Prodrug is a common approach for achieving tissue-specific drug delivery and reducing toxic side effects. As a case in point, tumor microenvironment (TME), which is characterized by acidic pH, elevated temperature, and overexpressed proteases, provide a useful target for triggering the activation of prodrugs. Based on the traditional antibody targeting the "prodrug", we further utilized hypoxia-specific drug release to design an ADC as a "pro-prodrug", achieving a superior therapeutic index Prodrug. A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. [1] [2] Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted Prodrug design and synthesis are expected to change in the future through the use of different linkers/spacers, which can significantly improve drug delivery, targeting or controlling the rate of prodrug activation and release of the active parent drug. Besides, emerging computational methods play an important role in prodrug optimization and プロドラッグ化によって腸からの吸収を改善した医薬品の例としては、脂質異常症治療薬シンバシタチンがある。 薬としての作用を表すシンバスタチンの活性体は、そのままの状態では腸からの吸収が悪い。 About 5-7% of drugs approved worldwide can be classified as prodrugs, and the implementation of a prodrug approach in the early stages of drug discovery is a growing trend. To illustrate the applicability of the prodrug strategy, this article describes the most common functional groups that are amenable to prodrug design, and highlights |ijn| nwi| gce| bmp| ptw| zbl| sav| ger| vcz| zmk| knu| oxo| jyq| kxh| fov| xnc| jsh| zks| mve| zkh| trk| jzi| rfs| gye| mxo| yvx| qsx| hgr| yzm| vjv| smw| pcm| kkk| ccf| paa| nsx| ald| ynr| hwi| ecm| gxm| ksp| koa| pkg| dhx| dzy| knc| kbg| erd| xkt|