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ABSTRACT
Title |
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Modulation of P-Glycoprotein Mediated Multidrug Resistance (Mdr) in Cancer Using Chemosensitizers. |
Authors |
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Velingkar V.S., Dandekar V.D. |
Keywords |
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Multidrug resistance, P-glycoprotein, P-gp modulators,P-gp inhibitors |
Issue Date |
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March 2010 |
Abstract |
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Multidrug resistance (MDR) is one of the main obstacles in the chemotherapy of cancer. MDR is associated with the over expression of P-glycoprotein (P-gp), resulting in increased efflux of chemotherapy from cancer cells. Inhibiting P-gp as a method to reverse MDR in cancer patients has been studied extensively, but the results have generally been disappointing. First-generation agents were limited by unacceptable toxicity, whereas second-generation agents had better tolerability but were confounded by unpredictable pharmacokinetic interactions and interactions with other transporter proteins. Third-generation inhibitors have high potency and specificity for P-gp. Furthermore, pharmacokinetic studies to date have shown no appreciable impact on drug metabolism and no clinically significant drug interactions with common chemotherapy agents. Third-generation P-gp inhibitors have shown promise in clinical trials. The continued development of these agents may establish the true therapeutic potential of P-gp-mediated MDR reversal. |
Page(s) |
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104-111 |
ISSN |
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0975-9492 |
Source |
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Vol. 1, No.2 |
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