SYNTHESIS OF BULK CHEMICALS & DRUGS FOR PRECLINICAL USE

大宗化学品的合成

• 批准号: 6091054
• 负责人: JACK J PARSONS
• 金额: $ 97.63万
• 依托单位: STARKS ASSOCIATES, INC.
• 依托单位国家: 美国
• 财政年份: 1996
• 资助国家: 美国
• 起止时间: 1996-06-29 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/6091054
• 关键词: antiAIDS agent; antineoplastics; chemical registry /resource; drug design /synthesis /production; drug quality /standard

The Pharmaceuticals Resources Branch (PRB) of the Developmental Therapeutics Program (DTP) of the Division of Cancer Treatment, Diagnosis and Chemotherapy (DCTDC) of the National Cancer Institute has primary responsibility for the production of a variety of compounds as bulk pharmaceuticals for use in both clinical and preclinical evaluations as potential anti-AIDS agents and anticancer agents. The PRB works closely with the DTP screening group to prepare larger quantities of drug candidates for in vivo evaluation and for the preparation of derivatives of drug candidates with improved physical properties, such as improved solubility or better pharmacokinetic properties, through the use of pro-drugs or other selected chemical derivatives. As part of this process, the PRB may undertake the development of existing or new, more efficient, chemical processes, procedures, and techniques for the preparation of those compounds of interest. Once identified as a potential drug candidate for anti-AIDS or anticancer treatment, the PRB undertakes the scale-up preparation of varying amounts of compound, based on the immediate needs of the program. The amounts may range from milligram quantities to multi-kilogram quantities, depending upon the stage of development of the compound and its biological potency. Once accepted for human clinical trials, the PRB is responsible for the preparation of clinical materials that meet the FDA requirements for Good Manufacturing Practices (GMP) and Good Laboratory Practices (GLP) drug production. As such the procedures developed by PRB will define the purity standards and criteria for the clinical bulk pharmaceutical based on those produced during the scale-up process. The purpose of this project is to obtain contractors who have the equipment and expertise to conduct organic synthesis and purification of potential anti-AIDS and anticancer drug candidates in quantities up to multi-kilogram amounts. Further, they must be capable of production under GMP and GLP conditions when needed. They will be called upon to procure, purify (if necessary) and characterize substances from suitable sources; perform preliminary stability, solubility, and analytical studies on the products; and prepare analytical reference standards, and novel derivatives as needed by the program.

发展局药品资源处 (PRB) 癌症治疗、诊断科的治疗计划（DTP） 美国国家癌症研究所的化疗和化疗 (DCTDC) 拥有主要 负责生产各种散装化合物 用于临床和临床前评估的药物 潜在的抗艾滋病剂和抗癌剂。 PRB 与 DTP 筛选小组密切合作，准备更大规模的 大量候选药物用于体内评估和 制备具有改善物理性能的候选药物衍生物 特性，例如改善的溶解度或更好的药代动力学 通过使用前药或其他选定的化学品来改变特性 衍生物。作为此过程的一部分，PRB 可以采取以下措施： 开发现有的或新的、更高效的化学工艺， 制备这些化合物的程序和技术 兴趣。 一旦被确定为抗艾滋病或抗癌的潜在候选药物 处理后，PRB进行不同数量的放大制备 化合物，基于该计划的直接需求。金额可能 范围从毫克到公斤，具体取决于 化合物的开发阶段及其生物效力。 一旦接受人体临床试验，PRB 负责 准备符合 FDA Good 要求的临床材料 药品生产规范 (GMP) 和良好实验室规范 (GLP) 生产。因此，PRB 制定的程序将定义 纯度标准和临床原料药标准 在放大过程中生产的那些。 该项目的目的是获得具有以下能力的承包商： 进行有机合成和纯化的设备和专业知识 潜在的抗艾滋病和抗癌候选药物数量高达 数公斤的数量。此外，它们必须能够在 需要时符合 GMP 和 GLP 条件。 他们将被要求 从合适的物质中采购、纯化（如有必要）和表征物质 来源；进行初步稳定性、溶解度和分析 对产品的研究；并准备分析参考标准，以及 程序所需的新颖衍生品。