Selinexor for advanced hematologic malignancies

Integrated safety profile of selinexor in multiple myeloma: experience from 437 patients enrolled in clinical trials

(2020) Maria Gavriatopoulou et al.   LEUKEMIA

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing

(2020) David E. Gordon et al.   NATURE

Phase 1 study of selinexor plus carfilzomib and dexamethasone for the treatment of relapsed/refractory multiple myeloma

(2019) Andrzej J. Jakubowiak et al.   BRITISH JOURNAL OF HAEMATOLOGY

A Phase II Trial of Selinexor (KPT‐330) for Metastatic Triple‐Negative Breast Cancer

(2019) Michael Shafique et al.   ONCOLOGIST

Inhibitors of nuclear transport

(2019) David A Jans et al.   CURRENT OPINION IN CELL BIOLOGY

NUCLEAR EXPORT INHIBITION ENHANCES THE ACTIVITY OF R-CHOP IN NON-HODGKIN'S LYMPHOMA

(2019) A.S. Azmi et al.   HEMATOLOGICAL ONCOLOGY

A PHASE 2B STUDY OF SELINEXOR IN PATIENTS WITH RELAPSED/REFRACTORY (R/R) DIFFUSE LARGE B-CELL LYMPHOMA (DLBCL)

(2019) N. Kalakonda et al.   HEMATOLOGICAL ONCOLOGY

Altered nuclear export signal recognition as a driver of oncogenesis

(2019) Justin Taylor et al.   Cancer Discovery

Final analysis from RESONATE: up to 6 years of follow‐up on ibrutinib in patients with previously treated chronic lymphocytic leukemia or small lymphocytic lymphoma

(2019) Talha Munir et al.   AMERICAN JOURNAL OF HEMATOLOGY

Selinexor in combination with decitabine in patients with acute myeloid leukemia: results from a phase 1 study

(2019) Bhavana Bhatnagar et al.   LEUKEMIA & LYMPHOMA

Oral Selinexor–Dexamethasone for Triple-Class Refractory Multiple Myeloma

(2019) Ajai Chari et al.   NEW ENGLAND JOURNAL OF MEDICINE

Selinexor Combined with Ibrutinib Demonstrates Tolerability and Efficacy in Advanced B-Cell Malignancies: A Phase I Study

(2019) Deborah M. Stephens et al.   BLOOD

Eltanexor (KPT-8602), a Second-Generation Selective Inhibitor of Nuclear Export (SINE) Compound, in Patients with Higher-Risk Myelodysplastic Syndrome

(2019) Sangmin Lee et al.   BLOOD

Phase I Clinical Trial of Selinexor in Combination with Daunorubicin and Cytarabine in Previously Untreated Poor-Risk Acute Myeloid Leukemia

(2019) Kendra Sweet et al.   CLINICAL CANCER RESEARCH

Selinexor combined with cladribine, cytarabine, and filgrastim in relapsed or refractory acute myeloid leukemia

(2019) Ramzi Abboud et al.   HAEMATOLOGICA

Selinexor: A First-in-Class Nuclear Export Inhibitor for Management of Multiply Relapsed Multiple Myeloma

(2019) Tim J. Peterson et al.   ANNALS OF PHARMACOTHERAPY

Preclinical Assessment with Clinical Validation of Selinexor with Gemcitabine and Nab-Paclitaxel for the Treatment of Pancreatic Ductal Adenocarcinoma

(2019) Asfar S. Azmi et al.   CLINICAL CANCER RESEARCH

Phase I Study of Selinexor, Ixazomib, and Low-dose Dexamethasone in Patients With Relapsed or Refractory Multiple Myeloma

(2019) Meghan Salcedo et al.   Clinical Lymphoma Myeloma & Leukemia

Phase 2 study of the Exportin 1 inhibitor selinexor in patients with recurrent gynecological malignancies

(2019) I.B. Vergote et al.   GYNECOLOGIC ONCOLOGY

Resistance to BTK inhibition by ibrutinib can be overcome by preventing FOXO3a nuclear export and PI3K/AKT activation in B-cell lymphoid malignancies

(2019) Isha Kapoor et al.   Cell Death & Disease

FoxO-1 contributes to the efficacy of the combination of the XPO1 inhibitor selinexor and cisplatin in ovarian carcinoma preclinical models

(2018) Cristina Corno et al.   BIOCHEMICAL PHARMACOLOGY

Combinatorial targeting of XPO1 and FLT3 exerts synergistic anti-leukemia effects through induction of differentiation and apoptosis in FLT3-mutated acute myeloid leukemias: from concept to clinical trial

(2018) Weiguo Zhang et al.   HAEMATOLOGICA

Selective Inhibition of Nuclear Export With Oral Selinexor for Treatment of Relapsed or Refractory Multiple Myeloma

(2018) Dan T. Vogl et al.   JOURNAL OF CLINICAL ONCOLOGY

A phase I study of selinexor in combination with high-dose cytarabine and mitoxantrone for remission induction in patients with acute myeloid leukemia

(2018) Amy Y. Wang et al.   Journal of Hematology & Oncology

Correlation of CRM1-NES affinity with nuclear export activity

(2018) Szu-Chin Fu et al.   MOLECULAR BIOLOGY OF THE CELL

A Phase II Trial of Selinexor, an Oral Selective Inhibitor of Nuclear Export Compound, in Abiraterone‐ and/or Enzalutamide‐Refractory Metastatic Castration‐Resistant Prostate Cancer

(2018) Xiao X. Wei et al.   ONCOLOGIST

Selinexor synergizes with dexamethasone to repress mTORC1 signaling and induce multiple myeloma cell death

(2018) Christian Argueta et al.   Oncotarget

Combinatorial targeting of XPO1 and FLT3 exerts synergistic anti-leukemia effects through induction of differentiation and apoptosis in FLT3-mutated acute myeloid leukemias: from concept to clinical trial

(2018) Weiguo Zhang et al.   HAEMATOLOGICA

Inhibition of XPO1 enhances cell death induced by ABT-199 in acute myeloid leukaemia via Mcl-1

(2018) Daniel A. Luedtke et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Phase 2 results of selinexor in advanced de-differentiated (DDLS) liposarcoma (SEAL) study: A phase 2/3, randomized, double blind, placebo controlled cross-over study.

(2018) Mrinal M. Gounder et al.   JOURNAL OF CLINICAL ONCOLOGY

In vitro toxicity and efficacy of verdinexor, an exportin 1 inhibitor, on opportunistic viruses affecting immunocompromised individuals

(2018) Douglas G. Widman et al.   PLoS One

Selinexor plus low-dose bortezomib and dexamethasone for patients with relapsed or refractory multiple myeloma

(2018) Nizar J. Bahlis et al.   BLOOD

Verdinexor (KPT-335), a selective inhibitor of nuclear export, reduces RSV replication in vitro

(2018) Patricia A. Jorquera et al.   JOURNAL OF VIROLOGY

Promising activity of selinexor in the treatment of a patient with refractory diffuse large B-cell lymphoma and central nervous system involvement

(2017) Sabela Bobillo et al.   HAEMATOLOGICA

Identification of potential ibrutinib combinations in hematological malignancies using a combination high-throughput screen

(2017) Michael Schaffer et al.   LEUKEMIA & LYMPHOMA

Selinexor Overcomes Hypoxia-Induced Drug Resistance in Multiple Myeloma

(2017) Barbara Muz et al.   Translational Oncology

In vitro evaluation of Selective Inhibitors of Nuclear Export (SINE) drugs KPT-185 and KPT-335 against canine mammary carcinoma and transitional cell carcinoma tumor initiating cells

(2017) J. E. Grayton et al.   Veterinary and Comparative Oncology

Pharmacological treatment with inhibitors of nuclear export enhances the antitumor activity of docetaxel in human prostate cancer

(2017) Giovanni Luca Gravina et al.   Oncotarget

Selective Inhibitors of Nuclear Export (SINE) compounds block proliferation and migration of triple negative breast cancer cells by restoring expression of ARRDC3

(2017) Young Hwa Soung et al.   Oncotarget

Inhibition of exportin-1 function results in rapid cell cycle-associated DNA damage in cancer cells

(2017) Russell T. Burke et al.   Oncotarget

CRM1 Inhibitors for Antiviral Therapy

(2017) Cynthia Mathew et al.   Frontiers in Microbiology

Promising activity of selinexor in the treatment of a patient with refractory diffuse large B-cell lymphoma and central nervous system involvement

(2017) Sabela Bobillo et al.   HAEMATOLOGICA

Selinexor (KPT-330) has antitumor activity against anaplastic thyroid carcinoma in vitro and in vivo and enhances sensitivity to doxorubicin

(2017) Manoj Garg et al.   Scientific Reports

Recurrent mutations of the exportin 1 gene (XPO1) and their impact on selective inhibitor of nuclear export compounds sensitivity in primary mediastinal B-cell lymphoma

