Unprecedented Diversion-/Abuse-Resistance: Molecular Deactivation of Opioid Drugs

前所未有的抗转移/滥用：阿片类药物的分子失活

基本信息

批准号：
9058022
负责人：
Thomas E Jenkins
金额：
$ 35.54万
依托单位：
ELYSIUM THERAPEUTICS, INC.
依托单位国家：
美国
项目类别：
财政年份：
2014
资助国家：
美国
起止时间：
2014-09-15 至 2017-07-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/9058022
关键词：
Absence of pain sensation Address Agonist Air Bags American Americas Automobiles Bioavailable Biological Assay Clinical Consult Coupled Data Development Dose Drug Controls Epidemic Exposure to Family Feasibility Studies Formulation Friends Grant Half-Life Health Hour Human Hydrocodone In Vitro Ingestion Intestines Lead Liquid substance Liver Microsomes Manufacturer Name Marketing Measures Medicine Molecular Naltrexone National Institute of Drug Abuse Opioid Oral Overdose Oxycodone Pain Pain management Pharmaceutical Preparations Pharmacologic Substance Phase Policies Polymers Principal Investigator Process Publishing Rattus Resistance Route Safety Small Business Innovation Research Grant Solubility Solvents Source Specific qualifier value Stomach Technology Therapeutic Equivalency Time Whole Blood analytical method base clinical lot commercialization controlled release design expiration feeding human data in vivo innovation interest meetings novel pill pre-clinical prescription drug abuse prescription opioid prescription opioid abuse programs prototype screening solid state

项目摘要

DESCRIPTION: Elysium has discovered a novel molecular deactivation (XpiRx" or "expiring pill") technology that is designed to effectively curb the widespread abuse and diversion of unused prescription opioid drugs. Using Elysium's technology, opioid drug products will safely, and irreversibly lose their potency over a specified time window beyond the prescribed use period, rendering them devoid of opioid agonist effects, and, therefore, completely abuse-resistant. Our XpiRx technology enables: (i) effective pain relief during the prescribed use period; (ii) abuse-resistance via non-oral routes; (iii) oral abuse-deterrence beyond the prescribed use period; and (iv) oral overdose protection beyond the programmed expiration date. According to President Obama, "Prescription drug abuse is America's fastest-growing drug problem, and one largely fed by an unlikely source - Americans' medicine cabinets." Over 70% of abusers obtain unused prescription opioids from their friends and family. Current opioid pills lose only ~1% of their potency per year, resulting in a 70-year potency half-life. Elysium's XpiRx technology dramatically shortens the opioid drug's potency half-life, which would substantially decrease the pool of drugs ("diversion pool") that attract abusers. We are applying for Fast-Track because NIDA program officials assured us that our proposed project is an excellent Fast-Track candidate based on: Compelling in vitro data from studies led by our Principal Investigator coupled with published Phase 1 human data demonstrate the feasibility of achieving unprecedented abuse- and diversion-resistance with XpiRx technology; The lack of technologies in development or on the market that address diversion, the primary source for abused prescription opioid drugs; and Key stakeholder interest: The Office for National Drug Control Policy (ONDCP) and The National Institute on Drug Abuse (NIDA) have identified diversion as a high priority issue because it fuels the prescription drug abuse epidemic. Pharmaceutical company leaders believe that XpiRx could become a standard safety requirement for opioid drugs (like airbags for automobiles).

描述：Elysium 发现了一种新型分子失活（XpiRx”或“过期药丸”）技术，旨在有效遏制未使用的处方阿片类药物的广泛滥用和转移。利用 Elysium 的技术，阿片类药物产品将安全且不可逆转地失去其活性。在超出规定使用期限的指定时间窗口内发挥效力，使它们没有阿片类激动剂作用，因此，我们的 XpiRx 技术能够： (i) 在规定的使用期限内有效缓解疼痛； (ii) 通过非口服途径抗滥用； (iii) 在规定的使用期限之后进行口服滥用预防；以及 (iv) 在规定的有效期之后进行口服过量保护。奥巴马总统表示，“处方药滥用是美国发展最快的毒品问题，而这一问题主要是由一个不太可能的来源造成的——超过 70% 的滥用者从他们的朋友和家人那里获得未使用的处方阿片类药物。”药丸每年仅损失约 1% 的效力，从而导致 70 年的效力半衰期。 Elysium 的 XpiRx 技术极大地缩短了阿片类药物的效力半衰期，这将大大减少吸引滥用者的药物池（“转移池”）。我们正在申请快速通道，因为 NIDA 项目官员向我们保证，我们提出的项目是一个优秀的快速通道候选项目，基于：由我们的首席研究员领导的研究得出的令人信服的体外数据，加上已发布的第一阶段人体数据，证明了实现这一目标的可行性XpiRx 技术具有前所未有的防滥用和防转移能力；开发中或市场上缺乏解决转移问题的技术，转移是滥用处方阿片类药物的主要来源；主要利益相关者的利益：国家药物管制政策办公室 (ONDCP) 和国家药物滥用研究所 (NIDA) 已将转移问题确定为高度优先的问题，因为它助长了处方药滥用的流行。制药公司领导人相信 XpiRx 可能成为阿片类药物（如汽车安全气囊）的标准安全要求。