Hypoxia-inducible factor (HIF) inhibitors: a patent survey (2016-2020)

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Title
Hypoxia-inducible factor (HIF) inhibitors: a patent survey (2016-2020)
Author(s)
Hyun Seung Ban; Y Uto; H Nakamura
Bibliographic Citation
Expert Opinion on Therapeutic Patents, vol. 31, no. 5, pp. 387-397
Publication Year
2021
Abstract
Introduction: Hypoxia-inducible factor (HIF) is a master regulator of oxygen homeostasis. The increased expression of genes targeted by HIF is associated with many human diseases, including ischemic cardiovascular disease, stroke, chronic lung disease, and cancer. Areas covered: This patent survey summarizes the information about patented HIF inhibitors over the last 5 years. Expert opinion: HIF inhibitors have shown promise for the treatment of hypoxic pulmonary hypertension, a circadian rhythm disorder, calcific aortic valve disease, cerebrovascular accident, and heterotopic ossification. In addition, HIF-2α inhibitors can be used for the treatment or prevention of iron overload disorders, Crohn’s disease, ulcerative colitis, and thyroid eye disease, or to improve muscle generation and repair. PT2385 completed phase I clinical trials for the treatment of clear cell renal cell carcinoma. It exerted a higher synergistic inhibitory effect on tumor growth in combination with anti?PD-1 antibody, in comparison with each treatment alone, indicating that effective immunotherapy for solid tumors counteracts of the immunosuppression induced by hypoxia. Therefore, considering the effects of hypoxia on cancer cells, stromal cells, and effector immune cells, it is important to develop inhibitors of molecular pathways activated by hypoxia for successful treatments.
Keyword
CancerHypoxia-inducible factor (HIF)HIF inhibitorsOxygen-regulationMicroenvironmentImmunosuppression
ISSN
1354-3776
Publisher
T&F (Taylor & Francis)
DOI
http://dx.doi.org/10.1080/13543776.2021.1874345
Type
Article
Appears in Collections:
Division of Biomedical Research > Biotherapeutics Translational Research Center > 1. Journal Articles
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