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.設計了靶向構建體及其藥物製劑,可改善活性劑的時空傳輸和/或改善生物分佈,該靶向構建體及其藥物製劑包含至少一個由治療劑、預防劑或診斷劑之類的活性劑經由可選內部連接基團與靶向基團連接而構成的結合物。提供了製備該靶向構建體及其製劑的方法。提供了為需要的對象施用該製劑的方法,例如用於治療或預防癌症或傳染性疾病。