Drug intelligence / Profile preview

selinexor + lomustine

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

Overview

**Selinexor + lomustine** is a combination of two small molecule antineoplastic drugs studied specifically for recurrent glioblastoma (rGBM). **Selinexor** is a first-in-class, oral selective inhibitor of nuclear export (SINE), specifically targeting exportin-1 (XPO1), resulting in the nuclear retention and reactivation of tumor suppressor proteins[4]. **Lomustine** is an alkylating agent from the nitrosourea class that cross-links DNA, inducing cytotoxicity primarily in rapidly dividing cells. This combination exploits the synergistic anti-tumor effects observed in preclinical models, and was specifically investigated in a terminated Phase 1/2 clinical trial (NCT04421378, XPORT-GBM-029)[1][2][3][4][5]. The primary indication is for first relapse or recurrent GBM after frontline radiation and temozolomide. Selinexor was developed by Karyopharm Therapeutics.

Other names
selinexor + lomustine
02

Targets

DNAXPO1 (Exportin-1)

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