(2016) Fabrice Jardin et al.   AMERICAN JOURNAL OF HEMATOLOGY

The 2016 revision of the World Health Organization classification of lymphoid neoplasms

(2016) S. H. Swerdlow et al.   BLOOD

Anti-tumor activity of selective inhibitor of nuclear export (SINE) compounds, is enhanced in non-Hodgkin lymphoma through combination with mTOR inhibitor and dexamethasone

(2016) Irfana Muqbil et al.   CANCER LETTERS

CRM1 Inhibition Promotes Cytotoxicity in Ewing Sarcoma Cells by Repressing EWS-FLI1-Dependent IGF-1 Signaling

(2016) H. Sun et al.   CANCER RESEARCH

Anti-inflammatory natural product goniothalamin reduces colitis-associated and sporadic colorectal tumorigenesis

(2016) Débora Barbosa Vendramini-Costa et al.   CARCINOGENESIS

Inhibition of the Nuclear Export Receptor XPO1 as a Therapeutic Target for Platinum-Resistant Ovarian Cancer

(2016) Ying Chen et al.   CLINICAL CANCER RESEARCH

XPO1 Inhibition using Selinexor Synergizes with Chemotherapy in Acute Myeloid Leukemia by Targeting DNA Repair and Restoring Topoisomerase II  to the Nucleus

(2016) P. Ranganathan et al.   CLINICAL CANCER RESEARCH

The Bruton Tyrosine Kinase (BTK) Inhibitor Acalabrutinib Demonstrates Potent On-Target Effects and Efficacy in Two Mouse Models of Chronic Lymphocytic Leukemia

(2016) Sarah E.M. Herman et al.   CLINICAL CANCER RESEARCH

XPO1 Inhibition Preferentially Disrupts the 3D Nuclear Organization of Telomeres in Tumor Cells

(2016) Cheryl Taylor-Kashton et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Phase I Study of Selinexor, a Selective Inhibitor of Nuclear Export, in Combination With Fludarabine and Cytarabine, in Pediatric Relapsed or Refractory Acute Leukemia

(2016) Thomas B. Alexander et al.   JOURNAL OF CLINICAL ONCOLOGY

First-in-Class, First-in-Human Phase I Study of Selinexor, a Selective Inhibitor of Nuclear Export, in Patients With Advanced Solid Tumors

(2016) Albiruni R. Abdul Razak et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase IB Study of Selinexor, a First-in-Class Inhibitor of Nuclear Export, in Patients With Advanced Refractory Bone or Soft Tissue Sarcoma

(2016) Mrinal M. Gounder et al.   JOURNAL OF CLINICAL ONCOLOGY

Treatment of acquired drug resistance in multiple myeloma by combination therapy with XPO1 and topoisomerase II inhibitors

(2016) Joel G. Turner et al.   Journal of Hematology & Oncology

Venetoclax in relapsed or refractory chronic lymphocytic leukaemia with 17p deletion: a multicentre, open-label, phase 2 study

(2016) Stephan Stilgenbauer et al.   LANCET ONCOLOGY

KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells

(2016) J Etchin et al.   LEUKEMIA

Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies

(2016) Z A Hing et al.   LEUKEMIA

Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia

(2016) John C. Byrd et al.   NEW ENGLAND JOURNAL OF MEDICINE

Antiviral Efficacy of Verdinexor In Vivo in Two Animal Models of Influenza A Virus Infection

(2016) Olivia Perwitasari et al.   PLoS One

Molecular mechanism and therapeutic implications of selinexor (KPT-330) in liposarcoma

(2016) Manoj Garg et al.   Oncotarget

Preclinical activity of selinexor, an inhibitor of XPO1, in sarcoma

(2016) Robert Nakayama et al.   Oncotarget

Selinexor is effective in acquired resistance to ibrutinib and synergizes with ibrutinib in chronic lymphocytic leukemia

(2015) Z. A. Hing et al.   BLOOD

Decitabine priming enhances the antileukemic effects of exportin 1 (XPO1) selective inhibitor selinexor in acute myeloid leukemia

(2015) P. Ranganathan et al.   BLOOD

shRNA library screening identifies nucleocytoplasmic transport as a mediator of BCR-ABL1 kinase-independent resistance

(2015) J. S. Khorashad et al.   BLOOD

A phase 2 study of idelalisib plus rituximab in treatment-naive older patients with chronic lymphocytic leukemia

(2015) S. M. O'Brien et al.   BLOOD

Deciphering mechanisms of drug sensitivity and resistance to Selective Inhibitor of Nuclear Export (SINE) compounds

(2015) Marsha Crochiere et al.   BMC CANCER

KPT-330, a potent and selective exportin-1 (XPO-1) inhibitor, shows antitumor effects modulating the expression of cyclin D1 and survivin in prostate cancer models

(2015) Giovanni Luca Gravina et al.   BMC CANCER

Identifying Drug-Target Selectivity of Small-Molecule CRM1/XPO1 Inhibitors by CRISPR/Cas9 Genome Editing

(2015) Jasper E. Neggers et al.   CHEMISTRY & BIOLOGY

XPO1 Inhibition Enhances Radiation Response in Preclinical Models of Rectal Cancer

(2015) I. Ferreiro-Neira et al.   CLINICAL CANCER RESEARCH

The phosphoinositide-3-kinase (PI3K)-delta and gamma inhibitor, IPI-145 (Duvelisib), overcomes signals from the PI3K/AKT/S6 pathway and promotes apoptosis in CLL

(2015) K Balakrishnan et al.   LEUKEMIA

Activity of a selective inhibitor of nuclear export, selinexor (KPT-330), against AML-initiating cells engrafted into immunosuppressed NSG mice

(2015) J Etchin et al.   LEUKEMIA

CRM1 as a new therapeutic target for non-Hodgkin lymphoma

(2015) Xiaohong Han et al.   LEUKEMIA RESEARCH

Synergistic Myeloma Cell Death via Novel Intracellular Activation of Caspase-10-Dependent Apoptosis by Carfilzomib and Selinexor

(2015) S. Rosebeck et al.   MOLECULAR CANCER THERAPEUTICS

Anti-tumor activity of selective inhibitors of XPO1/CRM1-mediated nuclear export in diffuse malignant peritoneal mesothelioma: the role of survivin

(2015) Michelandrea De Cesare et al.   Oncotarget

A method for quantification of exportin-1 (XPO1) occupancy by Selective Inhibitor of Nuclear Export (SINE) compounds

(2015) Marsha L. Crochiere et al.   Oncotarget

Targeting the Nuclear Export Protein XPO1/CRM1 Reverses Epithelial to Mesenchymal Transition

(2015) Asfar S. Azmi et al.   Scientific Reports

A deep proteomics perspective on CRM1-mediated nuclear export and nucleocytoplasmic partitioning

(2015) Koray Kırlı et al.   eLife

Structural determinants of nuclear export signal orientation in binding to exportin CRM1

(2015) Ho Yee Joyce Fung et al.   eLife

LocNES: a computational tool for locating classical NESs in CRM1 cargo proteins

(2014) Darui Xu et al.   BIOINFORMATICS

Biologic activity of the novel orally bioavailable selective inhibitor of nuclear export (SINE) KPT-335 against canine melanoma cell lines

(2014) Megan N Breit et al.   BMC Veterinary Research

KPT-330 has antitumour activity against non-small cell lung cancer

(2014) H Sun et al.   BRITISH JOURNAL OF CANCER

KPT-330 inhibitor of XPO1-mediated nuclear export has anti-proliferative activity in hepatocellular carcinoma

(2014) Yun Zheng et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

XPO1/CRM1-Selective Inhibitors of Nuclear Export (SINE) reduce tumor spreading and improve overall survival in preclinical models of prostate cancer (PCa)

(2014) Giovanni Gravina et al.   Journal of Hematology & Oncology

Verdinexor, a Novel Selective Inhibitor of Nuclear Export, Reduces Influenza A Virus Replication In Vitro and In Vivo

(2014) O. Perwitasari et al.   JOURNAL OF VIROLOGY

Selinexor suppresses downstream effectors of B-cell activation, proliferation and migration in chronic lymphocytic leukemia cells

(2014) Y Zhong et al.   LEUKEMIA

CBS9106-Induced CRM1 Degradation Is Mediated by Cullin Ring Ligase Activity and the Neddylation Pathway

(2014) N. Saito et al.   MOLECULAR CANCER THERAPEUTICS

Preclinical antitumor efficacy of selective exportin 1 inhibitors in glioblastoma

(2014) Adam L. Green et al.   NEURO-ONCOLOGY

Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia

(2014) Richard R. Furman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Preclinical Evaluation of the Novel, Orally Bioavailable Selective Inhibitor of Nuclear Export (SINE) KPT-335 in Spontaneous Canine Cancer: Results of a Phase I Study

(2014) Cheryl A. London et al.   PLoS One

Specific Inhibition of the Nuclear Exporter Exportin-1 Attenuates Kidney Cancer Growth

(2014) Hiromi I. Wettersten et al.   PLoS One

Inhibition of CRM1-dependent nuclear export sensitizes malignant cells to cytotoxic and targeted agents

(2014) Joel G. Turner et al.   SEMINARS IN CANCER BIOLOGY

Prognostic impact and targeting of CRM1 in acute myeloid leukemia

(2013) K. Kojima et al.   BLOOD

Preclinical and clinical efficacy of XPO1/CRM1 inhibition by the karyopherin inhibitor KPT-330 in Ph+ leukemias

(2013) C. J. Walker et al.   BLOOD

KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia

(2013) Julia Etchin et al.   BRITISH JOURNAL OF HAEMATOLOGY

Selective inhibitors of nuclear export for the treatment of non-Hodgkin's lymphomas

(2013) A. S. Azmi et al.   HAEMATOLOGICA

Release of Severe Acute Respiratory Syndrome Coronavirus Nuclear Import Block Enhances Host Transcription in Human Lung Cells

(2013) A. C. Sims et al.   JOURNAL OF VIROLOGY

Genome-wide studies in multiple myeloma identify XPO1/CRM1 as a critical target validated using the selective nuclear export inhibitor KPT-276

(2013) J Schmidt et al.   LEUKEMIA

CRM1 inhibition induces tumor cell cytotoxicity and impairs osteoclastogenesis in multiple myeloma: molecular mechanisms and therapeutic implications

(2013) Y-T Tai et al.   LEUKEMIA

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

(2013) Andrew J Souers et al.   NATURE MEDICINE

Targeting BTK with Ibrutinib in Relapsed Chronic Lymphocytic Leukemia

(2013) John C. Byrd et al.   NEW ENGLAND JOURNAL OF MEDICINE

Selective inhibitors of nuclear export show that CRM1/XPO1 is a target in chronic lymphocytic leukemia

(2012) R. Lapalombella et al.   BLOOD

Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia

(2012) P. Ranganathan et al.   BLOOD

Two palmitylated cysteine residues of the severe acute respiratory syndrome coronavirus spike (S) protein are critical for S incorporation into virus-like particles, but not for M-S co-localization

(2012) M. Ujike et al.   JOURNAL OF GENERAL VIROLOGY

Antileukemic activity of nuclear export inhibitors that spare normal hematopoietic cells

(2012) J Etchin et al.   LEUKEMIA

Sequence and structural analyses of nuclear export signals in the NESdb database

(2012) Darui Xu et al.   MOLECULAR BIOLOGY OF THE CELL

Nuclear export of proteins and drug resistance in cancer

(2011) Joel G. Turner et al.   BIOCHEMICAL PHARMACOLOGY

Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765

(2011) S. E. M. Herman et al.   BLOOD

High dose cytarabine and mitoxantrone: an effective induction regimen for high-risk Acute Myeloid Leukemia (AML)

(2011) Sarah M. Larson et al.   LEUKEMIA & LYMPHOMA

Whole-genome sequencing identifies recurrent mutations in chronic lymphocytic leukaemia

(2011) Xose S. Puente et al.   NATURE

SARS-CoV 9b Protein Diffuses into Nucleus, Undergoes Active Crm1 Mediated Nucleocytoplasmic Export and Triggers Apoptosis When Retained in the Nucleus

(2011) Kulbhushan Sharma et al.   PLoS One

CAL-101, a p110  selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability

(2010) B. J. Lannutti et al.   BLOOD

Identification of Nuclear Export Inhibitors with Potent Anticancer Activity In vivo

(2009) S. C. Mutka et al.   CANCER RESEARCH

The Respiratory Syncytial Virus Matrix Protein Possesses a Crm1-Mediated Nuclear Export Mechanism

(2009) R. Ghildyal et al.   JOURNAL OF VIROLOGY

Molecular Determinants for Subcellular Localization of the Severe Acute Respiratory Syndrome Coronavirus Open Reading Frame 3b Protein

(2009) E. C. Freundt et al.   JOURNAL OF VIROLOGY

Structural basis for assembly and disassembly of the CRM1 nuclear export complex

(2009) Xiuhua Dong et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: Structure–activity relationship and mechanism of action

(2008) Tine Van Neck et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Combined Analysis of Murine and Human Microarrays and ChIP Analysis Reveals Genes Associated with the Ability of MYC To Maintain Tumorigenesis

(2008) Chi-Hwa Wu et al.   PLoS Genetics