Accession Number
Small Molecule
Approved, Investigational

Selinexor is a first-in-class selective inhibitor of nuclear transport (SINE) compound. It is currently approved for the treatment of multiple myeloma, a cancer which forms from antibody-producing plasma cells.6,7 This condition is typically treated with high dose bortezomib and dexamethasone chemotherapy followed by autologous stem-cell transplant. Other chemotherapies for multiple myeloma include lenalidomide and dexamethasone, thalidomide, and may include melphalan if the patient is not eligible for transplant.8 Selinexor was approved by the FDA in June 2019. It was granted fast track and orphan designation as well as accelerated approval based on single arm, open label trial data. The Bortezomib, Selinexor, and Dexamethasone in Patients With Multiple Myeloma (BOSTON) trial is planned to finish in 2020.9

  • Selinexor
External IDs
KPT 330 / KPT-330
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
XpovioTablet, film coated20 mg/1OralKaryopharm Therapeutics Inc.2019-07-10Not applicableUs
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

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CAS number
Average: 443.313
Monoisotopic: 443.09292698
Chemical Formula
InChI Key



Selinexor is indicated for the treatment of relapsed or refractory multiple myeloma in combination with dexamethasone.Label Patients must have received at least 4 prior therapies and have disease which is refractory to least two proteasome inhibitors, at least two immunomodulatory agents, and an anti‐CD38 monoclonal antibody.

Associated Conditions

Selinexor causes cell cycle arrest and apoptosis in cancer cells.Label

Mechanism of action

Selinexor binds to and inhibits exportin-1 (XPO1).Label XPO1 is a nuclear exporter protein which contains a pocket to which nuclear proteins can bind. When complexed with these proteins and Ran, activated through guanosine triphosphate (GTP) binding, the XPO1-protein-Ran-GTP complex is able to exit the nucleus through a nuclear pore. Once outside, GTP is hydrolyzed and the complex dissociates.4 The inhibition of this process in cancer cells allows the targets of XPO1, many of which are tumor suppressors, to collect in the nucleus and result in increased transcription of tumor suppressor genes. Tumor suppressor proteins known to be affected by XPO1 inhibition include p53, p73, adenomatous polyposis coli, retinoblastoma, forkhead box protein O, breast cancer 1, nucleophosmin, and merlin. Regulators of cell cycle progression are also affected, namely p21, p27, galectin-3, and Tob. Inhibitor of NFκB also collects in the nucleus as a result leading to reduced activity of NFκB, a known contributor to cancer.4,5 XPO1 participates in the formation of a complex with eukaryotic initiation factor 4E and contributes to the transport of messenger RNA for several oncegenes including cell cycle promotors, cyclin D1, cyclin E, and CDK2/4/6, as well as antiapoptotic proteins, Mcl-1 and Bcl-xL.4 These wide ranging changes in protein expression and gene transcription culminate in cell cycle arrest and the promotion of apoptosis in cancer cells.

Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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A single 80 mg dose of selinexor produces a mean Cmax of 680 ng/mL and a mean AUC of 5386 ng*h/mL.Label This relationship is dose proportion over the range of 3-85 mg/m2 which encompasses the range of 0.06-1.8 times the approved dosage. The official FDA labeling reports the Tmax as 4 hours but phase 1 studies have found a range of 2-4 hours.Label,1,2,3 Administering selinexor with food, either a high or low fat meal, results in an increase in the AUC of approximately 15-20% but this is not expected to be clinically significant.2

Volume of distribution

The mean apparent volume of distribution is 125 L.Label A phase 1 study reported mean apparent volumes of distribution ranging from 1.9-2.9 L/kg in their investigation of food and formulation effects.2

Protein binding

Selinexor is 95% bound to plasma proteins.Label


Selinexor is known to be metabolized through CYP3A4, UDP‐glucuronosyltransferases, and glutathione S-transferases although the metabolite profile has yet to be characterized in published literature.Label The primary metabolites found in urine and plasma are glucuronide conjugates.3

