CHEMICAL SYNTHESIS FACILITY

化学合成设施

• 批准号: 10939296
• 负责人: VADIM GURVICH
• 金额: $ 74.89万
• 依托单位: UNIVERSITY OF MINNESOTA
• 依托单位国家: 美国
• 财政年份: 2022
• 资助国家: 美国
• 起止时间: 2022-09-29 至 2024-09-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/10939296
• 关键词: Agonist; Androgens; Area; Chemical Agents; Chemicals; Clinical Research; Contraceptive Agents; Contraceptive methods; Contractor; Contracts; Development; Estrogens; Evaluation; Female Contraceptive Agents; Fertility Agents; Goals; Good Manufacturing Process; Government; Human; Kilogram; Laboratories; Male Contraceptive Agents; Natural Products; Peptides; Pharmaceutical Preparations; Preparation; Progestins; Program Development; Proteins; Research Support; Role; Steroids; Testing; Toxicology; Woman; analog; antagonist; chemical synthesis; drug candidate; manufacture; men; milligram; new chemical entity; preclinical safety; programs; safety study; small molecule; unnatural amino acids

The Contraceptive Development Program (CDP) supports research in the synthesis and testing of a broad spectrum of male and female contraceptive agents. Successful development of new contraceptive methods for men and women has been a goal for many decades. From the inception of this program, the CDP has had a continuing need for a Chemical Synthesis Facility (CSF) capable of synthesizing potential anti-fertility agents on a laboratory milligram to gram scale to a relatively larger kilogram scale. The kilogram scale chemical agents are manufactured under current Good Manufacturing Practices (cGMP) for comprehensive contraceptive evaluation, including toxicology studies and preclinical safety studies before entering human clinical studies. The CSF provides the Government with chemicals, chemical intermediates, steroids, drug candidates, and drugs, which are either a new chemical entity (NCE) commercially unavailable or unduly expensive to obtain commercially. The areas of chemical synthesis for CSF consist of small molecule antagonists or agonists of protein targets, including but not limited to active natural products, natural product analogues, active steroids estrogens, progestins, androgens, and their analogues. In addition, CSF has an important role in support of providing intermediates for the synthesis of many unnatural amino acids that may be incorporated into the preparation of unnatural peptide agonists or antagonists by another CDP's contractor.

避孕药开发计划 (CDP) 支持广泛的男性和女性避孕药的合成和测试研究。成功开发针对男性和女性的新避孕方法一直是几十年来的目标。从该计划启动以来，CDP 一直需要一个化学合成设施 (CSF)，该设施能够在实验室毫克到克规模到相对较大的公斤规模上合成潜在的抗生育药物。公斤级化学制剂是根据现行良好生产规范（cGMP）生产的，用于全面的避孕评估，包括进入人体临床研究之前的毒理学研究和临床前安全性研究。 CSF 向政府提供化学品、化学中间体、类固醇、候选药物和药物，这些产品要么是商业上无法获得的新化学实体 (NCE)，要么是商业上获得的成本过高。 CSF化学合成领域包括蛋白质靶点的小分子拮抗剂或激动剂，包括但不限于活性天然产物、天然产物类似物、活性类固醇雌激素、孕激素、雄激素及其类似物。此外，CSF 在支持为许多非天然氨基酸的合成提供中间体方面发挥着重要作用，这些中间体可能被另一个 CDP 承包商纳入非天然肽激动剂或拮抗剂的制备中。