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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

[273]

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