Route of elimination
Not Available
Half life

Selinexor has a mean half-life of elimination of 6-8 hours.Label,1,2,3


Selinexor has a mean apparent clearance of 17.9 L/h.Label

Not Available
Affected organisms
Not Available
Not Available
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
AmbrisentanThe excretion of Ambrisentan can be decreased when combined with Selinexor.
AtorvastatinThe excretion of Atorvastatin can be decreased when combined with Selinexor.
Bempedoic acidThe excretion of Bempedoic acid can be decreased when combined with Selinexor.
CaspofunginThe excretion of Caspofungin can be decreased when combined with Selinexor.
CenobamateThe serum concentration of Selinexor can be decreased when it is combined with Cenobamate.
CholecystokininThe excretion of Cholecystokinin can be decreased when combined with Selinexor.
Cholic AcidThe excretion of Cholic Acid can be decreased when combined with Selinexor.
CobimetinibThe excretion of Cobimetinib can be decreased when combined with Selinexor.
Conjugated estrogensThe excretion of Conjugated estrogens can be decreased when combined with Selinexor.
DocetaxelThe excretion of Docetaxel can be decreased when combined with Selinexor.
Additional Data Available
  • Extended Description
    Extended Description

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  • Severity

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  • Evidence Level
    Evidence Level

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  • Action

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Food Interactions
  • Take with or without food. Co-administration with food does not affect pharmacokinetics.


General References
  1. Alexander TB, Lacayo NJ, Choi JK, Ribeiro RC, Pui CH, Rubnitz JE: Phase I Study of Selinexor, a Selective Inhibitor of Nuclear Export, in Combination With Fludarabine and Cytarabine, in Pediatric Relapsed or Refractory Acute Leukemia. J Clin Oncol. 2016 Dec;34(34):4094-4101. doi: 10.1200/JCO.2016.67.5066. Epub 2016 Oct 31. [PubMed:27507877]
  2. Gounder MM, Zer A, Tap WD, Salah S, Dickson MA, Gupta AA, Keohan ML, Loong HH, D'Angelo SP, Baker S, Condy M, Nyquist-Schultz K, Tanner L, Erinjeri JP, Jasmine FH, Friedlander S, Carlson R, Unger TJ, Saint-Martin JR, Rashal T, Ellis J, Kauffman M, Shacham S, Schwartz GK, Abdul Razak AR: Phase IB Study of Selinexor, a First-in-Class Inhibitor of Nuclear Export, in Patients With Advanced Refractory Bone or Soft Tissue Sarcoma. J Clin Oncol. 2016 Sep 10;34(26):3166-74. doi: 10.1200/JCO.2016.67.6346. Epub 2016 Jul 25. [PubMed:27458288]
  3. Abdul Razak AR, Mau-Soerensen M, Gabrail NY, Gerecitano JF, Shields AF, Unger TJ, Saint-Martin JR, Carlson R, Landesman Y, McCauley D, Rashal T, Lassen U, Kim R, Stayner LA, Mirza MR, Kauffman M, Shacham S, Mahipal A: First-in-Class, First-in-Human Phase I Study of Selinexor, a Selective Inhibitor of Nuclear Export, in Patients With Advanced Solid Tumors. J Clin Oncol. 2016 Dec;34(34):4142-4150. doi: 10.1200/JCO.2015.65.3949. Epub 2016 Oct 31. [PubMed:26926685]
  4. Gandhi UH, Senapedis W, Baloglu E, Unger TJ, Chari A, Vogl D, Cornell RF: Clinical Implications of Targeting XPO1-mediated Nuclear Export in Multiple Myeloma. Clin Lymphoma Myeloma Leuk. 2018 May;18(5):335-345. doi: 10.1016/j.clml.2018.03.003. Epub 2018 Mar 14. [PubMed:29610030]
  5. Xia Y, Shen S, Verma IM: NF-kappaB, an active player in human cancers. Cancer Immunol Res. 2014 Sep;2(9):823-30. doi: 10.1158/2326-6066.CIR-14-0112. [PubMed:25187272]
  6. Xpovio FDA Announcement [Link]
  7. Multiple Myeloma [Link]
  8. BC Cancer Agency: Treatment of Multiple Myeloma [Link]
  9. Clinical Trials: BOSTON Trial [Link]
  10. ChemSpider: Selinexor [Link]
  11. FDA Approved Drug Products: Xpovio oral tablets [Link]
External Links
PubChem Compound
PubChem Substance
FDA label
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Clinical Trials

