Catalog
Synthetic pentadecapeptide (gastric origin)

BPC-157

aka Body Protective Compound 157 · PLD-116 · PL-10 · PL14736 · Bepectin

Strong rodent healing data, essentially zero controlled human trials. FDA Cat 2 (2023). WADA-monitored.

Research-only / unregulatedGrade D — Plausible, unprovenFDA Category 2 (2023) — barred from 503A compounding
Target
VEGFR2 up-regulation, eNOS/NO pathway, modulation of 5-HT2A and dopaminergic signaling, EGR-1/NAB2; no canonical receptor identified
Sequence / engineering
15 aa: Gly-Glu-Pro-Pro-Pro-Gly-Lys-Pro-Ala-Asp-Asp-Ala-Gly-Leu-Val. MW 1419.55 Da. Sequence partially derived from human gastric juice protein BPC; not homologous to known intestinal peptides. Stable in gastric juice and water.

Mechanism of action

Pleiotropic cytoprotective pentadecapeptide. Proposed mechanisms (preclinical, largely rat): (1) angiogenesis via VEGFR-2 up-regulation in endothelial cells and ischemic tissue (Hsieh 2017); (2) eNOS-derived NO release with downstream HO-1 induction and platelet/vascular effects; (3) modulation of 5-HT2A (counters serotonin-syndrome features) and dopaminergic tone (antagonizes haloperidol catalepsy and amphetamine-induced behavior); (4) EGR-1 / NAB2 induction implicated in granulation-tissue formation; (5) interaction with arachidonic acid → COX-1/COX-2 → PG pathway, partly explaining its protection against NSAID-induced GI and hepatic injury. No canonical receptor has been cloned (Józwiak 2025 review).

Pharmacokinetics

Single rat/dog PK study (He et al.): IM bioavailability ~14–19% (rat) and ~45–51% (dog). Tmax ~3 min (rat IM), 6–9 min (dog IM). Wide tissue distribution (kidney highest; low brain penetration → poor BBB crossing). Rapidly degraded to six small peptide metabolites (proline is the major one). Elimination t½ < 30 min. One human PK study (Veljaca 2002) is reported but details are scant. Claims of oral bioavailability based on 'gastric juice stability' are not rigorously demonstrated in humans.

Clinical context

No approved human indication anywhere. Marketed off-label/grey-market for tendinopathy, ligament injury, IBD/colitis, post-surgical recovery, joint pain, alcohol/NSAID-induced GI injury, and (more speculatively) depression and post-stroke recovery. Phase I safety/PK trial NCT02637284 (n=42 healthy volunteers, 2015) was withdrawn before results were posted. The few human reports are case series (e.g., 12-pt retrospective intra-articular knee injection) with no validated outcome instruments.

Dosing
No validated human dose. Preclinical efficacy across very wide dose ranges (10 ng/kg to 10 µg/kg, IP/IG/IM, in rats). Acute and 28-day toxicity studies in rats (up to 20 mg/kg single IM; 4 mg/kg/day × 28 d) and beagle dogs (10 mg/kg single IM; 2 mg/kg/day × 28 d) reported no overt toxicity (Xu 2020) — but no human dose-finding has been completed.

Monitoring

  • No validated monitoring protocol
  • If patient insists on use: discuss VEGF/angiogenesis-related theoretical risks (cancer screening per age/risk), document informed consent, and source verification

Safety

Contraindications
  • Pregnancy/lactation (no data)
  • Active or prior malignancy — theoretical concern given VEGFR-2 up-regulation, NO/eNOS stimulation, and EGR-1 induction (all implicated in tumor angiogenesis and progression)
  • Patients with cardiovascular disease on NO-modulating drugs (theoretical interaction with eNOS/PKG/cGMP pathway)
Adverse effects
  • No formal human pharmacovigilance dataset
  • Pain and/or local necrosis reported with aqueous/saline injection (1998 patent record)
  • Theoretical: pro-angiogenic effect could promote occult tumor growth or aberrant neovascularization
  • Theoretical: chronic NO elevation may interfere with heme insertion in hemoglobin and CYP enzymes (drug-metabolism implications) and may contribute to iron-mediated neurodegeneration
  • Proline metabolite — at high turnover, proline-oxidase activity can generate ROS (peroxynitrite) — relevance unclear
  • Source/purity is the dominant real-world risk: grey-market vials routinely fail identity/purity testing

Myth vs reality

CLAIMBPC-157 is proven to heal tendons in humans.
REALITYThere is no published RCT in humans. All efficacy claims rest on rat (and a few dog) models. The single registered Phase I trial (NCT02637284) was withdrawn before results were reported.
CLAIMBPC-157 is safe because it's a fragment of a stomach protein.
REALITYEndogenous origin says nothing about pharmacological-dose safety. Insulin and angiotensin are also endogenous.
CLAIMOral BPC-157 capsules work because the peptide is gastric-juice-stable.
REALITYStability in gastric juice in vitro does not establish systemic oral bioavailability in humans, which has never been formally measured.

Patient counseling points

  • Frame honestly: 'The animal data are genuinely interesting; the human data are essentially absent — one phase 1 trial was started and withdrawn.'
  • Name the regulatory reality: FDA placed BPC-157 on the 503A Category 2 list in 2023, meaning it cannot legally be compounded by 503A pharmacies in the US.
  • Athletes: BPC-157 is on the WADA Monitoring Program and falls under S0 (non-approved substances) — detected use can end a competitive career.
  • Cancer screening: discuss the theoretical pro-angiogenic risk before any chronic use, especially in patients with personal/family history of malignancy.

Covered in modules

Module 06
BPC-157, TB-500 & 'Healing Peptides'
The grey-market repair narrative — what the rat data show, what humans don't have.
Module 14
Safety, Regulation & Compounded Peptides
503A vs 503B vs research-only — what the FDA actually says.

Key references

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CJC-1295 (with/without DAC)
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TB-500 (Thymosin β4 fragment)

Generate prescriber-grade deep dive

Pull in expanded mechanism, PK/PD, dosing strategies for special populations, drug interactions, monitoring cadence, head-to-head differentials, prescriber pearls, and patient FAQs for BPC-157.

Educational reference. Not medical advice. Always verify against current FDA labeling and local regulatory guidance before prescribing or counseling.