Abstract
AbstractTirapazamine (TPZ, 3‐amino‐1,2,4‐benzotriazine 1,4‐dioxide), a representative hypoxia‐activated prodrugs (HAPs), has entered Phase II/III clinical trials. Despite a promising phase II clinical trial results, TPZ does not bring benefits to cancer therapy in most phase III clinical trials, which making the clinical trials failed. To improve its therapeutic effects, in this study, we synthesize a novel TPZ derivative, 3‐(3‐(5‐hydroxypentyl)ureido)benzo[e][1,2,4]triazine 1,4‐dioxide (TPZH), and covalently conjugated it to poly (L‐glutamic acid) (PLG) to obtain TPZH nanoparticles (TPZH‐NPs). The TPZH‐NPs shows prolonged blood circulation, enhanced tumor accumulation, and increased maximum tolerated dose (MTD) than TPZH. In addition, TPZH‐NPs exhibits significantly enhanced antitumor therapeutic efficiency than free TPZH against 4T1 breast tumors.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
