Drug intelligence / Profile preview

selinexor + lenalidomide + methylprednisolone

Development stage
Phase 1
Lead developer
Karyopharm Therapeutics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Selinexor + lenalidomide + methylprednisolone is an **oral combination therapy** under clinical investigation for the treatment of multiple myeloma, particularly in patients refractory to prior therapies. - **Selinexor** is a small molecule, first-in-class selective inhibitor of nuclear export (SINE), blocking the nuclear export protein XPO1, leading to nuclear retention and activation of tumor suppressor proteins and apoptosis in cancer cells. - **Lenalidomide** is an immunomodulatory agent (IMiD) with anti-angiogenic, anti-proliferative, and immunomodulatory effects, whose mechanism includes the targeting of cereblon, resulting in the degradation of transcription factors essential for myeloma cell survival. - **Methylprednisolone** is a synthetic glucocorticoid corticosteroid used for its anti-inflammatory and cytotoxic effects on myeloma cells. The combination is administered in cycles, with all agents given orally. This combination is specifically under study in multiple myeloma patients who are refractory to lenalidomide-containing therapy, and each of the three drugs is approved individually for use in multiple myeloma, but this triple combination (with methylprednisolone rather than dexamethasone) is investigational[3].

02

Targets

CRBN (Cereblon)XPO1 (Exportin-1)GR (Glucocorticoid receptor)

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