Phase I and pharmacokinetic study of TZT-1027, a novel synthetic dolastatin 10 derivative, administered as a 1-hour intravenous infusion every 3 weeks in patients with advanced refractory cancer

Schöffski, Patrick; Thate, B; Beutel, G; Bolte, O; Otto, D; Hofmann, M; Ganser, A; Jenner, A; Cheverton, P; Wanders, J; Oguma, T; Atsumi, R; Satomi, M

doi:10.1093/annonc/mdh141

Phase I and pharmacokinetic study of TZT-1027, a novel synthetic dolastatin 10 derivative, administered as a 1-hour intravenous infusion every 3 weeks in patients with advanced refractory cancer

Author:

Schöffski, Patrick

Thate, B ; Beutel, G ; Bolte, O ; Otto, D ; Hofmann, M ; Ganser, A ; Jenner, A ; Cheverton, P ; Wanders, J ; Oguma, T ; Atsumi, R ; Satomi, M

Keywords:

dolastatins, phase i study, solid tumors, tzt-1027, potent antitumor agent, antimicrotubule agent, antineoplastic agents, Science & Technology, Life Sciences & Biomedicine, Oncology, phase I study, TZT-1027, POTENT ANTITUMOR AGENT, ANTIMICROTUBULE AGENT, Adult, Aged, Alopecia, Anorexia, Antineoplastic Agents, Area Under Curve, Constipation, Depsipeptides, Dose-Response Relationship, Drug, Fatigue, Female, Humans, Infusions, Intravenous, Leukopenia, Male, Middle Aged, Nausea, Neoplasms, Neutropenia, Oligopeptides, 1112 Oncology and Carcinogenesis, Oncology & Carcinogenesis, 3202 Clinical sciences, 3211 Oncology and carcinogenesis

Abstract:

Background: TZT-1027 is a synthetic dolastatin 10 analog with antineoplastic properties in various cell lines and tumor xenografts. The purpose of this phase I study was to evaluate the safety and toxicity, maximum tolerated dose, pharmacokinetics and pharmacodynamics, clinical and metabolic antitumor activity of TZT-1027 when given as a 1-h intravenous infusion every 3 weeks in patients with refractory solid tumors.