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Laboratoires GLAXO, Centre de Recherches, 25 avenue du Quebec, 91951 Les Ulis Cedex, France
1 To whom requests for reprints should be addressed.
N-{4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)-ethyl]-phenyl}-9,10-dihydro-5-methoxy-9-oxo-4-acridine carboxamide (GF120918) has been selected from a chemical program aimed at identifying an optimized inhibitor of multidrug resitance (MDR). The potency of GF120918 is assessed by dose-dependent sensitization of CHRC5, OV1/DXR and MCF7/ADR cells to the cytotoxicity of doxorubicin and vincristine respectively: GF120918 fully reverses multidrug resistance at 0.05 to 0.1 µM and is half maximally active at 0.02 µM. The spectrum of drugs sensitized by GF120918 coincides with those having the classical MDR phenotype. In CHRC5 cells, 0.01–0.1 µM GF120918 enhances the uptake of [3H]daunorubicin and blocks the efflux from preloaded cells. It is also shown that GF120918 is still active several hours after being taken away from the culture medium showing that it is not, like verapamil, effluxed rapidly by P-glycoprotein. GF120918 effectively competes with [3H]azidopine for binding P-glycoprotein, pointing to this transport membrane protein as its likely site of action.
After i.v. administration to mice, GF120918 penetrates thoroughly various organs that have a tissue level/blood level ratio above 10. It is eliminated from organs and blood with a half-time of approximately 2.7 h. It is well absorbed after p.o. administration.
In mice implanted i.p. with the MDR P388/Dox tumor, a single i.v. or p.o. dose of GF120918 restores sensitivity of the tumor to a single i.p. dose (5 mg/kg) of doxorubicin administered 1 h later. A statistically significant effect is observed at 1 mg/kg GF120918 i.v. and maximal effect is reached at 5 mg/kg. Similarly, whereas neither drug alone is effective, GF120918 (10 mg/kg i.p.) associated with doxorubicin (5 mg/kg i.p.) inhibits the growth of the moderately MDR C26 tumor implanted s.c. as assessed by tumor size at day 19. GF120918 does not modify significantly the distribution or the elimination of doxorubicin in mice ruling out the possibility that the antitumor effects seen might be explained by pharmacokinetic interactions.
The costs of publication of this article were defrayed in part by the payment of page charges. This article must therefore be hereby marked advertisement in accordance with 18 U.S.C. Section 1734 solely to indicate this fact.
Received 3/19/93. Accepted 7/23/93.
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G. D. Luker, K. R. Nilsson, D. F. Covey, and D. Piwnica-Worms Multidrug Resistance (MDR1) P-glycoprotein Enhances Esterification of Plasma Membrane Cholesterol J. Biol. Chem., March 12, 1999; 274(11): 6979 - 6991. [Abstract] [Full Text] [PDF]
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M. C. Cabot, A. E. Giuliano, T.-Y. Han, and Y.-Y. Liu SDZ PSC 833, the Cyclosporine A Analogue and Multidrug Resistance Modulator, Activates Ceramide Synthesis and Increases Vinblastine Sensitivity in Drug-sensitive and Drug-resistant Cancer Cells Cancer Res., February 1, 1999; 59(4): 880 - 885. [Abstract] [Full Text] [PDF]
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G. D. Luker, T. P. Flagg, Q. Sha, K. E. Luker, C. M. Pica, C. G. Nichols, and D. Piwnica-Worms MDR1 P-glycoprotein Reduces Influx of Substrates without Affecting Membrane Potential J. Biol. Chem., December 21, 2001; 276(52): 49053 - 49060. [Abstract] [Full Text] [PDF]
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