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Selinexor

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Also known as KPT-330NexpovioXpovioSELINEXOR (KPT-330)

Summary

Selinexor (CHEMBL3545185) is an approved small-molecule exportin 1 inhibitor (ATC L01XX66) targeting XPO1; indicated across 46 conditions including neoplasm and diffuse large b-cell lymphoma; with CIViC clinical evidence for 1 variant-indication association (e.g. FLT3 ITD & Y842C in acute myeloid leukemia).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01XX66
  • Targets: 1 (XPO1)
  • Indications: 46 conditions
  • Clinical trials: 162
  • Precision-oncology evidence (CIViC): 1 variant–indication association
  • Chemistry: 443.3 Da · C17H11F6N7O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3545185
NameSelinexor
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID71481097
ChEBICHEBI:229764
ATCL01XX66
Molecular formulaC17H11F6N7O
Molecular weight443.3
InChIKeyDEVSOMFAQLZNKR-RJRFIUFISA-N

SMILES: C1=CN=C(C=N1)NNC(=O)/C=C\N2C=NC(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F

IUPAC name: (Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N’-pyrazin-2-ylprop-2-enehydrazide

ChEBI definition: A member of the class of triazoles that is 1H-1,2,4-triazole substituted by (1Z)-3-oxo-3-[2-(pyrazin-2-yl)hydrazinyl]prop-1-en-1-yl and 3,5-bis(trifluoromethyl)phenyl groups at positions 1 and 3, respectively. It is a prescription medicine approved for the treatment of adult patients with relapsed or refractory diffuse large B-cell lymphoma.

Pharmacological roles (ChEBI): exportin 1 inhibitor, antineoplastic agent, anti-inflammatory agent, apoptosis inducer.

Also known as: KPT-330, Nexpovio, Selinexor, Xpovio, SELINEXOR, SELINEXOR (KPT-330), Selinexor (KPT-330), selinexor

Patent coverage: 683 distinct patent families (1,675 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,537 (92%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
XPO1exportin 1Inhibition7.920.2%O14980

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Equilibrative nucleoside transporter 1, Estrogen receptor, 5-hydroxytryptamine receptor 1A, Prostaglandin G/H synthase 1, Prostaglandin G/H synthase 2, Histamine H1 receptor, 3’,5’-cyclic-AMP phosphodiesterase 4D, Prostaglandin G/H synthase 1, Exportin-1.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 13 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
XPO17.92EC5012nMCHEMBL_ACT_25916255
XPO17.73Kd18.74nMCHEMBL_ACT_19267151
XPO17.47IC5034nMCHEMBL_ACT_25500502
XPO17.26IC5055nMCHEMBL_ACT_25500503
PTGS27.21AC5061nMCHEMBL_ACT_25165972
PTGS16.64AC50230nMCHEMBL_ACT_25206111
PTGS15.43AC503730nMCHEMBL_ACT_25205178

Target pathways

Aggregated over 1 target gene(s): XPO1.

Top Reactome pathways

19 total, by targets touching each:

PathwayTargetsGenes
Amplification of signal from unattached kinetochores via a MAD2 inhibitory signal1XPO1
Rev-mediated nuclear export of HIV RNA1XPO1
NEP/NS2 Interacts with the Cellular Export Machinery1XPO1
Downregulation of TGF-beta receptor signaling1XPO1
Separation of Sister Chromatids1XPO1
Resolution of Sister Chromatid Cohesion1XPO1
Deactivation of the beta-catenin transactivating complex1XPO1
HuR (ELAVL1) binds and stabilizes mRNA1XPO1
RHO GTPases Activate Formins1XPO1
MAPK6/MAPK4 signaling1XPO1
Mitotic Prometaphase1XPO1
Cyclin A/B1/B2 associated events during G2/M transition1XPO1
Estrogen-dependent nuclear events downstream of ESR-membrane signaling1XPO1
EML4 and NUDC in mitotic spindle formation1XPO1
Heme signaling1XPO1
NPAS4 regulates expression of target genes1XPO1
Maturation of hRSV A proteins1XPO1
Transcriptional and post-translational regulation of MITF-M expression and activity1XPO1
Maturation of DENV proteins1XPO1

