Selinexor

In nonclinical studies, selinexor reversibly inhibits nuclear export of tumor suppressor proteins (TSPs), growth regulators, and mRNAs of oncogenic proteins by blocking exportin 1 (XPO1). XPO1 inhibition by selinexor leads to accumulation of TSPs in the nucleus and reductions in several oncoproteins, such as c-myc and cyclin D1, cell cycle arrest, and apoptosis of cancer cells.

• XPOVIO is a nuclear export inhibitor indicated: In combination with bortezomib and dexamethasone for the treatment of adult patients with multiple myeloma who have received at least one prior therapy ( 1.1 ). In combination with dexamethasone for the treatment of adult patients with relapsed or refractory multiple myeloma who have received at least four prior therapies and whose disease is refractory to at least two proteasome inhibitors, at least two immunomodulatory agents, and an anti-CD38 monoclonal antibody ( 1.1 ).ICD-10: C90.00

• None. None ( 4 ).contraindicated

Multiple Myeloma in Combination with Bortezomib and Dexamethasone (XVd) : Recommended dosage of XPOVIO is 100 mg taken orally once weekly in combination with bortezomib and dexamethasone ( 2.1 ). Multiple Myeloma in Combination with Dexamethasone (Xd) : Recommended dosage of XPOVIO is 80 mg taken orally on Days 1 and 3 of each week in combination with dexamethasone ( 2.1 ). See Full Prescribing Information for dosage in patients with severe hepatic impairment ( 2.5 , 8.6 ). 2.1 Recommended Dosage for Multiple Myeloma In Combination with Bortezomib and Dexamethasone (XVd) The recommended dosage of XPOVIO is 100 mg taken orally once weekly on Day 1 of each week until disease progression or unacceptable toxicity in combination with: Bortezomib 1.3 mg/m 2 administered subcutaneously once weekly on Day 1 of each week for 4 weeks followed by 1 week off. Dexamethasone 20 mg taken orally twice weekly on Days 1 and 2 of each week. Refer to Clinical Studies ( 14.1 ) and the prescribing information of bortezomib and dexamethasone for additional dosing information. In Combination with Dexamethasone (Xd) The recommended dosage of XPOVIO is 80 mg taken orally on Days 1 and 3 of each week until disease progression or unacceptable toxicity in combination with dexamethasone 20 mg taken orally with each dose of XPOVIO on Days 1 and 3 of each week. For additional information regarding the administration of dexamethasone, refer to its prescribing information.

Thrombocytopenia : Monitor platelet counts throughout treatment. Manage with dose interruption and/or reduction and supportive care ( 2.4 , 5.1 ). Neutropenia : Monitor neutrophil counts throughout treatment. Manage with dose interruption and/or reduction and granulocyte colony-stimulating factors ( 2.4 , 5.2 ). Gastrointestinal Toxicity : Nausea, vomiting, diarrhea, anorexia, and weight loss may occur. Provide antiemetic prophylaxis. Manage with dose interruption and/or reduction, antiemetics, and supportive care ( 2.4 , 5.3 ). Hyponatremia : Monitor serum sodium levels throughout treatment. Correct for concurrent hyperglycemia and high serum paraprotein levels. Manage with dose interruption, reduction, or discontinuation, and supportive care ( 2.4 , 5.4 ). Serious Infection : Monitor for infection and treat promptly ( 5.2 , 5.5 ). Neurological Toxicity : Advise patients to refrain from driving and engaging in hazardous occupations or activities until neurological toxicity resolves. Optimize hydration status and concomitant medications to avoid dizziness or mental status changes ( 5.6 ). Embryo-Fetal Toxicity : Can cause fetal harm. Advise females of reproductive potential and males with a female partner of reproductive potential, of the potential risk to a fetus and use of effective contraception ( 5.7 , 8.1 , 8.3 ). Cataract : Cataracts may develop or progress. Treatment of cataracts usually requires surgical removal of the cataract ( 5.8 ). 5.1 Thrombocytopenia XPOVIO can cause life-threatening thrombocytopenia, potentially leading to hemorrhage.

The following clinically significant adverse reactions are described in detail in other labeling sections: Thrombocytopenia [see Warnings and Precautions ( 5.1 )] . Neutropenia [see Warnings and Precautions ( 5.2 )] . Gastrointestinal Toxicity [see Warnings and Precautions ( 5.3 )] . Hyponatremia [see Warnings and Precautions ( 5.4 )] . Serious Infection [see Warnings and Precautions ( 5.5 )] . Neurological Toxicity [see Warnings and Precautions ( 5.6 )] . Cataract [see Warnings and Precautions ( 5.8 )] . The most common adverse reactions (≥20%) in patients with multiple myeloma who receive XVd are fatigue, nausea, decreased appetite, diarrhea, peripheral neuropathy, upper respiratory tract infection, weight decreased, cataract, and vomiting. Grade 3-4 laboratory abnormalities (≥10%) are thrombocytopenia, lymphopenia, hypophosphatemia, anemia, hyponatremia, and neutropenia ( 6.1 ). The most common adverse reactions (≥20%) in patients with multiple myeloma who receive Xd are thrombocytopenia, fatigue, nausea, anemia, decreased appetite, weight decreased, diarrhea, vomiting, hyponatremia, neutropenia, leukopenia, constipation, dyspnea, and upper respiratory tract infection ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Karyopharm Therapeutics Inc. at 1-888-209-9326 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Lactation : Advise not to breastfeed ( 8.2 ). 8.1 Pregnancy Risk Summary Based on findings in animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , XPOVIO can cause fetal harm when administered to a pregnant woman. There are no available data in pregnant women to inform the drug-associated risk. In animal reproduction studies, administration of selinexor to pregnant rats during organogenesis resulted in structural abnormalities and alterations to growth at exposures that were below those occurring clinically at the recommended dose (see Data ) . Advise pregnant women of the risks to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal data In an embryo-fetal development study in pregnant rats, daily oral administration of selinexor at 0, 0.25, 0.75, or 2 mg/kg throughout organogenesis caused incomplete or delayed ossification, skeletal variations, and reduced fetal weight compared with controls at a dose of 0.75 mg/kg (approximately 0.08-fold of human area under the curve [AUC] at the recommended dose).

Metabolism

Selinexor C max and AUC increased proportionally over a dose range from 3 mg/m 2 to 85 mg/m 2 (0.05 to 1.44) times the maximum approved recommended dose, based on 1.7 m 2 body surface area. No clinically relevant accumulation at steady state was observed.

• Jul 3, 2019NDANDA212306Karyopharm Theraps

1. 1Nausea2,55931%
2. 2Fatigue1,93723%
3. 3Decreased Appetite1,36716%
4. 4Diarrhoea1,28815%
5. 5Plasma Cell Myeloma1,15714%
6. 6Vomiting92811%
7. 7Asthenia85010%
8. 8Death83210.0%
9. 9Thrombocytopenia7358.8%
10. 10Platelet Count Decreased6637.9%
11. 11Weight Decreased6377.6%
12. 12Off Label Use5046.0%
13. 13Pneumonia4645.6%
14. 14Anaemia4635.5%
15. 15Dizziness4505.4%

The 10 most recently updated of 201 ClinicalTrials.gov registrations naming Selinexor as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of the Drug Selinexor With Radiation Therapy in Patients With Newly-Diagnosed Diffuse Intrinsic Pontine (DIPG) Glioma and High-Grade Glioma (HGG)
  Recruiting · Phase 1 · Phase 2 · Interventional · 132 enrolled · National Cancer Institute (NCI)
  NCT05099003updated 2026-06-12
• Study Assessing Activity of Intravenous (IV) Etentamig Monotherapy Versus Standard Available Therapies in Adult Participants With Relapsed or Refractory Multiple Myeloma
  Recruiting · Phase 3 · Interventional · 380 enrolled · AbbVie
  NCT06158841updated 2026-06-12
• Testing Atezolizumab With Selinexor in People ≥ 12 Years Old With Alveolar Soft Part Sarcoma, The AXIOM Trial
  Recruiting · Phase 2 · Interventional · 27 enrolled · National Cancer Institute (NCI)
  NCT05333458updated 2026-06-12
• NRSTS2021, A Risk Adapted Study Evaluating Maintenance Pazopanib, Limited Margin, Dose-Escalated Radiation Therapy and Selinexor in Non-Rhabdomyosarcoma Soft Tissue Sarcoma (NRSTS)
  Recruiting · Phase 1 · Phase 2 · Interventional · 139 enrolled · St. Jude Children's Research Hospital
  NCT06239272updated 2026-06-10
• Selinexor Maintenance Post CAR-T Cell Therapy for Multiple Myeloma
  Recruiting · Phase 1 · Interventional · 20 enrolled · Washington University School of Medicine
  NCT07200102updated 2026-06-08
• Selinexor in Myelofibrosis Refractory or Intolerant to JAK1/2 Inhibitors
  Terminated · Phase 2 · Interventional · 17 enrolled · University of Utah
  NCT03627403updated 2026-06-08
• The Efficacy and Safety of Selinisole Combined With Azacitidine and Venetoclax in the Treatment of Newly Diagnosed High-risk Myeloid Tumors With TP53 Mutations
  Not yet recruiting · Interventional · 30 enrolled · Bing Han
  NCT07632170updated 2026-06-08
• Selinexor Monotherapy for Cytoreduction in BCR::ABL1-Negative Myeloproliferative Neoplasms
  Not yet recruiting · Phase 2 · Interventional · 15 enrolled · Zhongshan Hospital (Xiamen), Fudan University
  NCT07626021updated 2026-06-04
• HCMT/MM2401: Ph2 Study of Selinexor + Bispecific Antibody for RRMM
  Recruiting · Phase 2 · Interventional · 27 enrolled · Duke University
  NCT06822972updated 2026-06-04
• Clinical Study of XPO-1 Inhibitors Plus CAR-T Cells in Relapsed Refractory B-cell Non-Hodgkin's Lymphoma
  Completed · Phase 2 · Interventional · 20 enrolled · The First Affiliated Hospital of Soochow University
  NCT05322330updated 2026-06-02

Frequently asked questions

How does Selinexor work?

In nonclinical studies, selinexor reversibly inhibits nuclear export of tumor suppressor proteins (TSPs), growth regulators, and mRNAs of oncogenic proteins by blocking exportin 1 (XPO1). XPO1 inhibition by selinexor leads to accumulation of TSPs in the nucleus and reductions in several oncoproteins, such as c-myc and cyclin D1, cell cycle arrest, and apoptosis of cancer cells.

What is Selinexor used for?

According to FDA labeling, Selinexor carries indications including: XPOVIO is a nuclear export inhibitor indicated: In combination with bortezomib and dexamethasone for the treatment of adult patients with multiple myeloma who have received at least one prior therapy ( 1.1 ). In combination with dexamethasone for the treatment of adult patients with relapsed or refractory multiple myeloma who have received at least four prior therapies and whose disease is refractory to at least two proteasome inhibitors, at least two immunomodulatory agents, and an anti-CD38 monoclonal antibody ( 1.1 ).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Selinexor?

Selinexor is classified as Other antineoplastic agents, Nuclear Export Inhibitor, Membrane Transporter Interactions, Nuclear Export Inhibitors, Cellular Cycle Alteration, Cellular Transport Alteration, Increased Cellular Death.

What are the brand names for Selinexor?

Selinexor is marketed under brand names including Xpovio.

What are the contraindications for Selinexor?

Selinexor labeling lists contraindications including: None. None ( 4 ).. Always consult the full prescribing information and a clinician.