Tissue-specific targeting approaches may enhance a drug’s selectivity and also reduce unwanted toxicity. The folate receptor (FR) represents an accepted tumor biomarker that can functionally deliver folates as well as folate-based small molecule drug conjugates (SMDC) inside cells via a non-destructive endocytosis mechanism. Tumor response to folate-SMDCs is dependent on FR expression, which can be anatomically assessed in a non-invasive, real-time format using the folate-targeted companion imaging agent,<sup> 99m</sup>Tc-etarfolatide. In early 2006, the first folate-SMDC, EC145 (folate-desacetylvinblastine; vintafolide), entered the clinic for the treatment of refractory cancer. Together with etarfolatide which is used for FR-positive patient selection, vintafolide has been evaluated both as a single agent against a variety of tumor types, and in combination with Doxil® to treat platinum-resistant ovarian cancer patients (PRECEDENT and PROCEED trials), as well as with docetaxel to treat non-small cell lung cancer (TARGET trial). The outcomes of these groundbreaking trials will be reviewed, and future directions of this novel and personalized SMDC approach will be presented, including an update on advances with EC1456, the first tubulysin-based SMDC to be tested clinically.

<b>Award Address</b> (George and Christine Sosnovsky Award for Cancer Research sponsored by the George and Christine Sosnovsky Endowment Fund). Personalized medicine using targeted small molecule drug conjugates and companion imaging agents for cancer therapy

249th National Meeting (2015)

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Award Address (George and Christine Sosnovsky Award for Cancer Research sponsored by the George and Christine Sosnovsky Endowment Fund). Personalized medicine using targeted small molecule drug conjugates and companion imaging agents for cancer therapy