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DRUG:

DFF332

i
Other names: DFF332, DFF 332, DFF-332
Associations
Company:
Novartis
Drug class:
HIF-2α inhibitor
Associations
5ms
CDFF332A12101: DFF332 as a Single Agent and in Combination With Everolimus & Immuno-Oncology Agents in Advanced/Relapsed Renal Cancer & Other Malignancies (clinicaltrials.gov)
P1, N=40, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Sep 2025 --> Mar 2026 | Trial primary completion date: Sep 2025 --> Mar 2026
Trial completion date • Trial primary completion date • IO biomarker
|
VHL (von Hippel-Lindau tumor suppressor) • SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B) • EPAS1 (Endothelial PAS domain protein 1) • SDHC (Succinate Dehydrogenase Complex Subunit C) • SDHD (Succinate Dehydrogenase Complex Subunit D) • SDHA (Succinate Dehydrogenase Complex Flavoprotein Subunit A) • SDHAF2 (Succinate Dehydrogenase Complex Assembly Factor 2)
|
VHL mutation
|
everolimus • spartalizumab (PDR001) • DFF332 • taminadenant (NIR178)
5ms
Hypoxia Inducible Factor-2α (HIF-2α) Pathway Inhibitors. (PubMed, J Kidney Cancer VHL)
We discuss the major key inhibitors, with focus on belzutifan and review the various trials investigating its efficacy in monotherapy as well as in combination therapies in RCC...We also highlight emerging HIF-2α inhibitors currently in clinical trials, namely casdatifan, NKT-2152, and DFF332. Finally, we address the major toxicities and management of these inhibitors.
Review • Journal
|
VHL (von Hippel-Lindau tumor suppressor) • EPAS1 (Endothelial PAS domain protein 1) • CA9 (Carbonic anhydrase 9) • POU5F1 (POU Class 5 Homeobox 1) • ARNT (Aryl Hydrocarbon Receptor Nuclear Translocator)
|
Welireg (belzutifan) • DFF332 • NKT2152 • casdatifan (AB521)
9ms
A phase I dose escalation study of the HIF-2 alpha inhibitor DFF332 in patients with advanced clear cell renal cell carcinoma. (PubMed, Clin Cancer Res)
While clinical responses were limited in the doses evaluated, dose exploration halted prematurely, making it difficult to draw definitive conclusions about the efficacy of DFF332. Further investigation is required to establish a recommended dose regimen, assess its efficacy and safety, and evaluate its full potential as a partner in combination studies.
P1 data • Journal
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EPAS1 (Endothelial PAS domain protein 1)
|
VHL mutation
|
DFF332
11ms
CDFF332A12101: DFF332 as a Single Agent and in Combination With Everolimus & Immuno-Oncology Agents in Advanced/Relapsed Renal Cancer & Other Malignancies (clinicaltrials.gov)
P1, N=40, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Feb 2025 --> Sep 2025 | Trial primary completion date: Feb 2025 --> Sep 2025
Trial completion date • Trial primary completion date • IO biomarker
|
VHL (von Hippel-Lindau tumor suppressor) • SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B) • EPAS1 (Endothelial PAS domain protein 1) • SDHC (Succinate Dehydrogenase Complex Subunit C) • SDHD (Succinate Dehydrogenase Complex Subunit D) • SDHA (Succinate Dehydrogenase Complex Flavoprotein Subunit A) • SDHAF2 (Succinate Dehydrogenase Complex Assembly Factor 2)
|
VHL mutation • SDHB mutation
|
everolimus • spartalizumab (PDR001) • DFF332 • taminadenant (NIR178)
over1year
DFF332 as a Single Agent and in Combination With Everolimus & Immuno-Oncology Agents in Advanced/Relapsed Renal Cancer & Other Malignancies (clinicaltrials.gov)
P1, N=40, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Jul 2025 --> Feb 2025 | Trial primary completion date: Jul 2025 --> Feb 2025
Trial completion date • Trial primary completion date • Combination therapy • IO biomarker • Metastases • Immuno-oncology
|
VHL (von Hippel-Lindau tumor suppressor) • SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B) • EPAS1 (Endothelial PAS domain protein 1) • SDHC (Succinate Dehydrogenase Complex Subunit C) • SDHD (Succinate Dehydrogenase Complex Subunit D) • SDHA (Succinate Dehydrogenase Complex Flavoprotein Subunit A) • SDHAF2 (Succinate Dehydrogenase Complex Assembly Factor 2)
|
VHL mutation • SDHB mutation
|
everolimus • spartalizumab (PDR001) • DFF332 • taminadenant (NIR178)
almost2years
DFF332 as a Single Agent and in Combination With Everolimus & Immuno-Oncology Agents in Advanced/Relapsed Renal Cancer & Other Malignancies (clinicaltrials.gov)
P1, N=40, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting | N=180 --> 40
Enrollment closed • Enrollment change • Combination therapy • IO biomarker • Metastases • Immuno-oncology
|
VHL (von Hippel-Lindau tumor suppressor) • SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B) • EPAS1 (Endothelial PAS domain protein 1) • SDHC (Succinate Dehydrogenase Complex Subunit C) • SDHD (Succinate Dehydrogenase Complex Subunit D) • SDHA (Succinate Dehydrogenase Complex Flavoprotein Subunit A) • SDHAF2 (Succinate Dehydrogenase Complex Assembly Factor 2)
|
VHL mutation • SDHB mutation
|
everolimus • spartalizumab (PDR001) • DFF332 • taminadenant (NIR178)
4years
Clinical • Enrollment open • Combination therapy • IO biomarker
|
VHL (von Hippel-Lindau tumor suppressor) • SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B) • EPAS1 (Endothelial PAS domain protein 1) • SDHC (Succinate Dehydrogenase Complex Subunit C) • SDHD (Succinate Dehydrogenase Complex Subunit D) • SDHA (Succinate Dehydrogenase Complex Flavoprotein Subunit A) • SDHAF2 (Succinate Dehydrogenase Complex Assembly Factor 2)
|
VHL mutation • SDHB mutation
|
everolimus • spartalizumab (PDR001) • DFF332 • taminadenant (NIR178)
4years
Clinical • New P1 trial • Combination therapy
|
VHL (von Hippel-Lindau tumor suppressor) • SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B) • EPAS1 (Endothelial PAS domain protein 1) • SDHC (Succinate Dehydrogenase Complex Subunit C) • SDHD (Succinate Dehydrogenase Complex Subunit D) • SDHA (Succinate Dehydrogenase Complex Flavoprotein Subunit A) • SDHAF2 (Succinate Dehydrogenase Complex Assembly Factor 2)
|
VHL mutation • SDHB mutation
|
everolimus • spartalizumab (PDR001) • DFF332 • taminadenant (NIR178)
over4years
Clinical • New P1 trial • Combination therapy • IO biomarker
|
VHL (von Hippel-Lindau tumor suppressor) • SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B) • EPAS1 (Endothelial PAS domain protein 1) • SDHC (Succinate Dehydrogenase Complex Subunit C) • SDHD (Succinate Dehydrogenase Complex Subunit D) • SDHA (Succinate Dehydrogenase Complex Flavoprotein Subunit A) • SDHAF2 (Succinate Dehydrogenase Complex Assembly Factor 2)
|
VHL mutation • SDHB mutation
|
everolimus • spartalizumab (PDR001) • DFF332 • taminadenant (NIR178)