Zosuquidar逆转肝癌患者多药耐药性

Zosuquidar reverses P-glycoprotein-mediated multidrug resistance in patients with liver cancer

目的利用第三代P糖蛋白(Pgp)抑制剂zosuquidar.3HC1(LY335979)逆转人肝癌化疗耐药性。方法 60例未经治疗的原发性肝癌患者先后行两次99mTc-甲氧基异丁基异腈(99mTc-MIBI)单光子发射计算机断层成像术(SPECT)检测:经外周静脉注射20 mCi99mTc-MIBI后15、120 min行平面显像,半定量分析肿物部位的摄取比值(UR)。第1次SPECT检测后,口服zosuquidar.3HC1 500 mg/d,连续3 d后进行第2次SPECT检测,两次检测结果进行对照比较。结果 60例中,肿瘤部位99mTc-MIBI被排空50例(83.3%),经zosuquidar.3HC1治疗后第2次SPECT检测发现,肿瘤部位出现明显的99mTc-MIBI浓聚。结论 Zosuquidar.3HC1作为一种新型Pgp逆转剂可有效逆转临床肝癌患者的多药耐药性。

Objective To reverse multidrug resistance（MDR） by zosuquidar trihydrochloride（LY335979,zosuquidar.3HC1） in the patients with liver cancer.Methods 99mTc-MIBI single-photon emission computed tomography（SPECT） was performed at 15 min and 120 min after injection of 20 mCi 99mTc-MIBI,and early uptake,delayed uptake（L/Nd） and washout rate（L/Nwr） of 99mTc-MIBI were obtained in 60 patients with liver cancer.99mTc-MIBI SPECT examination was repeated after oral zosuquidar 500 mg/d for 3 days.The 99mTc-MIBI images of liver cancer before and after oral zosuquidar.3HC1 were compared.Results There was no 99mTc-MIBI uptake in the tumor lesions of 83.3%（50/60） patients with hepatocellular carcinoma,which was showen an aggregation of 99mTc-MIBI on 99mTc-MIBI SPECT immage after zosuquidar.3HC1 therapy.Conclusion MDR of the patients with liver cancer can be reversed effectively by zosuquidar.3HC1.