Casdatifan (AB521) is a novel and potent allosteric small molecule inhibitor of protumourigenic HIF-2α dependent transcription.
Schweickert PG, Piovesan D, Mitchell CG, Zepeda-Carranza B, Zhu WS, Lopez Espinoza AY, Rocha L, Singh J, Malgapo MIP, Meleza C, Northington KR, Ray RD, Zhao X, Lawson KV, Walters MJ, Sivick KE.
Schweickert PG, et al.
Br J Pharmacol. 2025 Sep;182(17):4147-4167. doi: 10.1111/bph.70075. Epub 2025 May 21.
Br J Pharmacol. 2025.
PMID: 40400177
BACKGROUND AND PURPOSE: Hypoxia-inducible factor 2alpha (HIF-2alpha) is a transcription factor that mediates the expression of genes critical for cell adaptation and survival in low oxygen (hypoxic) conditions. ...KEY RESULTS: AB521 inhibited HIF-2alpha-mediated tra …
BACKGROUND AND PURPOSE: Hypoxia-inducible factor 2alpha (HIF-2alpha) is a transcription factor that mediates the expression of …