Clinical Trials
1Active Not RecruitingTreatmentChronic Myelogenous Leukemia (CML) in Blast Crisis / Refractory Acute Lymphoblastic Leukemia (ALL) / Refractory Acute Myelogenous Leukemia (AML) / Refractory Biphenotypic Leukemia / Refractory Mixed Lineage Leukemia / Relapsed Acute Lymphoblastic Leukemia (ALL) / Relapsed Acute Myelogenous Leukemia (AML) / Relapsed Biphenotypic Leukemia / Relapsed Mixed Lineage Leukemia1
1Active Not RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML) / Leukemias1
1Active Not RecruitingTreatmentDe Novo Myelodysplastic Syndrome / Leukemia Acute Myeloid Leukemia (AML) / Myelodysplastic Syndrome / Secondary Acute Myeloid Leukemia (Secondary AML, sAML) / Secondary Myelodysplastic Syndromes1
1Active Not RecruitingTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
1Active Not RecruitingTreatmentMultiple Myeloma (MM) / Relapsed and/or Refractory Multiple Myeloma1
1Active Not RecruitingTreatmentPeripheral T-Cell Lymphoma (PTCL)1
1Active Not RecruitingTreatmentSoft Tissue Sarcoma (STS)1
1CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL) / Leukemia Acute Myeloid Leukemia (AML) / Mixed Phenotype Acute Leukemia (MPAL) / Myelodysplastic Syndromes (MDS)1
1CompletedTreatmentHaematological Malignancies1
1CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML)2
1CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML) / Secondary Acute Myeloid Leukemia (Secondary AML, sAML) / Untreated Adult Acute Myeloid Leukemia1
1CompletedTreatmentNeoplasms, Colorectal1
1CompletedTreatmentTumors, Solid1
1Not Yet RecruitingTreatmentAlveolar Soft Part Sarcoma (ASPS) / Ewing's Sarcoma (ES) / Liposarcoma / Malignant Peripheral Nerve Sheath Tumour (MPNST) / Sarcomas1
1RecruitingTreatmentAdult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Del(5q) / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(15;17)(q22;q12) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Recurrent Adult Acute Myeloid Leukemia / Secondary Acute Myeloid Leukemia (Secondary AML, sAML)1
1RecruitingTreatmentAdvanced Malignant Neoplasm / Recurrent Malignant Neoplasm / Refractory Malignant Neoplasm1
1RecruitingTreatmentChildhood Central Nervous System Neoplasm / Childhood Lymphoma / Childhood Solid Neoplasm / Gliomas, Malignant / Recurrent Brain Neoplasm / Recurrent Childhood Central Nervous System Neoplasm / Recurrent Childhood Glioblastoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Refractory Central Nervous System Neoplasm / Refractory Lymphomas / Refractory Malignant Solid Neoplasm / Refractory Primary Central Nervous System Neoplasm / Tumors, Solid / WHO Grade III Glioma1
1RecruitingTreatmentChronic Lymphocytic Leukemia (CLL) - Refractory / Leukemia, Prolymphocytic / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Small Lymphocytic Lymphoma1
1RecruitingTreatmentColorectal Cancer (CRC) / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1RecruitingTreatmentEndometrial Cancer / Ovarian Cancer1
1RecruitingTreatmentGlioblastomas / Gliosarcoma / Newly Diagnosed1
1RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML) / Lymphoma, Large B-Cell, Diffuse (DLBCL) / Non-Hodgkin's Lymphoma (NHL)1
1RecruitingTreatmentLymphoma, B-Cell1
1RecruitingTreatmentRectal Neoplasms1
1RecruitingTreatmentRecurrent Melanoma1
1RecruitingTreatmentRefractory Multiple Myeloma1
1RecruitingTreatmentTumors, Solid1
1TerminatedTreatmentEsophageal Cancers / Malignant Neoplasm of Stomach1
1, 2Active Not RecruitingTreatmentAcinar Cell Adenocarcinoma of the Pancreas / Duct Cell Adenocarcinoma of the Pancreas / Stage IV Pancreatic Cancer1
1, 2Active Not RecruitingTreatmentMultiple Myeloma (MM)1
1, 2CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1, 2CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML) / Leukemias1
1, 2RecruitingTreatmentDrug Use / GIST / Maximum Tolerated Dose / Metastatic Adult Soft Tissue Sarcoma / Therapeutic Agent Toxicity1
1, 2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2RecruitingTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL) / Recurrent B-Cell Non-Hodgkin Lymphoma / Recurrent Extranodal Marginal Zone Lymphoma / Recurrent Follicular Lymphoma / Recurrent Indolent Adult Non-Hodgkin Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Waldenstrom Macroglobulinemia / Refractory B-Cell Non-Hodgkin Lymphoma / Refractory Extranodal Marginal Zone Lymphoma / Refractory Follicular Lymphoma / Refractory Mantle Cell Lymphoma / Stage III Non-Hodgkin Lymphoma / Stage IV Non-Hodgkin Lymphoma / Transformed Recurrent Non-Hodgkin Lymphoma1
1, 2RecruitingTreatmentMultiple Myeloma (MM)2
1, 2WithdrawnTreatmentDiabetic Foot Ulcers (DFU)1
1, 2WithdrawnTreatmentMultiple Myeloma (MM)1
1, 2WithdrawnTreatmentRecurrent Squamous Cell Lung Carcinoma / Stage IV Squamous Cell Lung Carcinoma1
2Active Not RecruitingTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
2Active Not RecruitingTreatmentMyelodysplastic Syndromes1
2CompletedTreatmentAcute Myeloid Leukemia (Relapsed/Refractory)1
2CompletedTreatmentBreast Cancer1
2CompletedTreatmentBreast Cancer / Cervical Carcinoma / Endometrial Carcinoma / Ovarian Carcinoma1
2CompletedTreatmentGlioblastomas / Gliomas1
2CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML)1
2CompletedTreatmentMultiple Myeloma (MM)1
2CompletedTreatmentNeuroendocrine Carcinomas1
2Not Yet RecruitingTreatmentInfections, Coronavirus / Novel Coronavirus Infectious Disease (COVID-19)1
2RecruitingTreatmentAdvanced thymic carcinoma / Advanced Thymic Epithelial Tumor1
2RecruitingTreatmentAdvanced thymic carcinoma / Advanced Thymic Epithelial Tumour1
2RecruitingTreatmentInfections, Coronavirus / Novel Coronavirus Infectious Disease (COVID-19)1
2RecruitingTreatmentMultiple Myeloma in Relapse / Relapse/Refractory Multiple Myeloma1
2RecruitingTreatmentPost Essential Thrombocythaemia Myelofibrosis / Post Polycythemia Vera Myelofibrosis / Primary Myelofibrosis1
2RecruitingTreatmentRefractory Multiple Myeloma1
2RecruitingTreatmentRelapsed/Refractory Diffuse Large B-Cell Lymphoma (DLBCL)1
2RecruitingTreatmentUntreated Adult Acute Myeloid Leukemia1
2TerminatedTreatmentCastration Levels of Testosterone / Hormone-Resistant Prostate Cancer / Metastatic Castration-Resistant Prostate Cancer (mCRPC) / Metastatic Prostate Carcinoma in the Soft Tissue / Prostate Carcinoma Metastatic in the Bone / PSA Progression / Stage IV Prostate Adenocarcinoma AJCC v71
2TerminatedTreatmentCutaneous T-Cell Lymphoma (CTCL) / Peripheral T-Cell Lymphoma (PTCL)1
2TerminatedTreatmentLeukemia Acute Myeloid Leukemia (AML)1
2TerminatedTreatmentProstate Cancer1
2TerminatedTreatmentRecurrent Small Cell Lung Carcinoma1
2TerminatedTreatmentRichter's Transformation1
2TerminatedTreatmentSquamous Cell Carcinoma (SCC)1
2WithdrawnTreatmentMultiple Myeloma (MM)1
2WithdrawnTreatmentMyelodysplastic Syndrome1
2, 3RecruitingTreatmentLiposarcomas, Dedifferentiated1
3Active Not RecruitingTreatmentMultiple Myeloma (MM)1
3RecruitingTreatmentEndometrial Cancer1
Not AvailableActive Not RecruitingTreatmentAdvanced / Metastatic / Recurrent / Salivary Gland Cancers1
Not AvailableNo Longer AvailableNot AvailableMultiple Myeloma (MM)1


