Drug intelligence / Profile preview

DFF332

Development stage
Phase 1
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

DFF332 is a small molecule inhibitor that selectively targets hypoxia-inducible factor 2 alpha (HIF-2α), a transcription factor implicated in the growth and progression of certain cancers, particularly clear cell renal cell carcinoma (ccRCC). By binding to HIF-2α, DFF332 prevents its heterodimerization and subsequent DNA binding, thereby inhibiting its transcriptional activity. This mechanism disrupts oncogenic pathways driven by HIF-2α. The drug is administered orally and has shown dose-dependent antitumor efficacy in preclinical models as well as early clinical trials. Developed by Novartis, DFF332 has been evaluated as monotherapy in phase 1 studies for patients with advanced ccRCC[1][2][3][4][5][6][7].

Other names
HIF2alpha inhibitor DFF332HIF-2alpha inhibitor DFF332HIF 2alpha inhibitor DFF332
02

Targets

EPAS1 (Hypoxia-inducible factor 2-alpha)

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