Ketoconazole: A Novel and Rapid Treatment for Advanced Prostatic Cancer

Abstract

Ketoconazole is an orally administered broad-spectrum antifungal agent that acts through the inhibition of the steroid synthetic pathways. At high doses in humans ketoconazole can lower rapidly serum testosterone and maintain it in the castrate range with frequent administration. This property suggested that ketoconazole might be useful in the treatment of prostatic cancer. We report a case of prostatic cancer in which ketoconazole resulted in rapid and sustained reduction in serum androgens as well as rapid induction of a clinical remission. Ketoconazole may be a valuable agent in the treatment of prostatic cancer.

Leuprorelin depot injection: patient considerations in the management of prostatic cancer

“…In 1983, ketoconazole in high dose was identifi ed as able to produce castrate levels of androgens within 4-8 h of the fi rst dose (Trachtenberg and Point 1983), and represents an alternative treatment where urgent androgen ablation is required (Lowe and Bamberger 1990).…”

Pre-clinical evaluation of 1-nitroacridine derived chemotherapeutic agent that has preferential cytotoxic activity towards prostate cancer

“…9,10 Another serious problem with many chemotherapeutic agents is the side effects observed with aggressive high dose chemotherapy [11][12][13][14][15] that in severe cases extend to fatal myelo-suppression 16 and neuropathy. 17 Among several chemotherapeutic regimens being explored are docetaxel, in phase II trials, with response rates between 20-40%; 8,[18][19][20] estramustine plus taxane in phase III Southwest Oncology Group (SWOG) trial with objective responses in less than 20% of patients; 8,20,21 ketoconazole in Eastern Cooperative Oncology Group (ECOG)-sponsored phase III trial 8,[22][23][24] and carboplatin in phase II trials, showed significant prostate specific antigen (PSA) reductions, while less than 10% of patients exhibited a complete response. 25 Only a subpopulation of patients benefit from chemotherapy and since none of the agents are specific for CaP alongwith unacceptable toxicity profiles [30][31][32][33][34][35][36][37][38] makes it imperative to search for alternative chemotherapeutic agents.…”

Evaluation of the Possible Interaction of the Antifungal Triazole SCH 39304 with Oral Contraceptives in Normal Healthy Women

“…Ketoconazol has been shown to strongly decrease endogenous produc tion of gonadal and adrenocortical steroids and to in crease the biological half-life of coadministered drugs by inhibiting steroidogenic and drug-metabolizing cyto chrome P-450 enzymes [2][3][4][5][6]. Fluconazol, on the other hand, has been reported to interact neither with the endogenous endocrinological profile nor with the endo crine effects of coadministered oral contraceptives (OCs) [7], Since there are no such data available for SCH 39304, the present study was carried out.…”