Targeting drugs for delivery and release has the potential to increase the efficacy of treatment. A bifunctional linker, A-Z- @entity69095 Linker was used to create a targeted prodrug, A-Z- @entity69095 310. A-Z- @entity69095 Linker links to a potent chemotherapeutic agent, @entity1311 , via an energy-reversible @entity13507 bond and also binds a targeting agent, the monoclonal antibody trastuzumab (Herceptin). This study demonstrates the effectiveness of a single-treatment use of A-Z- @entity69095 310 in decreasing @entity5 volume and @entity5 cell density of @entity1 @entity1722 -positive @entity1 mammary @entity5 cells implanted in scid @entity19 , compared to treatment with simultaneously administered trastuzumab and @entity1311 and with saline control. After treatment with A-Z- @entity69095 310, some @entity19 received light exposure at 6 h for 5 min adjacent to the @entity5 to cause light-accelerated release of @entity1311 . Changes in @entity5 volume were measured for 28 days following treatment; changes in histology were measured at 31 days. Animals treated with A-Z- @entity69095 310, then light, showed dose-dependent decreases in @entity5 volume and @entity5 cell density which were more rapid and extensive than those seen with A-Z- @entity69095 310 without light or a 10-fold higher concentration of co-administered trastuzumab plus @entity1311 . This suggests that targeted delivery of @entity1311 using A-Z- @entity69095 310 kills @entity5 cells by localized release of @entity1311 at the @entity5 site, which can be accelerated by light treatment. These results indicate that a targeted prodrug therapy containing trastuzumab as the targeting agent and A-Z- @entity69095 - @entity1311 as the prodrug results in a conjugate that is more effective in killing @entity5 cells than equivalent concentrations of co-administered trastuzumab and @entity1311 . Targeting of a drug can reduce the dose needed for effective therapy and can increase local bioavailability. This makes targeted therapy using an A-Z- @entity69095 prodrug delivery system feasible for treating both primary and @entity3 .

Targeted prodrug treatment of XXXX -positive breast tumor cells using trastuzumab and @entity1311 linked by A-Z- @entity69095 Linker.

@entity1 :: ('9606', 'Species') :: ['BT-474', 'human'] @entity5 :: ('MESH:D009369', 'Disease') :: ['tumor'] @entity19 :: ('10090', 'Species') :: ['mice'] @entity1311 :: ('MESH:D017239', 'Chemical') :: ['paclitaxel'] @entity69095 :: ('100188835', 'Gene') :: ['CINN'] @entity3 :: ('MESH:D009362', 'Disease') :: ['metastatic tumors'] @entity13507 :: ('CHEBI:35701', 'Chemical') :: ['ester'] @entity1722 :: ('2064', 'Gene') :: ['HER-2']
@entity1722 :: (2064,Gene) :: ['HER-2']
