MK-6482 as a potential treatment for von Hippel-Lindau disease-associated clear cell renal cell carcinoma

The oral HIF-2 α inhibitor MK-6482 in patients with advanced clear cell renal cell carcinoma (RCC): Updated follow-up of a phase I/II study.

(2021) Todd Michael Bauer et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase II study of the oral hypoxia-inducible factor 2α (HIF-2α) inhibitor MK-6482 for Von Hippel-Lindau (VHL) disease-associated clear cell renal cell carcinoma (ccRCC).

(2021) Othon Iliopoulos et al.   JOURNAL OF CLINICAL ONCOLOGY

LBA26 Phase II study of the oral HIF-2α inhibitor MK-6482 for Von Hippel-Lindau (VHL) disease-associated clear cell renal cell carcinoma (ccRCC): Update on RCC and non-RCC disease

(2020) R. Srinivasan et al.   ANNALS OF ONCOLOGY

Evaluation, diagnosis and surveillance of renal masses in the setting of VHL disease

(2020) Jad Chahoud et al.   WORLD JOURNAL OF UROLOGY

3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma

(2019) Rui Xu et al.   JOURNAL OF MEDICINAL CHEMISTRY

911PDA first-in-human phase I/II trial of the oral HIF-2a inhibitor PT2977 in patients with advanced RCC

(2019) E Jonasch et al.   ANNALS OF ONCOLOGY

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 Carcinoma

(2018) Kevin D. Courtney et al.   JOURNAL OF CLINICAL ONCOLOGY

A first-in-human phase 1 dose-escalation trial of the oral HIF-2a inhibitor PT2977 in patients with advanced solid tumors.

(2018) Kyriakos P. Papadopoulos et al.   JOURNAL OF CLINICAL ONCOLOGY

Pazopanib in patients with von Hippel-Lindau disease: a single-arm, single-centre, phase 2 trial

(2018) Eric Jonasch et al.   LANCET ONCOLOGY

Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)

(2018) Paul M. Wehn et al.   JOURNAL OF MEDICINAL CHEMISTRY

Von Hippel–Lindau disease: a single gene, several hereditary tumors

(2017) J. Crespigio et al.   JOURNAL OF ENDOCRINOLOGICAL INVESTIGATION

A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma

(2016) Eli M. Wallace et al.   CANCER RESEARCH

The prospect of precision therapy for renal cell carcinoma

(2016) Chiara Ciccarese et al.   CANCER TREATMENT REVIEWS

Targeting renal cell carcinoma with a HIF-2 antagonist

(2016) Wenfang Chen et al.   NATURE

On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models

(2016) Hyejin Cho et al.   NATURE

Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2

(2015) Thomas H. Scheuermann et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Inhibitors of the PAS-B Domain of the HIF-2α Transcription Factor

(2013) Jamie L. Rogers et al.   JOURNAL OF MEDICINAL CHEMISTRY

Allosteric inhibition of hypoxia inducible factor-2 with small molecules

(2013) Thomas H Scheuermann et al.   Nature Chemical Biology

Hypoxia-inducible factors: mediators of cancer progression and targets for cancer therapy

(2012) Gregg L. Semenza   TRENDS IN PHARMACOLOGICAL SCIENCES

Pilot trial of sunitinib therapy in patients with von Hippel-Lindau disease

(2011) E. Jonasch et al.   ANNALS OF ONCOLOGY

High-resolution genome-wide mapping of HIF-binding sites by ChIP-seq

(2011) J. Schodel et al.   BLOOD

Genetic and Functional Studies Implicate HIF1  as a 14q Kidney Cancer Suppressor Gene

(2011) C. Shen et al.   Cancer Discovery

Hypoxia-Inducible Factor 2 Regulates Hepatic Lipid Metabolism

(2009) E. B. Rankin et al.   MOLECULAR AND CELLULAR BIOLOGY

Integrative analysis of HIF binding and transactivation reveals its role in maintaining histone methylation homeostasis

(2009) X. Xia et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Artificial ligand binding within the HIF2  PAS-B domain of the HIF2 transcription factor

(2009) T. H. Scheuermann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

HIF-α Effects on c-Myc Distinguish Two Subtypes of Sporadic VHL-Deficient Clear Cell Renal Carcinoma

(2008) John D. Gordan et al.   CANCER CELL

Hypoxia-inducible factor-2 regulates vascular tumorigenesis in mice

(2008) E B Rankin et al.   ONCOGENE