METHOD FOR OVERCOMING DRUG RESISTANCE OF EGFR MUTATION AND CANCEROUS STEMNESS OF HUMAN NON-SMALL CELL LUNG CARCINOMA

專利類型

發明

專利國別 (專利申請國家)

美國

專利申請案號

15/460,500

專利證號

US 9,980,967 B1

專利獲證名稱

METHOD FOR OVERCOMING DRUG RESISTANCE OF EGFR MUTATION AND CANCEROUS STEMNESS OF HUMAN NON-SMALL CELL LUNG CARCINOMA

專利所屬機關 (申請機關)

國立交通大學

獲證日期

2018/05/29

技術說明

目前Gefitinib為肺癌病人常用的臨床抗癌藥物，許多肺癌病人在剛開始使用Gefitinib時有很好的療效，但過一陣子後，藥效就會大幅地降低，肺癌細胞對Gefitinib產生抗藥性，因此需要透過開發更有效的藥物來進行治療。 1. 新穎性：SP101是可以克服當代EGFR T790M 突變 和癌幹性細胞生長 2. 可利用性：SP101會抑制p-EGFR, Survivin的表現和癌幹性蛋白Oct4的表現而抑制細胞的增生。並且SP101誘發肺癌細胞的凋亡和細胞生長的抑制作用比Gefitinib效果更好，相當有潛力做為化療藥物提供於癌症的治療。 3. 進步性及優勢： (1) SP101可克服上皮生長因子受體突變(EGFR-T790M)所導致抗藥性。 (2) SP101可克服人類肺癌細胞 (K-Ras-G12S)所導致抗藥性。 (3) SP101可克服癌幹性OCT4及Nanog所導致抗藥性。 This invention provides a Gefitinib derivative, Dodecyl-4-(4-(3-(4-(3-chloro-4-fluorophenylamino)-7-methoxyquinazolin-6 -yloxy)propyl)piperazin-1-yl)-4-oxobutanoate, hereinafter referred to as SP101. SP101 displays the anticancer ablity in inducing cell death and apoptosis in the Gefitinib-resistant EGFR (T790M) of H1975 cells. SP101 is more potent on the reduction of cell viability than Gefitinib and also induced more apoptosis than Gefitinib in the A549-ON which expressed Oct4 and Nanog proteins in lung cancer cells displaying cancerous stemness and drug resistance. In addition, SP101 is more effective in inducing cell death and apoptosis than Gefitinib in the PLC26 cells which were from clinical lung cancer patients having Gefitinib-drug resistance. More importantly, SP101 significantly inhibits drug-resistant tumor growth in the xenograft human lung tumors in nude mice.

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