title: Vintafolide: a novel targeted agent for epithelial ovarian cancer.
abstract: Vintafolide (EC145) is a novel folate-conjugated vinca alkaloid (desacetylvinblastine hydrazide; DAVBLH) that binds with high affinity to the folate receptor (FR), expressed in a majority of epithelial ovarian cancers. In preclinical studies, vintafolide had significant antiproliferative activity and tolerability. Phase I studies demonstrated an acceptable safety profile, with constipation being the dose-limiting toxicity. A Phase II study of vintafolide plus pegylated liposomal doxorubicin (PLD) versus PLD alone in patients with platinum-resistant ovarian cancer showed a statistically significant improvement in progression-free survival with combination therapy. (99m)Tc-etarfolatide, a diagnostic radiopharmaceutical, determines FR status, which allows determination of those patients most likely to benefit from treatment with vintafolide. A Phase III study evaluating vintafolide plus PLD versus PLD alone in patients with platinum-resistant ovarian cancer is currently underway.
authors.affiliation: Medical University of South Carolina, Division of Gynecologic Oncology, 96 Jonathan Lucas Street, CSB 634, MSC 619, Charleston, SC, USA.
authors.forename: Whitney S
authors.initials: WS
authors.lastname: Graybill
authors.forename: Robert L
authors.initials: RL
authors.lastname: Coleman
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D000077216:Carcinoma, Ovarian Epithelial; D002986:Clinical Trials as Topic; D004353:Drug Evaluation, Preclinical; D005260:Female; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D058990:Molecular Targeted Therapy; D009375:Neoplasms, Glandular and Epithelial / Q000175:diagnosis / Q000188:drug therapy*; D010051:Ovarian Neoplasms / Q000175:diagnosis / Q000188:drug therapy*; D016896:Treatment Outcome; D014748:Vinca Alkaloids / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; C520389:EC145; D014748:Vinca Alkaloids; D005492:Folic Acid