Targeted constructs and pharmaceutical formulations thereof, comprising at least one conjugate of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via an optional internal linker moiety have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the targeted constructs and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.