AbstractProstate cancer that has progressed after androgen deprivation, abiraterone, and taxane therapy is challenging to treat successfully. Herein we report a dramatic response to continuous‐infusion 5‐fluorouracil (5‐FU) at a dose of 200 mg/m2 in a patient with rapidly progressive, heavily pretreated, metastatic castrate‐resistant prostate cancer. Baseline prostate‐specific antigen values declined from 1,890 ng/mL to <1 ng/mL after 5‐FU therapy. We hypothesized that prostate‐specific membrane antigen overexpression may result in cancer cells uniquely susceptible to antifolate therapies.
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