SURVIVAL SIGNALING INHIBITORS AS CANCER DRUGS

ProlX制药公司已经证明，有强有力的证据证明：1)PtdIns-3-Kinase和Akt是抗癌药物发现的两个新的有效分子靶点；2)这些靶点与多种人类癌症相关；以及3)用小分子药物抑制这些靶点原则上应该可以克服人类肿瘤抑制基因PTEN的影响。这项由ProlX制药公司进行的第一阶段研究的目标是确定并形成一组具有不同体外特性的4种类似物，这是体内最活跃的抗肿瘤化合物。ProlX制药公司将确定先导化合物对肿瘤移植瘤的活性，并获得化合物是否具有口服活性的初步信息。 拟议的商业应用：在美国，早期四分之一的死亡是由癌症引起的。美国的抗癌药物市场总额超过20亿美元。有必要确定新的和选择性的基于小分子的癌症疗法。该提案寻求对一组新的临床候选药物进行临床前评估，并启动一项第一阶段临床试验，最终用于治疗卵巢癌、胰腺前列腺癌和乳腺癌。

ProlX Pharmaceuticals has demonstrated that there is strong evidence for the following: 1) PtdIns-3-kinase and Akt are two novel validated molecular targets for anti-cancer drug discovery; 2) The targets are relevant to a variety for human cancers; and 3) Inhibiting the targets with a small molecule drug should in principle overcome the effects of the human tumor suppressor gene PTEN. The objective of the Phase I study, to be conducted by ProlX Pharmaceuticals, is to identify, form a group of 4 analogues with different in vitro properties, the most active in vivo anti- tumor compound. ProlX Pharmaceuticals will establish the activity of the lead compounds against tumor xenografts and obtain preliminary information whether the compounds are orally active. PROPOSED COMMERCIAL APPLICATIONS: One in early four deaths in the US is due to cancer. The overall cancer drug market exceeds $2 billion in the USA. There is significant need to identify novel and selective small molecule-based cancer therapies. The proposal seeks to undertake preclinical evaluation of a novel group of clinical candidates and initiate a Phase 1 Clinical Trial for its eventual use as a therapy against ovarian, pancreatic prostate and breast cancer.