 micrograms per kilogram (μg/kg) or 10 nanograms per kilogram (ng/kg) body weight administered once or twice daily. The peptide can be administered through various routes including intraperitoneal injection, subcutaneous injection, intramuscular injection, intravenous infusion, or oral administration. [3] The half-life following intramuscular or intravenous administration is less than 30 minutes, indicating rapid clearance from circulation. [3]

A 2025 pilot study in humans evaluated intravenous infusion of BPC-157 at doses of 10 mg and 20 mg in two adults, demonstrating no adverse effects on cardiac, hepatic, renal, thyroid, or glucose biomarkers, with the peptide being well-tolerated​. [9]

Research

Pre-clinical research has indicated that BPC-157 may have cytoprotective, neuroprotective, and anti-inflammatory effects, and may also accelerate tissue and organ healing​. [8] [10] [11] [4] [12] [13]

Vascular and Organ Protection

Research has demonstrated that BPC-157 can counteract vessel occlusion syndromes by rapidly activating collateral blood vessel pathways, effectively bypassing occluded or damaged vessels​. [14] Studies in rat models have shown effectiveness in treating complications from occlusion of major vessels including the superior mesenteric artery and vein, as well as therapeutic effects in models of glaucoma induced by episcleral vein cauterization​. [15]

Musculoskeletal and Neurological Applications

BPC-157 has demonstrated beneficial effects in various musculoskeletal injury models, including tendon ruptures, ligament tears, muscle detachment, and bone healing​. [16] The peptide has shown neuroprotective properties in models of traumatic brain injury, spinal cord compression, and peripheral nerve transection​. [17] Animal studies have documented effects on neurotransmitter systems, particularly serotonergic and dopaminergic pathways​. [7]

This substance is sometimes used in functional medicine despite not being approved by any drug regulatory agency​. [7] The compound promotes angiogenesis and as a result has some concerns over cancer promotion. [18]

As of 2022, the peptide has been banned by the World Anti-Doping Agency under the S0 category of non-exempt substances. [19] [20]

BPC-157 has been widely used both by athletes and among the general public, mainly for recovery from injury or stimulating healing in chronic conditions, [21] [22] [16] [23] but there is as yet only very limited human trial data on efficacy and only a few preliminary safety studies​, [24] [25] [26] so use of BPC-157 is discouraged by health authorities and it has been controlled as a prescription medicine in several jurisdictions such as New Zealand and Australia, despite not actually being available for prescription. [27] [28]

Detection

BPC-157 is detected in urine using a weak cation exchange solid phase extraction and was found to be stable in urine for 4 days. [29]

