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Antitumor activity of methotrexate-albumin conjugates in rats bearing a Walker-256 carcinoma by Andreas Wunder; Gerd Stehle; Hans Herrmann Schrenk; Gernot Hartung; Dieter Ludwig Heene; Wolfgang Maier-Borst; Hannsjörg Sinn is a Medicine article available to read on EtoBox.

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We have recently reported that albumin accumulates in solid tumors and serves there as a source of nitrogen and energy. Methotrexate-albumin conjugates [MTX( 1)-RSA] derivatized at a molar ratio of 1:1 differ favorably from original MTX in terms of plasma presence and tumor uptake. The purpose of this study was to evaluate the therapeutic efficacy of these novel conjugates in a comparative study with low m.w. MTX in Sprague-Dawley rats bearing a Walker-256 carcinoma. The maximum tolerated dose (MTD) for MTX and MTX(1)-RSA was determined (2 mg/kg based on MTX injected on days 1, 3 and 8). The tumor-bearing rats received injections of either the MTD or MTD/2 of MTX, MTXalbumin or mixtures containing the MTD/2 or MTD/4 of both MTX and MTX-albumin. No toxic side effects were observed. Cure rate and tumor growth retardation were slightly better for the conjugate compared with MTX alone in the MTD group (16 complete remissions vs. 14 of 20 rats). The best results were achieved for the combination treatment with MTX and MTX-albumin, with complete remission in all 20 rats. In conclusion, MTX-albumin conjugates show therapeutic activity in vivo without toxic side effects. Additive effects w

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Author

Andreas Wunder; Gerd Stehle; Hans Herrmann Schrenk; Gernot Hartung; Dieter Ludwig Heene; Wolfgang Maier-Borst; Hannsjörg Sinn

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley; Research Square; Test accounts (ISSN 0020-7136)

Published

1998

Language

EN

Field

Medicine (Health Sciences)