Davit Barbara M, Kanfer Isadore, Tsang Yu Chung, Cardot Jean-Michel
Merck Research Laboratories, Rahway, New Jersey, USA.
Rhodes University, Grahamstown, South Africa.
AAPS J. 2016 May;18(3):612-8. doi: 10.1208/s12248-016-9877-2. Epub 2016 Mar 4.
The Biopharmaceutics Classification System (BCS), based on aqueous solubility and intestinal permeability, has enjoyed wide use since 1995 as a mechanism for waiving in vivo bioavailability and bioequivalence studies. In 2000, the US-FDA was the first regulatory agency to publish guidance for industry describing how to meet criteria for requesting a waiver of in vivo bioavailability and bioequivalence studies for highly soluble, highly permeable (BCS Class I) drugs. Subsequently, the World Health Organization (WHO) and European Medicines Agency (EMA) published guidelines recommending how to obtain BCS biowaivers for BCS Class III drugs (high solubility, low permeability), in addition to Class I drugs. In 2015, the US-FDA became better harmonized with the EMA and WHO following publication of two guidances for industry outlining criteria for obtaining BCS biowaivers for both Class I and Class III drugs. A detailed review and comparison of the BCS Class I and Class III criteria currently recommended by the US-FDA, EMA, and WHO revealed good convergence of the three agencies with respect to BCS biowaiver criteria. The comparison also suggested that, by applying the most conservative of the three jurisdictional approaches, it should be possible for a sponsor to design the same set of BCS biowaiver studies in preparing a submission for worldwide filing to satisfy US, European, and emerging market regulators. It is hoped that the availability of BCS Class I and Class III biowaivers in multiple jurisdictions will encourage more sponsors to request waivers of in vivo bioavailability/bioequivalence testing using the BCS approach.
生物药剂学分类系统(BCS)基于水溶性和肠道渗透性,自1995年以来已被广泛用作免除体内生物利用度和生物等效性研究的一种机制。2000年,美国食品药品监督管理局(US-FDA)是第一个发布行业指南的监管机构,该指南描述了如何满足对高溶解性、高渗透性(BCS I类)药物免除体内生物利用度和生物等效性研究的标准。随后,世界卫生组织(WHO)和欧洲药品管理局(EMA)发布了指南,除了I类药物外,还推荐了如何获得BCS III类药物(高溶解性、低渗透性)的BCS生物豁免。2015年,美国食品药品监督管理局在发布了两份行业指南后,与EMA和WHO实现了更好的协调,这两份指南概述了获得I类和III类药物BCS生物豁免的标准。对美国食品药品监督管理局、EMA和WHO目前推荐的BCS I类和III类标准进行详细审查和比较后发现,这三个机构在BCS生物豁免标准方面具有良好的一致性。比较还表明,通过采用三个管辖区域方法中最保守的方法,申办者应该有可能设计出同一套BCS生物豁免研究,以便在准备全球申报文件时满足美国、欧洲和新兴市场监管机构的要求。希望多个管辖区域都能提供BCS I类和III类生物豁免,这将鼓励更多申办者采用BCS方法申请免除体内生物利用度/生物等效性测试。