Photocontrolled　therapeutic　release　holds　great　promise　due　to　its　versatile　manipulability,　superb　spatiotemporal　precision　and　minimal　tissue　invasiveness　in　biomedical　purposes.　However,　most　of　light-responsive　platforms　thus　far　have　relied　on　UV　or　visible　light　which　substantially　limit　the　potential　applicability　in　living　animals.　In　recent　decades,　near-infrared　(NIR)　light-mediated　theranostic　upconversion　nanocomposites　(UCNCs)　that　integrate　conventional　UV/Vis-sensitive　materials　and　classic　lanthanide-doped　upconversion　nanoparticles　(UCNPs)　have　significantly　promoted　the　development　of　deep-tissue　photoreleasable　therapeutics　in　vivo.　Herein,　we　seek　to　review　current　NIR　upconversion　triggered　photorelease　techniques　and　their　diverse　applications　in　the　biological　regulation,　as　well　as　diseases　therapy.　In　addition,　the　future　perspectives　and　challenges　for　advancing　UCNCs　based　NIR　photoreleasable　nanotherapeutics　into　clinical　translations　are　proposed.