PHASE I TRIAL OF D1694, AN INHIBITOR OF THYMIDYLATE SYNTHASE

胸苷酸合酶抑制剂 D1694 的 I 期试验

• 批准号: 6276836
• 负责人: JAMES A WHITLOCK
• 金额: $ 3.29万
• 依托单位: VANDERBILT UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1997
• 资助国家: 美国
• 起止时间: 1997-12-01 至 1998-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6276836
• 关键词: antineoplastics; child (0-11); clinical research; clinical trial phase I; dosage; drug screening /evaluation; enzyme inhibitors; human subject; human therapy evaluation; neoplasm /cancer chemotherapy; pediatric neoplasm /cancer; pediatric pharmacology; pharmacokinetics; thymidylate synthase

This phase I study is designed to define the MTD (maximum tolerated dose) of D1694 in pediatric patients. Analogs of folic acid have been successfully used for the treatment of cancer for more than 40 years. The underlying mechanism of action for classical antifols such as methotrexate (MTX) is their ability to block the denovo synthesis of purine and pyrimidine nucleotide precursors of DNA, primarily by inhibiting dihydrofolate reductase (DHFR). Thymidylate synthase (TS), an enzyme which acts by utilizing 5, 10-CH2FH4 in the reductive methylation of deoxyuridylate (dUMP),is required for the de novo synthesis of thymidylate and is thus a potential target of folic acid analogs. We are enrolling patients in all centers thus, finish the study soon.

该I期研究旨在确定MTD（最大耐受剂量）