See also

References

  1. ↑ Chang CH, Tsai WC, Lin MS, Hsu YH, Pang JH (2011). "The promoting effect of pentadecapeptide BPC 157 on tendon healing involves tendon outgrowth, cell survival, and cell migration". Journal of Applied Physiology. 110 (3). American Physiological Society: 774–780. doi:10.1152/japplphysiol.00945.2010. ISSN   8750-7587. PMID   21030672.
  2. ↑ Jelovac N, Sikiric P, Rucman R, Petek M, Marovic A, Perovic D, et al. (August 1999). "Pentadecapeptide BPC 157 attenuates disturbances induced by neuroleptics: the effect on catalepsy and gastric ulcers in mice and rats". European Journal of Pharmacology. 379 (1): 19–31. doi:10.1016/S0014-2999(99)00486-0. PMID   10499368.
  3. 1 2 3 He L, Feng D, Guo H, Zhou Y, Li Z, Zhang K, et al. (2022-12-14). "Pharmacokinetics, distribution, metabolism, and excretion of body-protective compound 157, a potential drug for treating various wounds, in rats and dogs". Frontiers in Pharmacology. 13 1026182. Frontiers Media SA. doi: 10.3389/fphar.2022.1026182 . ISSN   1663-9812. PMC   9794587 . PMID   36588717.
  4. 1 2 Sikiric P, Seiwerth S, Rucman R, Turkovic B, Rokotov DS, Brcic L, et al. (2011). "Stable gastric pentadecapeptide BPC 157: novel therapy in gastrointestinal tract". Current Pharmaceutical Design. 17 (16): 1612–32. doi:10.2174/138161211796196954. PMID   21548867.
  5. ↑ Hsieh MJ, Liu HT, Wang CN, Huang HY, Lin Y, Ko YS, et al. (March 2017). "Therapeutic potential of pro-angiogenic BPC157 is associated with VEGFR2 activation and up-regulation". Journal of Molecular Medicine. 95 (3): 323–333. doi:10.1007/s00109-016-1488-y. PMID   27847966.
  6. 1 2 Hsieh MJ, Lee CH, Chueh HY, Chang GJ, Huang HY, Lin Y, et al. (October 2020). "Modulatory effects of BPC 157 on vasomotor tone and the Src-Cav-1-eNOS signaling pathway in rats". Scientific Reports. 10 (1): 17078. doi:10.1038/s41598-020-74022-y. PMC   7555539 . PMID   33046803.
  7. 1 2 3 Sikiric P, Seiwerth S, Rucman R, Kolenc D, Vuletic LB, Drmic D, et al. (2016). "Brain-gut Axis and Pentadecapeptide BPC 157: Theoretical and Practical Implications". Current Neuropharmacology. 14 (8): 857–865. doi:10.2174/1570159x13666160502153022. PMC   5333585 . PMID   27138887.
  8. 1 2 Vukojevic J, Milavić M, Perović D, Ilić S, Čilić AZ, Đuran N, et al. (March 2022). "Pentadecapeptide BPC 157 and the central nervous system". Neural Regeneration Research. 17 (3): 482–487. doi: 10.4103/1673-5374.320969 . PMC   8504390 . PMID   34380875.
  9. ↑ Lee E, Walker C, Ayadi B (September 2025). "Safety of Intravenous Infusion of BPC157 in Humans: A Pilot Study". Alternative Therapies in Health and Medicine. PMID   40131143.
  10. ↑ Chang C, Tsai W, Lin M, Hsu Y, Pang JS (October 28, 2010). "The promoting effect of pentadecapeptide BPC 157 on tendon healing involves tendon outgrowth, cell survival, and cell migration" . Journal of Applied Physiology. 110 (3): 774–780. doi:10.1152/japplphysiol.00945.2010. PMID   21030672.
  11. ↑ Staresinic M, Sebecic B, Patrlj L, Jadrijevic S, Suknaic S, Perovic D, et al. (2003). "Gastric pentadecapeptide BPC 157 accelerates healing of transected rat Achilles tendon and in vitro stimulates tendocytes growth" . Journal of Orthopaedic Research. 21 (6): 976–983. doi:10.1016/S0736-0266(03)00110-4. PMID   14554208.
  12. ↑ Sikiric P, Seiwerth S, Brcic L, Blagaic AB, Zoricic I, Sever M, et al. (December 2006). "Stable gastric pentadecapeptide BPC 157 in trials for inflammatory bowel disease (PL-10, PLD-116, PL 14736, Pliva, Croatia). Full and distended stomach, and vascular response". Inflammopharmacology. 14 (5–6): 214–221. doi:10.1007/s10787-006-1531-7. PMID   17186181. S2CID   24132425.
  13. ↑ Cerovecki T, Bojanic I, Brcic L, Radic B, Vukoja I, Seiwerth S, et al. (September 2010). "Pentadecapeptide BPC 157 (PL 14736) improves ligament healing in the rat". Journal of Orthopaedic Research. 28 (9): 1155–1161. doi:10.1002/jor.21107. PMID   20225319. S2CID   22085833.
  14. ↑ Sikiric P, Seiwerth S, Blagaic AB, Batelja Vuletic L, Stupnisek M, Skrtic A, et al. (January 2022). "Cytoprotective gastric pentadecapeptide BPC 157 resolves major vessel occlusion disturbances, ischemia-reperfusion injury following Pringle maneuver, and Budd-Chiari syndrome". World Journal of Gastroenterology. 28 (1): 23–46. doi: 10.3748/wjg.v28.i1.23 . PMC   8793015 . PMID   35139112.
  15. ↑ Sikiric P, Drmic D, Stupnisek M, Kokot A, Vukojevic J, Zlatar M, et al. (December 2021). "Stable Gastric Pentadecapeptide BPC 157 Therapy of Rat Glaucoma". Biomedicines. 10 (1): 89. doi: 10.3390/biomedicines10010089 . PMC   8773185 . PMID   35010781.
  16. 1 2 Vasireddi N, Hahamyan H, Salata MJ, Karns M, Calcei JG, Voos JE, et al. (2025). "Emerging Use of BPC-157 in Orthopaedic Sports Medicine: A Systematic Review". HSS Journal 15563316251355551. doi:10.1177/15563316251355551. PMC   12313605 . PMID   40756949.
  17. ↑ Sikiric P, Skrtic A, Gojkovic S, Krezic I, Zoric L, Radic B, et al. (July 2019). "Stable gastric pentadecapeptide BPC 157 can improve the healing course of spinal cord injury and lead to functional recovery in rats". Journal of Orthopaedic Surgery and Research. 14 (1): 199. doi: 10.1186/s13018-019-1242-6 . PMC   6604284 . PMID   31355337.
  18. ↑ Sehgal P, Gupta R, Choudhary K, Singh R (2025). "BPC 157: A Promising Candidate for Cytoprotection and Tissue Repair". Pharmaceuticals. 18 (2). MDPI: 185. doi: 10.3390/ph18020185 . ISSN   1424-8247. PMC   11859134 . PMID   40005999.
  19. ↑ "2022 Prohibited List: SUBSTANCES AND METHODS PROHIBITED AT ALL TIMES (IN- AND OUT-OF-COMPETITION)" (PDF). World Anti-Doping Agency. WADA. Retrieved 21 February 2022.
  20. ↑ "WORLD ANTI-DOPING CODE INTERNATIONAL STANDARD PROHIBITED LIST 2025" (PDF). World Anti-Doping Agency. WADA. Retrieved 17 November 2025.
  21. ↑ Defoor MT, Dekker TJ (2025). "Injectable Therapeutic Peptides—An Adjunct to Regenerative Medicine and Sports Performance?". Arthroscopy. 41 (2): 150–152. doi:10.1016/j.arthro.2024.09.005. PMID   39265666.
  22. ↑ Józwiak M, Bauer M, Kamysz W, Kleczkowska P (2025). "Multifunctionality and Possible Medical Application of the BPC 157 Peptide—Literature and Patent Review". Pharmaceuticals. 18 (2): 185. doi: 10.3390/ph18020185 . PMC   11859134 . PMID   40005999.
  23. ↑ McGuire FP, Martinez R, Lenz A, Skinner L, Cushman DM (2025). "Regeneration or Risk? A Narrative Review of BPC-157 for Musculoskeletal Healing". Current Reviews in Musculoskeletal Medicine. 18 (12): 611–619. doi:10.1007/s12178-025-09990-7. PMC   12446177 . PMID   40789979.
  24. ↑ Xu C, Sun L, Ren F, Huang P, Tian Z, Cui J, et al. (2020). "Preclinical safety evaluation of body protective compound-157, a potential drug for treating various wounds". Regulatory Toxicology and Pharmacology. 114 104665. doi:10.1016/j.yrtph.2020.104665. PMID   32334036.
  25. ↑ Lee E, Padgett B (2021). "Intra-Articular Injection of BPC 157 for Multiple Types of Knee Pain". Alternative Therapies in Health and Medicine. 27 (4): 8–13. PMID   34324435.
  26. ↑ Lee E, Walker C, Ayadi B (2024). "Effect of BPC-157 on Symptoms in Patients with Interstitial Cystitis: A Pilot Study". Alternative Therapies in Health and Medicine. 30 (10): 12–17. PMID   39325560.
  27. ↑ Notice of interim decisions to amend (or not amend) the current Poisons Standard. Therapeutic Goods Administration, 3 April 2024
  28. ↑ Classification of Unscheduled Peptides. Submission to the Medicines Classification Committee. Medsafe, June 2025
  29. ↑ Cox HD, Miller GD, Eichner D (2017). "Detection and in vitro metabolism of the confiscated peptides BPC 157 and MGF R23H". Drug Testing and Analysis. 9 (10): 1490–1498. doi:10.1002/dta.2152. ISSN   1942-7603. PMID   28035768.
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