46P AB521, a clinical-stage, potent, and selective Hypoxia-Inducible Factor (HIF)-2α inhibitor, for the treatment of renal cell carcinoma
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Next-generation HIF-2α inhibitors such as YQ-0629 and casdatifan (AB521) have shown promising preclinical and early clinical activity.
“Continued efforts are now focused on developing next-generation HIF-2α inhibitors with enhanced selectivity and potency, such as YQ-0629 and casdatifan (AB521), both of which have shown promising preclinical and early clinical activity [[418], [419], [420]].”
From HIF inhibition: Current strategies and clinical challenges (2026) · cites this paper as [419]
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HIF-1 and HIF-2 in cancer: structure, regulation, and therapeutic prospects
Shi, Y., & Gilkes, D. M. (2025) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-024-05537-0 · Cited by 71 · see citing works
Novel Approaches with HIF-2α Targeted Therapies in Metastatic Renal Cell Carcinoma
Nguyen, C. B., Oh, E., Bahar, P., Vaishampayan, U. N., Else, T., & Alva, A. S. (2024) · Cancers · doi:10.3390/cancers16030601 · Cited by 25 · see citing works
Mata, G., Mailyan, A. K., Fournier, J. T. A., Beatty, J. W., Leleti, M. R., Powers, J. P., & Lawson, K. V. (2025) · Organic Letters · doi:10.1021/acs.orglett.4c04501 · Cited by 11 · see citing works
Self-citationNovel Targeted Therapies for Renal Cell Carcinoma
Saliby, R. M., Saad, E., Labaki, C., Xu, W. V., Braun, D. A., Viswanathan, S. R., & Bakouny, Z. (2023) · Hematology/Oncology Clinics of North America · doi:10.1016/j.hoc.2023.05.022 · Cited by 3 · see citing works
HIF inhibition: Current strategies and clinical challenges
Więch-Walów, A., Bartoszewska, S., Barton, A., Czechowicz, P., Dudzik, J., Wielockx, B., Collawn, J. F., & Bartoszewski, R. (2026) · Redox biology · doi:10.1016/j.redox.2026.104220 · Cited by 3 · see citing works
Mata, G., Mailyan, A. K., Drew, S. L., Beatty, J. W., Fournier, J., Rosen, B. R., Yan, X., Gál, B., Tran, A., Kalisiak, J., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c03647 · Cited by 2 · see citing works
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- Authors
- Lawson, K. V., Sivick Gauthier, K. E., Piovesan, D., Mailyan, A., Mata, G., Fournier, J. T. A., Yu, K., Liu, S., Soriano, F., Jin, L., Ginn, E., Schweickert, P. G., Meleza, C. A., Pham, A., Seitz, L., Liao, K., Paterson, E., Foster, P., Walters, M. J., & Leleti, M.
- Affiliations
- Arcus Biosciences (United States) (US)
- Venue
- Annals of Oncology
- Publisher
- Elsevier BV
- Published
- 2022-03
- Volume
- 33
- Pages
- S21
- ISSN
- 0923-7534 (ISSN-L)
- OpenAlex
- W4220802499
- Cited by
- 6
- References
- 0
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 1 · 2023: 1
- FWCI
- 0.42
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Annals of Oncology (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Hypoxia, and Metabolism
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Renal cell carcinoma treatment
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Ferroptosis and cancer prognosis
- Keywords
- HIF-2α inhibitor, clear cell renal cell carcinoma, HIF-2α, von Hippel-Lindau protein, tumor hypoxia, post-translational regulation, tumor growth inhibition
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