Dominant GO biological processes

GO termTargets
ribosomal subunit export from nucleus1
ribosomal large subunit export from nucleus1
ribosomal small subunit export from nucleus1
negative regulation of transcription by RNA polymerase II1
mRNA export from nucleus1
protein export from nucleus1
nucleocytoplasmic transport1
response to xenobiotic stimulus1
regulation of centrosome duplication1
regulation of proteasomal ubiquitin-dependent protein catabolic process1
protein localization to nucleus1
ribosome biogenesis1
regulation of protein export from nucleus1
cellular response to triglyceride1
cellular response to salt1

Indications & clinical

Indications

46 indications (4 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
neoplasm4MONDO:0005070EFO:0000616
diffuse large B-cell lymphoma4MONDO:0018905EFO:0000403
plasma cell myeloma4MONDO:0009693EFO:0001378
acute myeloid leukemia3MONDO:0018874EFO:0000222
endometrium neoplasm3MONDO:0021251MONDO:0011962
primary myelofibrosis3MONDO:0009692MONDO:0044903
melanoma2MONDO:0005105EFO:0000756
dedifferentiated liposarcoma2MONDO:0020563EFO:0003085
myelodysplastic syndrome2MONDO:0018881EFO:0000198
glioblastoma2MONDO:0018177EFO:0000519
squamous cell carcinoma2MONDO:0005096EFO:0000707
small cell lung carcinoma2MONDO:0008433EFO:0000702
neoplasm of mature B-cells2MONDO:0004949EFO:0000096
peripheral T-cell lymphoma, not otherwise specified2MONDO:0004964EFO:0000211
squamous cell lung carcinoma2MONDO:0005097EFO:0000708
thymoma2MONDO:0006456EFO:1000581
breast neoplasm2MONDO:0021100MONDO:0007254
ovarian carcinoma2MONDO:0005140EFO:0001075
metastatic melanoma2MONDO:0005191EFO:0002617
severe acute respiratory syndrome2MONDO:0005091MONDO:0100096
lymphoma2MONDO:0005062EFO:0000574
mature T-cell and NK-cell non-Hodgkin lymphoma2MONDO:0000430MONDO:0000430
liposarcoma2MONDO:0005060EFO:0000569
thymus neoplasm2MONDO:0005197EFO:0002626
paraganglioma2MONDO:0000448EFO:1000453
ovarian cancer2MONDO:0008170MONDO:0008170
lymphoid neoplasm1MONDO:0005157EFO:0001642
non-small cell lung carcinoma1MONDO:0005233EFO:0003060
colorectal neoplasm1MONDO:0005335EFO:0004142
rectal cancer1MONDO:0006519EFO:1000657
soft tissue sarcoma1MONDO:0018078EFO:1001968
acute lymphoblastic leukemia1MONDO:0004967EFO:0000220
chronic myeloid leukemia1MONDO:0011996EFO:0000339
gliosarcoma1MONDO:0016681EFO:1001465
sarcoma1MONDO:0005089EFO:0000691
fallopian tube carcinoma1MONDO:0006206EFO:1000251
urothelial carcinoma1MONDO:0040679EFO:0008528
acute biphenotypic leukemia1MONDO:0020322MONDO:0019460
hepatocellular carcinoma1MONDO:0007256EFO:0000182
triple-negative breast carcinoma1MONDO:0005494EFO:0005537
leukemia1MONDO:0005059EFO:0000565
hereditary amyloidosis0MONDO:0018634MONDO:0019438
amyloidosis0MONDO:0019065EFO:1001875

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 162.

