A Safe Analgesic Drug with Addiction Treatment Potential

一种具有成瘾治疗潜力的安全镇痛药

• 批准号: 6742227
• 负责人: JOHN A LAWSON
• 金额: $ 10万
• 依托单位: PHOENIX PHARMALABS, INC.
• 依托单位国家: 美国
• 财政年份: 2004
• 资助国家: 美国
• 起止时间: 2004-03-01 至 2005-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6742227
• 关键词: analgesics; drug abuse chemotherapy; drug design /synthesis /production; method development; opiate alkaloid; opioid receptor; stimulant /agonist

DESCRIPTION (provided by applicant): This SBIR grant is sought for the purpose of commercializing a promising and needed drug NIH 10497(D-1). It is a novel, orally active opioid with a unique chiral N-substituent that confers an unprecedented activity profile. It has promise as a safe potent analgesic and as a treatment for addiction, not with maintenance, but with potential for cure. NIH 10497 has already been shown by NIDA funded studies to possess an unusual balance of agonist activities at the kappa, mu, and delta opioid receptors. In particular, the drug was discovered to substitute for Morphine in dependent animals, while causing no physical dependence in non-dependent animals. This suggests a novel profile of activities. NIH 10497 was originally discovered in 1980 but was never marketed. The inventor of NIH 10497 founded a small business, Phoenix PharmaLabs, for the purpose of commercializing this drug. Our first goal is to create fresh Patents (the original Patents have expired) for a new Use and, with SBIR support, for a critical new Method of large-scale synthesis that is stereoselective and scalable. This will require the discovery of an improved reductive amination step using a chiral reducing agent. NIH 10497 also lacks sufficient in vivo evaluation, so under this grant, a consortium agreement with Dr. Lou Harris will fund a Morphine Substitution Study (MSS) in the rat at VCU. The PI and two of the consultants, Dr. Toll and Dr. Lukeman have traveled to China three times to meet with Ms. Peng Yan and interested investors. Investors are attracted to NIH 10497 for a number of reasons. Toxicology and Clinic trials are much less expensive in China and there is strong need for a treatment of addiction in that country. The PI and Dr. DeGraw will develop new synthetic methods for NIH 10497 to achieve a Method Patent that is crucial to attract the Investor. Dr. Harris will supervise the MS study in rats, and Dr. Lukeman will assist in the pharmacologic assessment of the results and determine the valuation of NIH 10497 in preparation for commercialization.

描述（由申请人提供）：该 SBIR 拨款的目的是将一种有前途且需要的药物 NIH 10497(D-1) 商业化。它是一种新型口服阿片类药物，具有独特的手性 N 取代基，具有前所未有的活性。它有望成为一种安全有效的镇痛剂和成瘾治疗方法，不是维持治疗，而是具有治愈的潜力。 NIDA 资助的研究已表明 NIH 10497 对 kappa、mu 和 delta 阿片受体激动剂活性具有异常平衡。特别是，该药物被发现可以在依赖性动物中替代吗啡，同时不会对非依赖性动物造成身体依赖性。这表明了一种新颖的活动概况。 NIH 10497 最初于 1980 年被发现，但从未上市。 NIH 10497 的发明者成立了一家小企业 Phoenix PharmaLabs，旨在将该药物商业化。我们的首要目标是为新用途创造新的专利（原始专利已过期），并在 SBIR 支持下，为立体选择性和可扩展的大规模合成的关键新方法创造新的专利。这将需要发现使用手性还原剂的改进的还原胺化步骤。 NIH 10497 也缺乏足够的体内评估，因此根据这笔拨款，与 Lou Harris 博士达成的财团协议将资助弗吉尼亚联邦大学的大鼠吗啡替代研究 (MSS)。 PI和两位顾问Toll博士和Lukeman博士已三次前往中国与彭岩女士和感兴趣的投资者会面。 NIH 10497 吸引投资者的原因有很多。在中国，毒理学和临床试验的费用要便宜得多，而且该国对成瘾治疗的需求非常强烈。 PI 和 DeGraw 博士将为 NIH 10497 开发新的合成方法，以获得对于吸引投资者至关重要的方法专利。 Harris 博士将监督大鼠 MS 研究，Lukeman 博士将协助对结果进行药理学评估并确定 NIH 10497 的估值，为商业化做准备。