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PARPs in Prostate Cancer







                         PARP Inhibitors are Health Canada Approved or Under Investigation for Prostate Cancer






                                                  Olaparib                                Rucaparib                       Veliparib            Talazoparib              Niraparib



        MW                                           434.5                                   323.4                          244.3                   380.8                  320.4


        PARP1 IC   50                                5 nM                                   0.65 nM                         1.2 nM                0.56 nM                  3.8 nM


        PARP2 IC   50                                1 nM                                   0.08 nM                        0.41 nM                0.15 nM                  2.1 nM


        Trapping                                      ++                                       ++                              +                    ++++                     +++



                                        Monotherapy for mCRPC with a
                                      deleterious or suspected deleterious
        Approved for prostate           BRCA or ATM mutation(germline                          No                             No                     No                      No
        cancer                                  and/or somatic)
                                      Prior treatment with new hormonal
                                                     agent*




         *Eg, abiraterone, enzalutamide, darolutamide, or apalutamide



      mCRPC, metastatic castration-resistant prostate cancer
      Carney B et al. Nat Comm 2018;9:176.
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