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Modulation of P‐glycoprotein activity by estramustine is limited by binding to plasma proteins

Background. Estramustine previously has been shown to interact with P‐glycoprotein and to restore intracellular accumulation of vinblastine and paclitaxel in cells overexpressing this drug transporter. However, the ability of estramustine to potentiate the cytotoxicities of several drugs was less than that expected. To resolve this apparent discordance, the authors examined the effects of serum on the actions of estramustine.