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Testosterone levels can be reduced within 24 hours with ketoconazole (Nizoral)—a drug approved by the FDA to treat fungal infections that also inhibits the synthesis of adrenal and testicular androgens. Ketoconazole is used only when lowering androgens rapidly might be beneficial (for example, to alleviate pain). It is used only in the short term, because it raises luteinizing hormone levels, which can cause testosterone levels to rise and disease progression to occur. Ketoconazole can also cause liver problems.

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Flutamide in combination with finasteride has been studied as a treatment option for advanced prostate cancer. Researchers hoped this combination would be effective, since finasteride lowers levels of dihydrotestosterone and could potentially enhance the ability of flutamide to block androgen action. But this approach is less effective than standard hormone therapy using an LH-RH analog or surgical castration.