Cited by 396Drug Transport and Resistance MechanismsAntibiotic Resistance in BacteriaPharmacogenetics and Drug Metabolism

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Lapatinib (Tykerb, GW572016) Reverses Multidrug Resistance in Cancer Cells by Inhibiting the Activity of ATP-Binding Cassette Subfamily B Member 1 and G Member 2

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Dai, Chun-ling, Tiwari, Amit K., Wu, Chung-Pu, Su, Xiao-dong, Wang, Si-Rong, Liu, Dong-geng, Ashby, Charles R., Huang, Yan, Robey, Robert W., Liang, Yong-ju, Chen, Li-ming, Shi, Cheng-Jun, Ambudkar, Suresh V., Chen, Zhe-Sheng, Fu, Li-wu·2008·Cancer Research

DOI 10.1158/0008-5472.can-08-0499PMC PMC2652245

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Abstract

Lapatinib is active at the ATP-binding site of tyrosine kinases that are associated with the human epidermal growth factor receptor (Her-1 or ErbB1) and Her-2. It is conceivable that lapatinib may inhibit the function of ATP-binding cassette (ABC) transporters by binding to their ATP-binding sites. The aim of this study was to investigate the ability of lapatinib to reverse tumor multidrug resistance (MDR) due to overexpression of ABC subfamily B member 1 (ABCB1) and ABC subfamily G member 2 (ABCG2) transporters. Our results showed that lapatinib significantly enhanced the sensitivity to ABCB1 or ABCG2 substrates in cells expressing these transporters, although a small synergetic effect was observed in combining lapatinib and conventional chemotherapeutic agents in parental sensitive MCF-7 or S1 cells. Lapatinib alone, however, did not significantly alter the sensitivity of non-ABCB1 or non-ABCG2 substrates in sensitive and resistant cells. Additionally, lapatinib significantly increased the accumulation of doxorubicin or mitoxantrone in ABCB1- or ABCG2-overexpressing cells and inhibited the transport of methotrexate and E217βG by ABCG2. Furthermore, lapatinib stimulated the ATPase activity of both ABCB1 and ABCG2 and inhibited the photolabeling of ABCB1 or ABCG2 with [125I]iodoarylazidoprazosin in a concentration-dependent manner. However, lapatinib did not affect the expression of these transporters at mRNA or protein levels. Importantly, lapatinib also strongly enhanced the effect of paclitaxel on the inhibition of growth of the ABCB1-overexpressing KBv200 cell xenografts in nude mice. Overall, we conclude that lapatinib reverses ABCB1- and ABCG2-mediated MDR by directly inhibiting their transport function. These findings may be useful for cancer combinational therapy with lapatinib in the clinic. [Cancer Res 2008;68(19):7905–14]

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Authors: Dai, C.-L., Tiwari, A. K., Wu, C.-P., Su, X.-D., Wang, S.-R., Liu, D.-G., Ashby, C. R., Huang, Y., Robey, R. W., Liang, Y.-J., Chen, L.-M., Shi, C.-J., Ambudkar, S. V., Chen, Z.-S., & Fu, L.-W.
Affiliations: Sun Yat-sen University (CN)
St. John's University (US)
National Institutes of Health (US)
1State Key Laboratory for Oncology in South China, Cancer Center, Sun Yat-Sen University, Guangzhou, China;
ORCID: Tiwari, Amit K.
Wu, Chung-Pu
Su, Xiao-dong
Ashby, Charles R.
Huang, Yan
Robey, Robert W.
Ambudkar, Suresh V.
Chen, Zhe-Sheng
Venue: Cancer Research
Publisher: American Association for Cancer Research (AACR)
Published: 2008-09-30
Volume: 68
Issue: 19
Pages: 7905-7914
ISSN: 0008-5472 (ISSN-L)
1538-7445
DOI: 10.1158/0008-5472.can-08-0499
PMC: PMC2652245
OpenAlex: W2098064809
Cited by: 386
References: 54
Citations by year: 2026: 6 · 2025: 8 · 2024: 10 · 2023: 11 · 2022: 22 · 2021: 17 · 2020: 32 · 2019: 26 · 2018: 20 · 2017: 23 · 2016: 22 · 2015: 26 · 2014: 43 · 2013: 16 · 2012: 38
FWCI: 11.43
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Cancer Research (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: St. John's University (579-1110)
Sun Yat-sen University
National Institutes of Health
National Cancer Institute (Z01BC010030, Z01BC010622)
Topics: Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Health Sciences › Medicine › Microbiology (medical) › Antibiotic Resistance in Bacteria
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Keywords: lapatinib, multidrug resistance reversal, P-glycoprotein, ABCG2, ABC transporters, drug efflux, doxorubicin accumulation, methotrexate transport, paclitaxel, tyrosine kinase inhibitors, combination chemotherapy
MeSH terms: ATP Binding Cassette Transporter, Subfamily G, Member 2, Lapatinib, Adenosine Triphosphatases, Animals, Antineoplastic Combined Chemotherapy Protocols, Cells, Cultured, Dose-Response Relationship, Drug, Humans, Mice, Nude, Neoplasm Proteins, Neoplasms, Quinazolines, Transfection, Up-Regulation, Gene Expression Regulation, Neoplastic, Paclitaxel, Drug Resistance, Multiple, ATP Binding Cassette Transporter, Subfamily B, ATP-Binding Cassette Transporters, Drug Resistance, Neoplasm, ATP Binding Cassette Transporter, Subfamily B, Member 1, Xenograft Model Antitumor Assays, Tumor Burden, Mice

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Lapatinib (Tykerb, GW572016) Reverses Multidrug Resistance in Cancer Cells by Inhibiting the Activity of ATP-Binding Cassette Subfamily B Member 1 and G Member 2

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