Eltanexor is an investigational medicine and has not been approved by The United States Food and Drug Administration (USFDA), Health Canada, the European Medicines Agency (EMA), nor any other regulatory agency.
Eltanexor is an investigational second-generation SINE compound that, like selinexor, is designed to selectively block the nuclear export protein XPO1. Most of the key tumor suppressor proteins, or TSPs, are cargos of XPO1 and inhibition of XPO1 by eltanexor is believed to sequester TSPs in the nucleus where they can carry out their normal functions.
In preclinical models, eltanexor has a broad therapeutic window with minimal penetration of the blood brain barrier and, therefore, has the potential to serve as a second generation SINE compound for cancer indications. Following oral administration, animals treated with eltanexor show lower percentage of body weight loss and improved food consumption than animals similarly treated with selinexor. This allows more frequent dosing of eltanexor, enabling a longer period of exposure at higher levels than is possible with selinexor. As a result, we believe that eltanexor represents a second generation SINE compound and are evaluating safety, tolerability and efficacy in humans.
To learn about our Phase 1/2 clinical study with eltanexor, A Phase 1/2 Open-Label Study of the Safety, Tolerability and Efficacy of the Selective Inhibitor of Nuclear Export (SINE) Compound KPT-8602 in Patients With Relapsed/Refractory Cancer Indications, please visit clinicaltrials.gov