The　construction　of　multifunctional　theranostic　nanoplatforms　to　integrate　accurate　imaging　and　enhanced　therapy　to　treat　tumors　is　highly　attractive　but　remains　a　challenge.　Here,　we　developed　a　molybdenum　disulfide　(MoS2)-based　hyaluronic　acid　(HA)-functionalized　nanoplatform　capable　of　achieving　the　targeted　co-delivery　of　the　gadolinium　(Gd)-based　contrast　agents　(CAs)　and　the　anticancer　drug　gefitinib　(Gef)　for　magnetic　resonance　imaging　(MRI)　and　synergetic　chemo-photothermal　therapy　of　tumors.　Gd3+　ions　were　coupled　to　HA-grafted　MoS2　nanosheets　with　diethylenetriaminepentaacetic　acid　(DTPA)　as　a　linker,　followed　by　the　incorporation　of　Gef.　The　resulting　MoS2-HA-DTPA-Gd/Gef　exhibited　enhanced　relaxivity,　3.3　times　greater　than　that　of　the　commercial　CA　DTPA-Gd,　which　facilitated　the　MRI　in　vivo.　Moreover,　the　nanoplatform　effectively　converted　the　absorbed　near-infrared　(NIR)　light　into　heat,　which　not　only　induced　the　photothermal　ablation　of　cancer　cells　but　also　triggered　the　release　of　Gef　from　MoS2-HA-DTPA-Gd/Gef,　enabling　the　synergetic　chemo-photothermal　therapy.　The　results　of　in　vitro　and　in　vivo　experiments　revealed　that　MoS2-HA-DTPA-Gd/Gef　upon　NIR　irradiation　effectively　blocked　the　phosphatidylinositol　3　kinase　(PI3K)/protein　kinase　B　(Akt)　signaling　pathway　and　activated　apoptosis-related　proteins　to　induce　cell　apoptosis　and　suppress　cell　proliferation,　thus　inhibiting　the　tumor　growth　in　lung　cancer　cell-bearing　mice.　Taken　together,　this　multifunctional　theranostic　nanoplatform　has　significant　promise　for　the　diagnosis　and　treatment　of　cancer.　©　2019