Vintafolide

Vintafolide(EC-145) is a small molecule drug conjugate consisting of a small molecule targeting the folate receptor and a potent chemotherapy drug, vinblastine. IC50 value: Target: Microtubule/Tubulin; folate receptor in vitro: EC-145 selectively binds to cells that overexpress the folate receptor, causing dose-dependent cytotoxicity. Furthermore, coincubation of the KB human nasopharyngeal carcinoma cell line with EC-145 and doxorubicin resulted in synergistic antitumor activity [1]. in vivo: Experiments in mouse tumor xenograft models have confirmed the potency of EC-145 and the curative effects of the drug conjugate were demonstrated in an aggressive lymphoma xenograft model. In a phase I clinical trial in patients with advanced or metastatic solid tumors, adverse events were generally of moderate severity with the most frequent being fatigue, constipation and peripheral sensory neuropathy [1].