Selinexor (1 brand name, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- XPOVIO
Contraindications
None.
Adverse Reactions
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)].
Mechanism of Action
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. Selinexor demonstrated pro-apoptotic activity in vitro in multiple myeloma cells and showed anti-tumor activity in murine xenograft models of multiple myeloma. The combination of selinexor and dexamethasone or bortezomib demonstrated synergistic cytotoxic effects in multiple myeloma in vitro and increased anti-tumor activity in murine xenograft multiple myeloma models in vivo, including those resistant to proteasome inhibitors.