Why ketoconazole?

It's not just an antifungal. It also inhibits the enzymatic conversion of androgens in the adrenal glands. GnRH agonists and antagonists (and orchiectomy), like Lupron or Firmagon, shut off testicular production of androgens, but a small amount may continue to go on in the adrenals. It's considered a second-line therapy after ADT failure. Because it does much the same thing that Zytiga does (and Zytiga also inhibits intratumoral synthesis of androgens), it's largely been replaced, although some argue that it's just as effective and a whole lot cheaper. A related antifungal, Itraconazole, may turn out to be even better.

- Allen

thank you for those answers and links. If I recall, isn't itraconozole a bit harsher on the liver? I assume that if there was liver mets that these wouldn't be a good choice? Does this also block estrogens like the Lupron does?

Would zytiga be unsafe with liver mets?

Which brings another question about labs but will start a new thread.....

Both drugs can be toxic to the liver but it is not as prevalent with itraconazole as with ketoconazole. Ketoconazole recently received a black-box warning in regards to liver toxicity.

Paul