Department of Pharmacology and Pathology, Medical Faculty University of Zagreb, Salata 11, POB 916, 10000 Zagreb, Croatia.
Curr Pharm Des. 2013;19(1):76-83. doi: 10.2174/13816128130111.
Stable gastric pentadecapeptide BPC 157 is an anti-ulcer peptidergic agent, proven in clinical trials to be both safe in inflammatory bowel disease (PL-10, PLD-116, PL 14736) and wound healing, stable in human gastric juice, with no toxicity being reported. Recently, we claim that BPC 157 may be used as an antidote against NSAIDs. We focused on BPC 157 beneficial effects on stomach, duodenum, intestine, liver and brain injuries, adjuvant arthritis, pain, hyper/hypothermia, obstructive thrombus formation and thrombolysis, blood vessel function, counteraction of prolonged bleeding and thrombocytopenia after application of various anticoagulants and antiplatelet agents and wound healing improvement. The arguments for BPC 157 antidote activity (i.e., the role of BPC 157 in cytoprotection, being a novel mediator of Robert's cytoprotection and BPC 157 beneficial effects on NSAIDs mediated lesions in the gastrointestinal tract, liver and brain and finally, counteraction of aspirin-induced prolonged bleeding and thrombocytopenia) obviously have a counteracting effect on several established side-effects of NSAIDs use. The mentioned variety of the beneficial effects portrayed by BPC 157 may well be a foundation for establishing BPC 157 as a NSAIDs antidote since no other single agent has portrayed a similar array of effects. Unlike NSAIDs, a very high safety (no reported toxicity (LD1 could be not achieved)) profile is reported for BPC 157. Also, unlike the different dosage levels of aspirin, as a NSAIDs prototype, which differ by a factor of about ten, all these beneficial and counteracting effects of BPC 157 were obtained using the equipotent dosage (μg, ng/kg) in parenteral or peroral regimens.
稳定的胃十五肽 BPC 157 是一种抗溃疡肽类药物，临床试验证明其在炎症性肠病（PL-10、PLD-116、PL 14736）和伤口愈合中既安全又稳定，在人类胃液中稳定，没有毒性报告。最近，我们声称 BPC 157 可作为 NSAIDs 的解毒剂。我们专注于 BPC 157 对胃、十二指肠、肠、肝和脑损伤、佐剂性关节炎、疼痛、高/低体温、阻塞性血栓形成和溶栓、血管功能、各种抗凝剂和抗血小板药物应用后延长出血和血小板减少的拮抗作用以及伤口愈合的改善。BPC 157 解毒作用的论据（即 BPC 157 在细胞保护中的作用、作为罗伯特细胞保护的新型介质以及 BPC 157 对胃肠道、肝脏和大脑中 NSAIDs 介导损伤的有益作用，最后，对抗阿司匹林引起的延长出血和血小板减少）显然对 NSAIDs 使用的几种已确立的副作用具有拮抗作用。BPC 157 所描绘的有益作用的多样性很可能为将 BPC 157 确立为 NSAIDs 解毒剂奠定基础，因为没有其他单一药物具有类似的多种作用。与 NSAIDs 不同，BPC 157 报告的安全性非常高（未报告毒性（LD1 无法达到））。此外，与作为 NSAIDs 原型的不同阿司匹林剂量水平不同，后者相差约 10 倍，BPC 157 的所有这些有益和拮抗作用都是通过使用等效剂量（μg、ng/kg）在肠外或口服方案中获得的。
