The invention provides a drug conjugate comprising: 1) a therapeutic agent that comprises a phosphate, phosphonate, carboxy, or phosphoramidate group, and 2) a fluorescent group linked to the phosphate, phosphonate, carboxy, or phosphoramidate group to form the corresponding ester and salts thereof. The conjugates are useful for therapy and as probes. The invention also provides therapeutic methods for treating diseases with conjugates of the invention as well as methods for determining optimal dosages of a conjugate or a therapeutic agent for a given patient using a conjugate of the invention.

Metal-organic frameworks (MOFs) comprising photosensitizers are described. The MOFs can also include moieties capable of absorbing X-rays or other ionizing irradiation energy and/or scintillation. Optionally, the photosensitizer or a derivative thereof can form a bridging ligand of the MOF. Further optionally, the MOF can comprise inorganic nanoparticles in the cavities or channels of the MOF or can be used in combination with an inorganic nanoparticle. Also described are methods of using MOFs and/or inorganic nanoparticles in photodynamic therapy, X-ray induced photodynamic therapy, radiotherapy, radiodynamic therapy, or in radiotherapy-radiodynamic therapy, either with or without the co-administration of one or more immunotherapeutic agent and/or one or more chemotherapeutic agent.

A pharmaceutical composition includes a plurality of metal nanoparticles and at least one therapeutic agent. Each of the metal nanoparticles includes a core and a stabilizing agent coated on a surface of the core. The at least one therapeutic agent is attached to the stabilizing agent of the metal nanoparticles. Each of the therapeutic agent is an amphiphilic compound and has at least one hydrophobic chain interacting with the stabilizing agent. The pharmaceutical composition may further include a polymer shell encapsulating the metal nanoparticles and the therapeutic agent for enabling controlled release of the therapeutic agent. The pharmaceutical compositions are bifunctional and may be used for diagnosing and treating cancer. Methods for using the pharmaceutical compositions in conjunction with radiation therapy to diagnose and treat cancer are also provided.

Devices, materials, compounds, systems, and processes for Cherenkov-Activated Nuclear-Targeted Photodynamic Therapy that involves generating Cherenkov light within the tissue of a target volume and using this light to activate photosensitizing material that is located in the nucleus of cells of the target volume.

The present invention includes new medical techniques involving radiation and electromagnetic actuation of reagents deployed and directed within bodily fluids (e.g., the bloodstream, digestive tract, or lymph ducts) of a patient. In one aspect of the invention, a medical reagent and/or particle is provided with multiple dipoles, oriented differently in three-dimensional space, allowing a remote control system to drive the acceleration and three-dimensional orientation of the medical agent or particle according to a three-dimensional path. In some embodiments, the medical reagent and/or particle is energized remotely to an activation energy level, and then driven into the treatment target. The design of each small-scale machine may include different sub-devices and electrostatic charges or magnetic dipoles, at different surface or internal locations. In some aspects, the sub-devices include actuable housings and other sub-devices, to deliver drugs or other factors at specific locations commanded by the control system or a user.

Provided is a Pt(IV) complex. As a prodrug, the Pt(IV) complex is activated by irradiation to release a Pt(II) complex for the treatment of tumors. Also provided is a pharmaceutical composition including the Pt(IV) complex, and the use of the Pt(IV) complex in the preparation of a drug for treating tumors by means of irradiation activation. Further provided is a kit including the Pt(IV) complex and the description, wherein the description indicates that radiotherapy is performed after administration to treat tumors.

Described herein is photocaging methodology using ruthenium (II) complexes with 7-deazahypoxanthine-based anticancer agents. Specifically, 7-deazahypoxanthines are converted into photoactivatable chemotherapeutic agents for the controlled release of these toxic agents selectively into tumor tissue upon irradiation with light.

Metal-organic frameworks (MOFs) comprising photosensitizers are described. The MOFs can also include moieties capable of absorbing X-rays and/or scintillation. Optionally, the photosensitizer or a derivative thereof can form a bridging ligand of the MOF. Further optionally, the MOF can comprise inorganic nanoparticles in the cavities or channels of the MOF or can be used in combination with an inorganic nanoparticle. Also described are methods of using MOFs and/or inorganic nanoparticles in photodynamic therapy or in X-ray induced photodynamic therapy, either with or without the co-administration of one or more immunotherapeutic agent and/or one or more chemotherapeutic agent.

Disclosed is a method for increasing susceptibility of cancer cells to ionizing radiation by delivering to the cells a radiosensitizing agent that has one of the following properties: it perturbs the process of chromosome segregation thereby increasing chromosome missegregation; or (b) it is an inhibitor of an agent that promotes faithful chromosome segregation induces numeric chromosome instability in said cells and this instability is induced substantially simultaneously with or closely prior to or closely after irradiating the cells. Examples of such radiosensitizing agent include inhibitors of one or more of the following: Kif2b, MCAK, MPS1, Eg5/Kinesin-5 5, Polo-like kinase 4, MCAK, Bub1 and Hec1. Such agents specifically target proteins involved in maintaining or promoting faithful chromosome segregation.

Provided herein are compositions including aptamers capable of binding to and/or inhibiting the activity of nucleolin. Methods of treating cancer in a subject by administering such compositions are also provided.