Table 1: Characteristics of selected FDA-approved bone targeting agents in mCRPC.

Zoledronic acid DenosumabSr-89Sm 153Ra 223

ClassBisphosphonateMonoclonal antibody against RANK-LPure Beta-emitter radiopharmaceuticalBeta and Gamma-emitter radiopharmaceuticalAlpha-emitter

Major side effectsFlu-like symptoms, hypocalcemia, osteonecrosis of the jawHypocalcemia, osteonecrosis of the jawmyelosuppressionmyelosuppressionNausea, vomiting, diarrhea.

Half-life (days)625.4501.9 11.4

Landmark randomized trial
Saad et al., 2002, 2004 [5, 6]
Fizzazi et al., 2011 [16]
Lewington et al., 1991 [17]
Serafini et al., 1998 [18]
Sartor et al., 2004, 2007 [19, 20]
Parker et al., 2012 [21]
 ArmsZoledronic acid versus placebo ( )
Denosumab versus zoledronic acid ( )Sr-89 versus placebo ( )
Sm 153 versus placebo ( )
Ra 223 versus placebo ( )
 EndpointSignificant decrease and delay in SREs and bone pain Significant delay in SREsSignificant decrease in bone painSignificant decrease in bone painSignificant increase in OS, PSA drop

Status FDA approved 2002FDA approved 2010FDA approved
1993
FDA approved 1997FDA approved 2013

AdministrationIntravenousSubcutaneousIntravenousIntravenousIntravenous