Sigurdson E R, Ridge J A, Daly J M
Surgery. 1986 Aug;100(2):285-91.
Tumor response rates after hepatic regional arterial chemotherapy infusion vary from 30% to 83% with little explanation for this variability. Drug clearance by the liver and plasma drug kinetics after arterial infusion have been described, but little is known about actual tumor drug uptake. This study measured fluorodeoxyuridine (FUdR) uptake in colorectal tumors metastatic to the liver and correlated these results with radionuclide flow scans and with tumor response to treatment. In 16 patients with unresectable colorectal hepatic metastases, FUdR (1 microCi/kg) and 99mTc-macroaggregated albumin (MAA) (6 mCi) were injected at a constant rate into the hepatic artery intraoperatively after insertion of a hepatic artery catheter. Liver and tumor biopsy specimens were obtained 2 and 5 minutes after infusion. 3H counts (representing drug uptake) and 99mTc disintegrations (representing blood flow) were measured by scintillation and gamma-counting. The tumor/liver ratios of FUdR and MAA were linearly related (r = 0.73, p less than 0.001). The mean tumor FUdR level was 9.2 +/- 8.9 nmol/gm, and the mean liver FUdR level was 24.5 +/- 16.8 nmol/gm. The mean FUdR tumor/liver ratio was 0.43 +/- 0.36. The extraction of FUdR by tumor was 49%. Thus substantially more drug was taken up by the liver than by the tumor after arterial infusion. There was considerable heterogeneity in FUdR uptake and MAA retention within both tissues. Tumor uptake of drug correlated significantly with MAA retention; higher FUdR levels were seen in tumors that appeared "hot" on radionuclide arterial perfusion scans. Tumor drug uptake was independent of lesion size and percentage of liver involvement.
肝动脉区域化疗灌注后的肿瘤反应率在30%至83%之间,对于这种变异性几乎没有解释。肝脏的药物清除和动脉灌注后的血浆药物动力学已有描述,但对实际肿瘤药物摄取了解甚少。本研究测量了转移至肝脏的结直肠癌肿瘤中氟脱氧尿苷(FUdR)的摄取情况,并将这些结果与放射性核素血流扫描以及肿瘤对治疗的反应相关联。在16例不可切除的结直肠癌肝转移患者中,在插入肝动脉导管后,术中以恒定速率将FUdR(1微居里/千克)和99mTc-大颗粒白蛋白(MAA)(6毫居里)注入肝动脉。在输注后2分钟和5分钟获取肝脏和肿瘤活检标本。通过闪烁计数和γ计数测量3H计数(代表药物摄取)和99mTc衰变(代表血流)。FUdR和MAA的肿瘤/肝脏比值呈线性相关(r = 0.73,p < 0.001)。肿瘤平均FUdR水平为9.2±8.9纳摩尔/克,肝脏平均FUdR水平为24.5±16.8纳摩尔/克。平均FUdR肿瘤/肝脏比值为0.43±0.36。肿瘤对FUdR的摄取率为49%。因此,动脉灌注后肝脏摄取的药物比肿瘤多得多。两种组织内的FUdR摄取和MAA滞留均存在相当大的异质性。肿瘤药物摄取与MAA滞留显著相关;在放射性核素动脉灌注扫描中显示为“热”的肿瘤中观察到更高的FUdR水平。肿瘤药物摄取与病变大小和肝脏受累百分比无关。