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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 chemosensitivity of human hepatocellular carcinoma using the third generation of Pgp inhibitor zosuquidar.3HC1 (LY335979). Methods Totally 99mTc-methoxyisobutylisonitrile (99mTc-MIBI) single photon emission computed tomography (SPECT) was performed in 60 untreated patients with primary liver cancer. After 20 mCi99mTc-MIBI 15,120 min line plane imaging, semi-quantitative analysis of tumor site uptake ratio (UR). The first SPECT test, oral zosuquidar.3HC1 500 mg / d, 3 consecutive days after the second SPECT test, the two test results were compared. Results In 60 cases, the 99mTc-MIBI in the tumor site was evacuated in 50 cases (83.3%). The second SPECT detected by zosuquidar.3HC1 showed significant 99mTc-MIBI accumulation in the tumor site. Conclusion Zosuquidar.3HC1 as a new Pgp reversal agent can effectively reverse the multidrug resistance in clinical liver cancer patients.