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AIM: To explore whether P-glycoprotein (Pgp) and other pumps, multidrug resistance-associated protein (MRP) and lung resistance protein (LRP), could affect tumor accumulation and efflux of 99mTc-MIBI in liver cancer.METHODS: Surgically treated 78 liver cancer patients were included in this study. Before surgery, 99mTc-MIBI SPECT was performed 15 min and 120 min after injection of 20 mci 99mTc-MIBI, respectively. Early uptake, delayed uptake (L/Nd),and washout rate (L/Nwr) of 99mTc-MIBI were obtained.Expressions of Pgp, MRP and LRP were investigated with West blotting and immunohistochemistry. Messenger RNA (mRNA) level of Pgp, MRP and LRP was determined by RT-PCR.RESULTS: No 99Tc-MIBI uptakes in tumor lesions of 68 of 78 (87.2%) patients with hepatocellular carcinoma were found on 99mTc-MIBI SPECT. P-gp expression was observed in tumor tissues of the patients with no uptake of 99mTc-MIBI (P＜0.017). No appreciable correlation was found between liver cancer 99mTc-MIBI images and expression of MRP or LRP on the level of protein or mRNA.CONCLUSION: 99Tc-MIBI SPECT is noninvasive, and useful in predicting the presence of MDR1 gene-encoded Pgp in patients with hepatocellular carcinoma.