NOVEL ANTITUMOR DISULFIDES

描述：（申请人描述）ProIX Pharmaceuticals，Inc.具有 证明硫氧还蛋白在维持 一些人类癌症的转化表型以及它们对 化疗药物和硫氧还蛋白是一种高度合理的新的靶点， 癌症药物研发 本文所述的研究表明， 抗凋亡癌基因，在许多人类癌症中过度表达。 ProIX制药公司拥有全球独家开发 硫氧还蛋白目标，并致力于利用这些观察， 快速发展的试剂，选择性地破坏这种新的信号， 转导途径 我们最初的第一阶段建议的目标是 开发基于一类新的硫氧还蛋白氧化还原系统的新型抑制剂， 我们发现的选择性抑制剂。 我们的第一阶段研究提供了 有前途的临床候选人，PX-12，以及第二代和第三代， 剂. 第二阶段提案的目标是将我们的小说 硫氧还蛋白氧化还原系统的抑制剂PX-12，通过更广泛的 临床前开发并进入I期临床试验。 其次， 我们打算继续第二和第三种药物的临床前开发， 产生硫氧还蛋白抑制剂。 建议的具体目标如下： 如下：1）完成PX-12的临床前评价，包括毒理学， 药物和药代动力学评价; 2）完成GMP生产 和PX-12的制剂; 3）启动PX-12的I期临床试验; 4） 总结第二代药物的临床前评价，并进行 新型第三代水溶性药物的平行临床前评价 衍生物. ProIX制药公司将拥有全球独家许可证 开发这些化合物作为氧化还原调节的新型抑制剂， 潜在的抗癌剂的专利获得的创始成员， 公司 拟议商业应用：不可用

DESCRIPTION: (Applicant's Description) ProIX Pharmaceuticals, Inc. has demonstrated that thioredoxin has an important role in maintaining the transformed phenotype of some human cancers as well as their resistance to chemotherapeutic drugs and thioredoxin is, a highly rational target for novel cancer drug development. The studies described herein suggest that a human anti-apoptosis oncogene that is overexpressed by a number of human cancers. ProIX Pharmaceuticals Inc. has the exclusive worldwide rights to develop the thioredoxin target and is dedicated to exploiting these observations and rapidly developing agents that selectively disrupt this novel signal transduction pathway. The objective of our initial Phase I proposal was to develop novel inhibitors of thioredoxin redox system based on a new class of selective inhibitors we had identified. Our Phase I studies have provided a promising clinical candidate, PX-12, as well as second and third generation agents. The objective of this Phase II proposal is to move our novel inhibitor of thioredoxin redox system, PX-12, through more extensive preclinical development and into a Phase I clinical trial. Secondary to this, we intend to continue the preclinical development of the second and third generation thioredoxin inhibitors. The Specific Aims of the proposal are as follows: 1) to complete Preclinical Evaluation of PX-12 including toxicologic, pharmaceutic and pharmacokinetic evaluation; 2) to complete GMP manufacture and formulation of PX-12; 3) to initiate a Phase I clinical trail of PX-12; 4) to conclude preclinical evaluation of second generation drugs, and to carry out parallel preclinical evaluation on novel third generation water soluble derivatives. ProIX Pharmaceuticals will have the exclusive world-wide license to develop these compounds as novel inhibitors of redox regulation and as potential anticancer agents by patents obtained from founding members of the company. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE