Table 2.

Novel cytochrome P450-based therapeutic options

TherapeuticDevelopment statusAntitumor activityMode of interaction with P450
Resveratrol (34)PreclinicalIn vitro activation by CYP1B1 to anticancer metaboliteProdrug activated by CYP1B1
Aryl oxime (35, 36)PreclinicalIn vitro activation by CYP1B1 to nitric oxide resulting in cell deathProdrug activated by CYP1B1
Phortress (38)Phase I clinical trialBreast cancerProdrug activated by CYP1A1, CYP1B1
AQ4N (45)Phase I clinicalRadioresistant tumorsBioreductive prodrug activated by CYP3A4, CYP1A1, and CYP1B1
MetXia (52, 53)Phase I/II clinical trialBreast cancerRetroviral vector encoding human CYP2B6 designed to activate cyclophosphamide at site of tumor
R116010 (65)PreclinicalHormone-independent prostate and breast tumorsSmall molecule inhibitor of CYP26A
AVI-4557 (70)Phase I clinical trialAdvanced cancerCYP3A4 antisense construct
Zyc300 (79)Phase I/II clinical trialBreast, ovarian, colorectal, and prostate cancerCYP1B1 vaccine