Drug intelligence / Profile preview

eltanexor + dexamethasone

Development stage
Unknown
Lead developer
Karyopharm Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Eltanexor + dexamethasone is a combination therapy of **eltanexor**, a selective inhibitor of nuclear export (SINE) compound targeting exportin 1 (XPO1), and **dexamethasone**, a synthetic glucocorticoid corticosteroid. Eltanexor works by inhibiting XPO1, resulting in nuclear retention of tumor suppressor proteins and promoting apoptosis of cancer cells. Dexamethasone acts via activation of the glucocorticoid receptor to induce anti-inflammatory and cytotoxic effects. The combination has shown synergistic efficacy in preclinical models and early clinical studies, particularly against hematologic malignancies such as multiple myeloma and acute lymphoblastic leukemia, through enhanced induction of apoptosis and cell cycle arrest by modulating NR3C1 (glucocorticoid receptor) and E2F-mediated transcription[1][4].

02

Targets

XPO1 (Exportin-1)GR (Glucocorticoid receptor)

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