Mifepristone　(RU486)　is　a　born-for-woman　molecule　discovered　three　decades　ago.　Unlike　those　antihypertensive　and　antipsychotic　pharmaceutical　blockbusters,　this　abortifacient　offers　relatively　low　profit　potential.　Current　understanding　of　mechanism　of　action　of　mifepristone　and　its　on-going　clinical　trials　are　changing　our　views　on　the　drug　beyond　its　abortifacient　scope.　Here　we　briefly　review　its　metabolism　and　pharmacokinetic　properties　including　its　unique　enterohepatic　circulation,　its　mechanisms　of　actions　involving　antiprogesterone　and　antiglucocorticoid,　growth　inhibition　of　various　cancer　cell　lines,　suppression　of　invasive　and　metastatic　cancer　potential,　downregulation　of　Cdk2,　Bcl-2,　and　NF-kappa　B,　interference　of　heterotypic　cell　adhesion　to　basement　membrane,　and　cell　migration.　We　comprehensively　analyze　recent　results　from　preclinical　and　clinical　studies　using　mifepristone　as　an　anticancer　drug　for　breast,　meningioma,　and　gliomas　tumors　in　the　central　nervous　system,　prostate　cancer,　ovarian　and　endometrial　cancer,　and　gastric　adenocarcinoma.　Although　mifepristone　has　more　benefits　for　global　public　health　than　we　originally　thought,　its　effect　as　a　postmetastatic　chemotherapeutic　agent　is　limited.　Nonetheless,　owing　to　its　unique　safe,　metabolism　and　other　pharmacological　properties,　metapristone　(the　primary　metabolite　of　mifepristone)　may　have　potential　for　cancer　metastatic　chemoprevention.　©　2014　Wiley　Periodicals,　Inc.