Xpovio

Multiple myeloma — in combination with bortezomib and dexamethasone for adult patients who have received at least one prior therapy; in combination with dexamethasone for adults with relapsed/refractory disease after at least four prior therapies; Diffuse large B-cell lymphoma (DLBCL) — relapsed or refractory after at least two lines of systemic therapy

MM (with bortezomib + dex): 100 mg PO once weekly on Day 1 of each week during Weeks 1-8 of 35-day cycles
MM (with dex only): 80 mg PO on Days 1 and 3 of each week
DLBCL: 60 mg PO on Days 1 and 3 of each week
Take with or without food on scheduled days
Supportive care: Initiate antiemetics (5-HT3 antagonist ± other agents), maintain hydration

Tablets: 20 mg

None listed.

• Thrombocytopenia: 74% (Grade 3-4: 61% in MM). Monitor platelets at baseline, during treatment. May require platelet transfusions and/or dose modification.
• Neutropenia: 34% (Grade 3-4: 21%). Monitor ANC at baseline and during treatment. Consider G-CSF.
• Gastrointestinal Toxicity: Nausea (72%), vomiting (41%), diarrhea (44%), anorexia (53%). Initiate prophylactic antiemetics and maintain hydration.
• Hyponatremia: 39% (Grade 3-4: 22%). Monitor sodium at baseline and during treatment.
• Serious Infection: 32% (Grade ≥3). Including pneumonia and sepsis.
• Neurological Toxicity: Including dizziness, syncope, mental status changes.
• Cataracts: New onset or worsening in 4-7%. Ophthalmologic exams recommended.
• Embryo-Fetal Toxicity

Thrombocytopenia (74%), fatigue (63%), nausea (72%), anorexia/weight loss (53%), anemia (59%), diarrhea (44%), vomiting (41%), hyponatremia (39%), neutropenia (34%), leukopenia (29%), constipation (17%)

Thrombocytopenia (74%, Grade 3-4 in 47%). Neutropenia (34%, Grade 3-4 in 21%). Monitor CBC frequently. Hyponatremia in 44% (Grade 3-4 in 14%). Nausea in 66% — use prophylactic 5-HT3 antagonist.

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Thrombocytopenia (74%, Grade 3-4 in 47%). Neutropenia (34%, Grade 3-4 in 21%). Monitor CBC frequently. Hyponatremia in 44% (Grade 3-4 in 14%). Nausea in 66% — use prophylactic 5-HT3 antagonist.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Selinexor is a first-in-class selective inhibitor of nuclear export (SINE) compound that blocks Exportin 1 (XPO1, also known as CRM1). XPO1 mediates the nuclear export of over 200 cargo proteins, including tumor suppressor proteins (p53, Rb, p21, p27, FOXO, IκB) and oncoproteins (c-Myc, Cyclin D1). By inhibiting XPO1, selinexor causes nuclear accumulation and functional restoration of tumor suppressors while reducing oncoproteins, leading to cell cycle arrest and apoptosis in cancer cells.

Tmax: approximately 4 hours. Half-life: 6-8 hours. Protein binding: 95%. Metabolized by CYP3A4 and multiple other CYP enzymes and glucuronidation. Excreted in feces and urine.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• STORM — Selinexor + dexamethasone in penta-refractory MM. Phase IIb, n=123.
  🔬 NCT02336815 ↗ 📄 Primary Publication ↗

Xpovio has FDA-approved indications across the following cancer types covered on PipelineEvidence: