In an effort to develop effective alternative strategies that increase the therapeu-tic efficacy and minimize the systemic toxicity of chemotherapeutic agents,moreefforts are being directed towards the investigation of dietary supplements andother phytotherapeutic agents for their synergistic efficacy in combination withanticancer drugs.One such agent is silibinin,which has shown promisingchemopreventive and anticancer effects in various in vitro and in vivo studies.The present review summarizes the effects of the combination of silibinin andchemotherapeutic drugs on the growth inhibition,cell cycle regulation,andapoptosis induction in prostate,breast,and lung cancer systems.Together,theresults indicate a synergistic effect of silibinin on growth inhibition,reversal ofchemoresistance,apoptosis induction,and a strong increase in G_2-M checkpointarrest when given in combination with these drugs.These results are highlysignificant with respect to the combined chemotherapy approach,wherein thecriteria for combination is that the response has to be synergistic and that thedrugs should not share common mechanisms of resistance and not overlap intheir major side-effects. In an effort to develop effective alternative strategies that increase therapeu-tic efficacy and minimize the systemic toxicity of chemotherapeutic agents, moreefforts are being directed to the investigation of dietary supplements andother phytotherapeutic agents for their synergistic efficacy in combination withanticancer drugs. One such agent is silibinin, which has shown promising in anticoagulation and anticancer effects in various in vitro and in vivo studies. The present review summarizes the effects of the combination of silibinin and chemotherapeutic drugs on the growth inhibition, cell cycle regulation, andapoptosis induction in prostate, breast, and lung cancer systems.Together, the results show a synergistic effect of silibinin on growth inhibition, reversal of chemoresistance, apoptosis induction, and a strong increase in G_2-M checkpointarrest when given in combination with these drugs. These results are highlysignificant with respect to the combined chemotherapy approach, Where thecriteria for combination is that the response has to be synergistic and that the drugs should not share common mechanisms of resistance and not overlap intheir major side-effects.