Medicine and Health Sciences Commons^™

Evaluation Of The Pharmacokinetic-Pharmacodynamic Relationship, Metabolism And Plasma Protein Binding Of The Novel Antitumor Agent, 2-Methoxyestradiol (2me2), Following Oral Administration In Patients With Solid Tumors., Nehal Jagdish Lakhani

Theses and Dissertations

The goal of this study was to determine safety, tolerability and pharmacokinetics of 2ME2 in patients with solid tumors and determine maximum tolerated dose (MTD). The following hypotheses were tested: 1) 2ME2 will be well tolerated in clinic when given orally and will have quantifiable effects on the ex vivo markers of angiogenesis and apoptosis; 2) 2ME2 will exhibit linear pharmacokinetics; 3) Plasma protein binding will be extensive and linear; 4) Sulfation will be the major metabolic pathway for 2ME2.This was a phase I dose escalation study. Twenty patients with refractory solid tumors were enrolled. 2ME2 was administered orally starting …