PRECLINICAL DEVELOPMENT OF A NEW DRUG FOR PCP

PCP 新药的临床前开发

• 批准号: 2659828
• 负责人: ALICE M. CLARK
• 金额: $ 9.99万
• 依托单位: ELSOHLY LABORATORIES, INC.
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-05-01 至 1999-10-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2659828
• 关键词: Pneumocystis carinii; antiprotozoal agents; drug design /synthesis /production; pharmacokinetics; quinoline

DESCRIPTION (Adapted from the Investigator's Abstract): The overall objective of this Phase 1 STTR application is to accomplish studies aimed at advancing a promising new drug candidate for the treatment of AIDS- related Pneumocystis carinii pneumonia (PCP) to human clinical trials. This will be accomplished through a plan of work to achieve the following specific aims: (1) develop a practical, economical and convergent synthesis of NPC1161 that is compatible with kilogram scale-up, future radiolabeling (for Phase II mechanism of action and pharmocokinetic studies), and prospective commercial development; (2) prepare putative metabolites of NPC1161 by chemical and/or bioconversion/biocatalysis methods; (3) develop a sensitive and quantitative analytical method(s) to detect putative metabolites (and parent drugs) in biological fluids; (4) determine in vitro uptake and toxicity to human red blood cells by NPC1161 derivatives and putative metabolites. PROPOSED COMMERCIAL APPLICATION: Potential commercial application not available.

描述（改编自研究者的摘要）：总体 STTR 第一阶段申请的目标是完成旨在 开发一种有前途的治疗艾滋病的新候选药物 卡氏肺囊虫肺炎（PCP）与人体临床试验相关。 这将通过一项工作计划来实现，以实现以下目标 具体目标： (1) 开发实用、经济、收敛的NPC1161合成方法 与公斤级放大、未来放射性标记（用于阶段 II 作用机制和药代动力学研究）和前瞻性 商业发展； (2)通过化学和/或制备NPC1161的推定代谢物 生物转化/生物催化方法； (3) 开发灵敏的定量分析方法来检测 生物体液中推定的代谢物（和母体药物）； (4) 测定体外对人红细胞的摄取和毒性 NPC1161 衍生物和推定代谢物。 拟议的商业应用： 潜在的商业应用不可用。