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DRUG CLASS:

Nuclear export inhibitor

Related drugs:
3d
Phase I Trial of the Selective Inhibitor of Nuclear Export, KPT-330, in Relapsed Childhood ALL and AML (clinicaltrials.gov)
P1, N=16, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Dec 2025 --> Jun 2026
Trial completion date • IO biomarker
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Xpovio (selinexor)
3d
Eltanexor (KPT-8602) With Inqovi (Decitabine-Cedazuridine) in High-Risk Myelodysplastic Syndromes (clinicaltrials.gov)
P1/2, N=3, Terminated, National Cancer Institute (NCI) | Completed --> Terminated; Drug company withdrew support.
Trial termination
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Inqovi (decitabine/cedazuridine) • eltanexor (KPT-8602)
1m
SINE: Selinexor, Carfilzomib, and Dexamethasone in Treating Patients With Relapsed or Refractory Multiple Myeloma (clinicaltrials.gov)
P1, N=52, Completed, University of Chicago | Recruiting --> Completed | N=100 --> 52 | Trial completion date: Dec 2026 --> Oct 2025 | Trial primary completion date: Jul 2026 --> Oct 2025
Trial completion • Enrollment change • Trial completion date • Trial primary completion date
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CRBN (Cereblon)
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Xpovio (selinexor) • carfilzomib • dexamethasone injection
1m
Targeting serine metabolism vulnerability in omipalisib-resistant acute myeloid leukemia with phosphoglycerate dehydrogenase inhibitors. (PubMed, Biomed Pharmacother)
Furthermore, we found that, like OCI-AML cells, the exportin 1 (XPO1) inhibitors selinexor and eltanexor significantly induced cell cycle arrest and reduced PHGDH expression in OCI-AML3-OR cells. Therefore, treatment with PHGDH inhibitors could be a therapeutic strategy for refractory AML to PI3K/mTOR inhibitors. Relevant clinical trials are warranted.
Journal • IO biomarker
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XPO1 (Exportin 1) • PHGDH (Phosphoglycerate Dehydrogenase)
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Xpovio (selinexor) • omipalisib (GSK2126458) • eltanexor (KPT-8602)
2ms
SENTRY: Study of Selinexor in Combination With Ruxolitinib in Myelofibrosis (clinicaltrials.gov)
P3, N=353, Active, not recruiting, Karyopharm Therapeutics Inc | Trial primary completion date: Sep 2025 --> Mar 2026 | Recruiting --> Active, not recruiting
Enrollment closed • Trial primary completion date
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CD4 (CD4 Molecule)
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Jakafi (ruxolitinib) • Xpovio (selinexor)
2ms
SINE: Selinexor, Carfilzomib, and Dexamethasone in Treating Patients With Relapsed or Refractory Multiple Myeloma (clinicaltrials.gov)
P1, N=100, Recruiting, University of Chicago | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Jul 2025 --> Jul 2026
Trial completion date • Trial primary completion date
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CRBN (Cereblon)
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Xpovio (selinexor) • carfilzomib • dexamethasone injection
4ms
Phase I Trial of the Selective Inhibitor of Nuclear Export, KPT-330, in Relapsed Childhood ALL and AML (clinicaltrials.gov)
P1, N=16, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Jun 2025 --> Dec 2025
Trial completion date • IO biomarker
|
Xpovio (selinexor)
5ms
Multitargeted Reduction of Inflammation and Atherosclerosis in Tet2 -deficient CHIP via XPO1 Inhibition and Atf3 restoration. (PubMed, bioRxiv)
Here, we show that the XPO1 nuclear export inhibitor eltanexor significantly reduces atherosclerotic plaque formation in a mouse model of Tet2 -mutant CHIP...Tet2 loss diminished ATF3 binding to the regulatory loci of inflammatory mediators, which was restored upon XPO1 inhibition. These results provide new insights into drivers of heightened inflammation in TET2 -mutant CHIP and highlight a novel therapeutic strategy for intervention.
Journal • IO biomarker
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TET2 (Tet Methylcytosine Dioxygenase 2) • ATF3 (Activating Transcription Factor 3)
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TET2 mutation
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eltanexor (KPT-8602)
5ms
The XPO1 inhibitor Eltanexor modulates the Wnt/β-catenin signaling pathway to reduce colorectal cancer tumorigenesis. (PubMed, Cancer Res Commun)
Drug sensitivity assays using organoids from Apcmin/+ mice tumors show increased sensitivity to Eltanexor compared to wild-type organoids. Collectively, these findings highlight XPO1 as a potent target for CRC chemoprevention.
Journal • IO biomarker
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XPO1 (Exportin 1) • FOXO3 (Forkhead box O3)
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eltanexor (KPT-8602)
6ms
Targeting EP300 in diffuse large b-cell lymphoma: efficacy of A485 and synergistic effects with XPO1 inhibition. (PubMed, BMC Cancer)
Our study elucidated that EP300 inhibition, especially in combination with XPO1 blockade, could serve as a promising therapeutic strategy for the treatment of DLBCL.
Journal • IO biomarker
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EP300 (E1A binding protein p300) • E2F1 (E2F transcription factor 1)
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eltanexor (KPT-8602)
7ms
Clinical Significance of XPO1 High Expression in Diffuse Large B-Cell Lymphoma and Its Mechanism (PubMed, Zhongguo Shi Yan Xue Ye Xue Za Zhi)
Cell proliferation, apoptosis, and cell cycle assays were performed to explore the effect of XPO1 inhibitor (KPT-8602) and XPO1 knockdown...Inhibiting the function of XPO1 or reducing its expression can significantly decrease the expression of MYBL1 XPO1 is highly expressed in DLBCL, which is associated with poor prognosis. The oncogenic roles of the new XPO1/MYBL1 signaling are identified in DLBCL and XPO1 inhibitor may be a potential option for newly-diagnosed DLBCL patients.
Journal • IO biomarker
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XPO1 (Exportin 1) • MYBL1 (MYB Proto-Oncogene Like 1)
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eltanexor (KPT-8602)