Ketoconazole is the perfect alternative for initial empirical hormonal therapy for these patients
Ketoconazole, an imidazole antifungal agent with inhibitory activity of the cytochrome P450 17A1 complex (CYP17), has demonstrated clinical activity in patients with metastatic castration-resistant prostate cancer (mCRPC) in prospective clinical trials (1, 2) and has been used for decades in the treatment of this disease
Ketoconazole has been used in high doses for the treatment of advanced prostate cancer and for Cushing's syndrome when other treatment options have failed
Figure 1
Experimental design: Chemotherapy-naïve patients with progressive metastatic castration-resistant prostate cancer (mCRPC) and prior ketoconazole therapy ≥28 days received abiraterone acetate 1,000 mg daily and prednisone 5 mg twice daily
Lenalidomide is an antiangiogenic and immunomodulatory agent with broad antitumor activity
Mild and often transient rises in serum liver enzyme activities are not uncommon in patients taking ketoconazole; the incidence is reported to be about 10–15% [24, 25], a higher incidence than was originally thought [26]
1,2 The majority of testosterone is primarily bound to albumin and sex hormone binding globulin, though some is
Since then, targeting of the androgen–androgen receptor (AR) signaling pathway either by blocking androgen synthesis or blocking androgenic effects has been standard of care
Abiraterone acetate is a potent, selective, and orally bioavailable small molecule inhibitor of CYP17, an enzyme that catalyzes two key serial reactions (17 alpha hydroxylase and 17,20 lyase) in androgen and estrogen biosynthesis
Prostate cancer continues to be a significant burden on men's health
Purpose: Increasing evidence indicates that enhanced intratumoral androgen synthesis contributes to prostate cancer progression after androgen deprivation therapy