Drug intelligence / Profile preview

decitabine + selinexor

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

Overview

**Decitabine + selinexor** is an investigational combination therapy composed of two small molecules, each with a distinct mechanism of action. **Decitabine** is a hypomethylating agent that inhibits DNA methyltransferase, leading to hypomethylation of DNA and potential reactivation of tumor suppressor genes. **Selinexor** is a first-in-class selective inhibitor of nuclear export (SINE) that targets the nuclear export protein exportin 1 (XPO1/CRM1), resulting in retention of tumor suppressor proteins in the nucleus, reactivation of tumor suppressor pathways, and induction of apoptosis in malignant cells. The combined regimen has been studied primarily in patients with relapsed or refractory acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), T lymphoblastic lymphoma (T-LBL), and secondary AML, where preclinical and early-phase clinical data suggest synergistic antileukemic effects, improved response rates compared to monotherapy, and a manageable safety profile[2][3][6][7][8].

02

Targets

DNMT1 (DNA (cytosine-5)-methyltransferase 1)XPO1 (Exportin-1)

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