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Table 2 DNMT inhibitors in clinical trials for PCa

From: Epigenetic modulators as therapeutic targets in prostate cancer

Drug Clinical trial ID Phase Status Protocol Outcome Ref.
5-Azacytidine (Vidaza) NCT00384839 II Completed Patients with CRPC received 75 mg/m2 of 5-azacytidine for five consecutive days of a 28-day cycle. Patients were treated until clinical progression up to a maximum of 12 cycles. n = 36 5-Azacytidine modulates PSA (doubling time > 3 months) in 56 % of patients. Clinical progression-free survival of 12.4 weeks [130]
5-Aza-2-deoxycytidine (decitabine) II Completed 14 patients with metastatic prostate cancer recurrent after total androgen blockade and flutamide withdrawal received three doses of 5-aza-2-deoxycytidine infusion (75 mg/m2). Cycles of therapy were repeated every 5 to 8 weeks. n = 14 Two of 12 patients evaluable for response had stable disease with a time to progression of more than 10 weeks. Modest clinical activity [131]
5-Azacytidine, docetaxel, and prednisone NCT00503984 I/II Ongoing not recruiting mCRPC patients, who progressed during or within 6 months of docetaxel chemotherapy, were eligible. In phase I, 5-azacytidine and docetaxel were alternately escalated in a three weekly cycle. All patients received prednisone 5 mg twice daily continuously. n = 22 Toxicity: myelosuppression
Reduction in GADD-45 methylation on day 5
5-Azacytidine, phenylbutyrate NCT00006019 II Completed Patients received 5-azacytidine subcutaneously on days 1–7 and phenylbutyrate I.v. over 1–2 h on days 8–12. Additional course was repeated every 21 to 28 days in the absence of disease progression or unacceptable toxicity. n = 20 Not available