Phase distribution

PhaseTrials
PHASE265
PHASE137
PHASE1/PHASE234
PHASE313
Not specified9
PHASE2/PHASE32
PHASE41
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05786989PHASE4UNKNOWNSelinexor Combined With R-GemOx as Second-line Treatment in Patients With Diffuse Large B-cell Lymphoma
NCT04562389PHASE3ACTIVE_NOT_RECRUITINGStudy of Selinexor in Combination With Ruxolitinib in Myelofibrosis
NCT05028348PHASE3ACTIVE_NOT_RECRUITINGA Study of Combination of Selinexor, Pomalidomide, and Dexamethasone (SPd) Versus Elotuzumab, Pomalidomide, and Dexamethasone (EloPd) in Subject With Previously Treated Multiple Myeloma
NCT05611931PHASE3ACTIVE_NOT_RECRUITINGSelinexor in Maintenance Therapy After Systemic Therapy for Participants With p53 Wild-Type, Advanced or Recurrent Endometrial Carcinoma
NCT05726110PHASE3RECRUITINGSelinexor in Combination With HAD or CAG Rregimens in Relapsed or Refractory Acute Myeloid Leukemia
NCT06158841PHASE3RECRUITINGStudy Assessing Activity of Intravenous (IV) Etentamig Monotherapy Versus Standard Available Therapies in Adult Participants With Relapsed or Refractory Multiple Myeloma
NCT06613035PHASE3NOT_YET_RECRUITINGTwice-per-weekSelinexor, 2 Days Melphalan
NCT07011056PHASE3RECRUITINGA Phase III Clinical Study of Purinostat Mesylate for Injection in Patients With Diffuse Large B-cell Lymphoma
NCT07138209PHASE3RECRUITINGA Study Comparing QLS32015 Monotherapy Versus Pomalidomide, Dexamethasone (Pd) or Selinexor, Dexamethasone (Sd) in Participants With Relapsed or Refractory Multiple Myeloma
NCT07569757PHASE3NOT_YET_RECRUITINGClinical Study of TQB2934 Injection in Relapsed/Refractory Multiple Myeloma
NCT02606461PHASE2/PHASE3COMPLETEDSelinexor in Advanced Liposarcoma
NCT03110562PHASE3COMPLETEDBortezomib, Selinexor, and Dexamethasone in Patients With Multiple Myeloma
NCT03555422PHASE3COMPLETEDMaintenance With Selinexor/Placebo After Combination Chemotherapy in Participants With Endometrial Cancer [SIENDO]
NCT04534725PHASE3COMPLETEDCOVID-19 Prevention and Treatment in Cancer; a Sequential Multiple Assignment Randomised Trial;
NCT05675319PHASE3TERMINATEDAllogeneic Stem Cell Transplantation vs. Conventional Therapy as Salvage Therapy for Relapsed / Progressive Patients With Multiple Myeloma After First-line Therapy
NCT05822050PHASE2/PHASE3UNKNOWNAn Open, Single Center, Non-randomized, Single Arm Clinical Study of Evaluating the Efficacy of Selinexor in the Maintenance Treatment of PTCL
NCT02227251PHASE2ACTIVE_NOT_RECRUITINGSelinexor (KPT-330) in Patients With Relapsed/Refractory Diffuse Large B-Cell Lymphoma (DLBCL)
NCT02343042PHASE1/PHASE2ACTIVE_NOT_RECRUITINGSelinexor and Backbone Treatments of Multiple Myeloma Patients
NCT02436707PHASE2ACTIVE_NOT_RECRUITINGNovel Combination Therapy in the Treatment of Relapsed and Refractory Aggressive B-Cell Lymphoma
NCT02835222PHASE2ACTIVE_NOT_RECRUITINGSelinexor With Combination With Induction/Consolidation Therapy in Acute Myeloid Leukemia Patients
NCT03147885PHASE1/PHASE2ACTIVE_NOT_RECRUITINGSelinexor Plus Combination Chemotherapy in Treating Patients With Advanced B Cell Non-Hodgkin Lymphoma
NCT03589222PHASE2ACTIVE_NOT_RECRUITINGSELIBORDARA: Selinexor, Bortezomib and Daratumumab in Multiple Myeloma