Not Available
Not Available
Dosage forms
Tablet, film coatedOral20 mg/1
Not Available
Patent NumberPediatric ExtensionApprovedExpires (estimated)
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Experimental Properties
water solubility20mg/mLChemSpider: Selinexor
Predicted Properties
Water Solubility0.00555 mg/mLALOGPS
pKa (Strongest Acidic)12.18ChemAxon
pKa (Strongest Basic)1.34ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area97.62 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity120 m3·mol-1ChemAxon
Polarizability35.61 Å3ChemAxon
Number of Rings3ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available


Mass Spec (NIST)
Not Available
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available


This compound belongs to the class of organic compounds known as phenyl-1,2,4-triazoles. These are organic compounds containing a 1,2,4-triazole substituted by a phenyl group.
Organic compounds
Super Class
Organoheterocyclic compounds
Sub Class
Direct Parent
Alternative Parents
Trifluoromethylbenzenes / Pyrazines / Imidolactams / Vinylogous amides / Heteroaromatic compounds / Acrylic acids and derivatives / Carboxylic acid hydrazides / Azacyclic compounds / Organonitrogen compounds / Organofluorides
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Phenyl-1,2,4-triazole / Trifluoromethylbenzene / Monocyclic benzene moiety / Pyrazine / Benzenoid / Imidolactam / Acrylic acid or derivatives / Heteroaromatic compound / Vinylogous amide / Carboxylic acid hydrazide
show 14 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available


Pharmacological action
General Function
Mediates the nuclear export of cellular proteins (cargos) bearing a leucine-rich nuclear export signal (NES) and of RNAs. In the nucleus, in association with RANBP3, binds cooperatively to the NES on its target protein and to the GTPase RAN in its active GTP-bound form (Ran-GTP). Docking of this complex to the nuclear pore complex (NPC) is mediated through binding to nucleoporins. Upon transit of a nuclear export complex into the cytoplasm, disassembling of the complex and hydrolysis of Ran-GTP to Ran-GDP (induced by RANBP1 and RANGAP1, respectively) cause release of the cargo from the export receptor. The directionality of nuclear export is thought to be conferred by an asymmetric distribution of the GTP- and GDP-bound forms of Ran between the cytoplasm and nucleus. Involved in U3 snoRNA transport from Cajal bodies to nucleoli. Binds to late precursor U3 snoRNA bearing a TMG cap.
Specific Function
Nuclear export signal receptor activity
Gene Name
Uniprot ID
Uniprot Name
Molecular Weight
123384.98 Da


Pharmacological action
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
Uniprot ID
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da


Pharmacological action
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
Uniprot ID
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da

Drug created on October 20, 2016 15:03 / Updated on May 16, 2020 15:51

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