BPC-157: Safety Profile & Research Summary
Preclinical Research Summary
Key Preclinical Studies
| Study | Model | Key Findings | Ref |
|---|---|---|---|
| He et al. (2022) | SD rats / Beagle dogs | PK study: IV t½ = 15.2 min (rats), 5.27 min (dogs); bioavailability 14-19% (rats IM), 45-51% (dogs IM); distributed to kidney, liver, stomach | [26] |
| Xu et al. (2020) | Mice, rats, rabbits, dogs | Multi-species toxicity: no LD1 achieved, no adverse signs at 20 mg/kg (rats) or 10 mg/kg (dogs) | [9] |
| Staresinic et al. (2003) | Rats — Achilles transection | 10 µg/kg IP: improved AFI scores, increased load-to-failure at 14-72 days; reversed corticosteroid impairment | [17] |
| Tudor et al. (2010) | Mice — TBI | 10 µg/kg IP: reduced brain edema, hemorrhage, and mortality; improved conscious/unconscious/death ratio | [19] |
| Perovic et al. (2019) | Rats — spinal cord | 200 µg/kg IP: axonal recovery maintained to 1 year; counteracted necrosis, demyelination, cyst formation | [20] |
| Vukojevic et al. (2020) | Rats — bilateral carotid occlusion | Upregulated Egr1/Akt1/Src/Vegfr2/Nos3; downregulated Nos2/Nfkb in hippocampus | [14] |
| Hsieh et al. (2017/2020) | Rat hind limb ischemia + CAM | 129–152% increased angiogenesis; VEGFR2-Akt-eNOS pathway confirmed | [7] |
| Sever et al. (2019) | Rats — bile duct ligation | Reversed liver fibrosis, cirrhosis, and portal hypertension; normalized enzymes/bilirubin | [23] |
| Matek et al. (2025) | Rats — quadriceps detachment | Oral BPC-157 in drinking water: full muscle-to-bone reattachment at 90 days; annihilated leg contracture | [18] |
| Chang et al. (2011/2014) | Rat tendon fibroblasts (in vitro) | ↑ GHR expression, activated FAK-paxillin pathway, enhanced cell survival and migration | [12][13] |
Clinical / Human Studies
| Study | Design | n= | Key Outcome | Ref |
|---|---|---|---|---|
| Phase II Ulcerative Colitis | Multicenter RCT, double-blind, placebo-controlled | 53 | 80 mg enema daily × 2 wks: significant DAI decrease vs placebo; very well-tolerated, no AEs vs placebo | [6] |
| Phase I PK/Safety | Single-blind, placebo-controlled | 32 | Rectal 0.25-2 mg/kg: very low systemic absorption; well-tolerated, no safety differences vs placebo | [27] |
| Knee Pain Retrospective | Chart review | 16 | 2 mg intra-articular: 91.6% significant improvement lasting 6 months–1 year; no adverse effects | [24] |
| Interstitial Cystitis Pilot | Pilot study | 12 | 10 mg intravesical: 83.3% complete resolution, remaining 2 subjects reported 80% improvement; no AEs | [25] |
| IV Safety Pilot | Pilot study | 2 | 10-20 mg IV: no adverse effects on cardiac, hepatic, renal, or thyroid biomarkers | [28] |
Pharmacokinetic Parameters
| Parameter | Value | Ref |
|---|---|---|
| IV Half-life (rats) | 15.2 minutes | [26] |
| IV Half-life (dogs) | 5.27 minutes | [26] |
| Bioavailability IM (rats) | 14–19% | [26] |
| Bioavailability IM (dogs) | 45–51% | [26] |
| Tmax (rats) | ~3 minutes | [26] |
| Major Metabolite | Proline (amino acid) | [26] |
| Gastric Stability | >24 hours in human gastric juice | [3] |
| Urine Detection | 4–5 days via LC-MS | [26] |
| Lethal Dose | Not achieved (>2 g/kg IV/IG in mice) | [9] |
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“Preclinical Research Summary Key Preclinical Studies StudyModelKey FindingsRef He et al.”
References
- Sikiric P, et al. A new gastric juice peptide, BPC. An overview of the stomach-stress-organoprotection hypothesis and beneficial effects of BPC. Journal of Physiology-Paris. 1993;87(5):313-327.
- Sikiric P, et al. Brain-gut Axis and Pentadecapeptide BPC 157: Theoretical and Practical Implications. Current Neuropharmacology. 2016;14(8):857-865.
- Sikiric P, Hahm KB, Blagaic AB, Tvrdeic A, et al. Stable Gastric Pentadecapeptide BPC 157, Robert's Stomach Cytoprotection/Adaptive Cytoprotection/Organoprotection, and Selye's Stress Coping Response: Progress, Achievements, and the Future. Gut and Liver. 2020;14(2):153-167.
- U.S. Food and Drug Administration. Certain Bulk Drug Substances for Use in Compounding that May Present Significant Safety Risks. FDA.gov. Updated 2023.
- World Anti-Doping Agency. The 2025 Prohibited List. WADA. January 1, 2025.
- Ruenzi M, et al. BPC-157 in patients with ulcerative colitis: A Phase II multicenter, randomized, double-blind, placebo-controlled study. Gastroenterology. 2005;128(Suppl 2):A-585.
