[HTML][HTML] Phase I dose-escalation trial of PT2385, a first-in-class hypoxia-inducible factor-2α antagonist in patients with previously treated advanced clear cell renal cell …

KD Courtney, JR Infante, ET Lam… - Journal of Clinical …, 2018 - ncbi.nlm.nih.gov
KD Courtney, JR Infante, ET Lam, RA Figlin, BI Rini, J Brugarolas, NJ Zojwalla, AM Lowe…
Journal of Clinical Oncology, 2018ncbi.nlm.nih.gov
Purpose The von Hippel-Lindau tumor suppressor is inactivated in the majority of clear cell
renal cell carcinomas (ccRCCs), leading to inappropriate stabilization of hypoxia-inducible
factor-2α (HIF-2α). PT2385 is a first-in-class HIF-2α antagonist. Objectives of this first-in-
human study were to characterize the safety, pharmacokinetics, pharmacodynamics, and
efficacy, and to identify the recommended phase II dose (RP2D) of PT2385.
Abstract
Purpose
The von Hippel-Lindau tumor suppressor is inactivated in the majority of clear cell renal cell carcinomas (ccRCCs), leading to inappropriate stabilization of hypoxia-inducible factor-2α (HIF-2α). PT2385 is a first-in-class HIF-2α antagonist. Objectives of this first-in-human study were to characterize the safety, pharmacokinetics, pharmacodynamics, and efficacy, and to identify the recommended phase II dose (RP2D) of PT2385.
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