NCT04414475PHASE2RECRUITINGA Study of Selinexor (Seli) + Low-dose Dexamethasone (LDD) in Penta-refractory Multiple Myeloma (MM), Seli and Bortezomib + LDD in Triple-class Refractory MM.
NCT04562870PHASE2ACTIVE_NOT_RECRUITINGA Study to Evaluate Single Agent Selinexor Versus Physician’s Choice in Participants With Previously Treated Myelofibrosis
NCT04756401PHASE2ACTIVE_NOT_RECRUITINGSelinexor, Daratumumab, Carfilzomib and Dexamethasone for the Treatment of High-Risk, Recurrent or Refractory Multiple Myeloma
NCT04764942PHASE1/PHASE2ACTIVE_NOT_RECRUITINGSelinexor, Pomalidomide, and Dexamethasone With or Without Carfilzomib for the Treatment of Patients With Relapsed Refractory Multiple Myeloma, The SCOPE Trial
NCT04782687PHASE2ACTIVE_NOT_RECRUITINGStudy of Selinexor Plus DRd for Newly Diagnosed Multiple Myeloma
NCT04925193PHASE2ACTIVE_NOT_RECRUITINGPersonalized Selinexor-based Therapy for Relapsed/Refractory Multiple Myeloma
NCT05035745PHASE1/PHASE2RECRUITINGSelinexor & Talazoparib in Advanced Refractory Solid Tumors; Advanced/Metastatic Triple Negative Breast Cancer (START)
NCT05099003PHASE1/PHASE2RECRUITINGA Study of the Drug Selinexor With Radiation Therapy in Patients With Newly-Diagnosed Diffuse Intrinsic Pontine (DIPG) Glioma and High-Grade Glioma (HGG)
NCT05333458PHASE2RECRUITINGTesting Atezolizumab With Selinexor in People ≥ 12 Years Old With Alveolar Soft Part Sarcoma, The AXIOM Trial
NCT05422027PHASE1/PHASE2RECRUITINGSelinexor Plus VRd in High Risk Newly Diagnosed Multiple Myeloma
NCT05422066PHASE2RECRUITINGSelinexor Plus R-CHOP in High-risk GCB-subtype Diffuse Large B-Cell Lymphoma
NCT05432804PHASE1/PHASE2RECRUITINGTesting the Addition of an Anti-cancer Drug, Selinexor, to the Usual Chemotherapy Treatment (Temozolomide) for Brain Tumors That Have Returned After Previous Treatment
NCT05530421PHASE2RECRUITINGSelinexor, Venetoclax, and Dexamethasone (XVenD) in t(11;14)-Positive Relapsed/Refractory Multiple Myeloma
NCT05597345PHASE2RECRUITINGSelinexor for the Treatment of Intermediate and High-Risk Smoldering Multiple Myeloma
NCT05675813PHASE1/PHASE2RECRUITINGGenotype-guided Treatment in Newly Diagnosed PTCL
NCT05698147PHASE1/PHASE2RECRUITINGSelinexor in Combination With MTX+Ritu to Treat R/R CNSL
NCT05736965PHASE2RECRUITINGA Study of Selinexor in Combination With Azacitidine and Venetoclax (SAV Regimen) in Treatment Naïve Participants With Acute Myeloid Leukemia
NCT05736978PHASE2RECRUITINGAdaptive Treatment for Acute Myeloid Leukemia Based on D14 MRD Results

Clinical evidence (CIViC)

Variant × indication × effect (1 predictive associations from 1 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
FLT3 ITD & Y842CAcute Myeloid LeukemiaResistanceSorafenib + SelinexorCIViC DEID9081

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

6 molecules share ≥1 primary target. Top 6 by shared-target count:

MoleculeSourceStatusShared targets
ZAFIRLUKASTChEMBL + PubChemPhase 4 (approved)XPO1
VERDINEXORChEMBL + PubChemPhase 2 (approved)XPO1
BicalutamidePubChemApprovedXPO1
ChloroquinePubChemApprovedXPO1
CoumarinPubChemApprovedXPO1
SitagliptinPubChemApprovedXPO1

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot