RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR . RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1 . RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy . Anticancer activity .