- Hsieh MJ, et al. Therapeutic potential of pro-angiogenic BPC157 is associated with VEGFR2 activation and up-regulation. Journal of Molecular Medicine. 2017;95(3):323-333.
- Sikiric P, et al. Stable Gastric Pentadecapeptide BPC 157 as a Therapy and Safety Key: A Special Beneficial Pleiotropic Effect Controlling and Modulating Angiogenesis and the NO-System. Pharmaceuticals (Basel). 2025;18(6):928.
- Xu C, et al. Preclinical safety evaluation of body protection compound-157, a potential drug for treating various wounds. Regulatory Toxicology and Pharmacology. 2020;114:104665.
- Chang CH, Tsai WC, Hsu YH, Pang JS. Pentadecapeptide BPC 157 enhances the growth hormone receptor expression in tendon fibroblasts. Molecules. 2014;19(11):19066-19077.
- Schlosser SK. BPC-157 Binding to SH3 Domains and Activation of Src Family Kinases: In Silico Modeling and Fluorescent Fusion Protein Production. Research Square. 2025. Preprint, not peer-reviewed.
- Chang CH, et al. The promoting effect of pentadecapeptide BPC 157 on tendon healing involves tendon outgrowth, cell survival, and cell migration. Journal of Applied Physiology. 2011;110(3):774-780.
- Chang CH, et al. Pentadecapeptide BPC 157 Enhances the Growth Hormone Receptor Expression in Tendon Fibroblasts. Molecules. 2014;19(12):19066-19077.
- Vukojević J, Siroglavić M, Kašnik K, Kralj T, et al. Rat inferior caval vein (ICV) ligature and particular new insights with the stable gastric pentadecapeptide BPC 157. Vascular Pharmacology. 2018;106:54-66.
- Sikiric P, et al. The pharmacological properties of the novel peptide BPC 157 (PL-10). Inflammopharmacology. 1999;7(1):1-14.
- Zemba Cilic A, Zemba M, Cilic M, Balenovic I, Strbe S, et al. Pentadecapeptide BPC 157 counteracts L-NAME-induced catalepsy. BPC 157, L-NAME, L-arginine, NO-relation, in the suited rat acute and chronic models resembling 'positive-like' symptoms of schizophrenia. Behavioural Brain Research. 2021;396:112919.
- Staresinic M, et al. Gastric pentadecapeptide BPC 157 accelerates healing of transected rat Achilles tendon and in vitro stimulates tendocytes growth. Journal of Orthopaedic Research. 2003;21(6):976-983.
- Matek D, et al. Stable Gastric Pentadecapeptide BPC 157 as Therapy After Surgical Detachment of the Quadriceps Muscle from Its Attachments for Muscle-to-Bone Reattachment in Rats. Pharmaceutics. 2025;17(1):119.
- Tudor M, et al. The gastroprotective and neuroprotective pentadecapeptide BPC 157 in the treatment of traumatic brain injury in rats. Regulatory Peptides. 2010;160(1-3):26-32.
- Perovic D, Kolenc D, Bilic V, Somun N, et al. 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. 2019;14(1):199.
- Sikiric P, et al. Vascular occlusion and stable gastric pentadecapeptide BPC 157. Current Pharmaceutical Design. 2022;28(25):2082-2093.
- Masnec S, et al. Perforating corneal injury in rat and pentadecapeptide BPC 157. Experimental Eye Research. 2015;136:9-15.
- Sever M, et al. Stable gastric pentadecapeptide BPC 157 counteracts liver fibrosis. Journal of Physiology and Pharmacology. 2019;70(3):391-400.
- Lee E, Padgett B. Intra-Articular Injection of BPC 157 for Multiple Types of Knee Pain. Alternative Therapies in Health and Medicine. 2021;27(4):8-13.
- Lee E, Walker C, Ayadi B. Effect of BPC-157 on Symptoms in Patients with Interstitial Cystitis: A Pilot Study. Alternative Therapies in Health and Medicine. 2024;30(10):12-17.
- He L, Feng D, Guo H, Zhou Y, et al. Pharmacokinetics, distribution, metabolism, and excretion of body-protective compound 157, a potential drug for treating various wounds, in rats and dogs. Frontiers in Pharmacology. 2022;13:1026182.
- Veljaca M, et al. BPC-157: Safety and pharmacokinetics after rectal administration in healthy male volunteers. Gut. 2003;52(Suppl VI):A246.
- Lee E, Burgess K. Safety of Intravenous Infusion of BPC157 in Humans: A Pilot Study. Alternative Therapies in Health and Medicine. 2025;31(5):20-24.
- Seiwerth S, Rucman R, Turkovic B, Sever M, et al. BPC 157 and Standard Angiogenic Growth Factors. Gastrointestinal Tract Healing, Lessons from Tendon, Ligament, Muscle and Bone Healing. Current Pharmaceutical Design. 2018;24(18):1972-1989.
- Seiwerth S, et al. Stable Gastric Pentadecapeptide BPC 157 and Wound Healing. Frontiers in Pharmacology. 2021;12:627533.
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