Eltanexor (KPT-8602) is an investigational second-generation SINE compound that, like selinexor, functions by binding with, and inhibiting, the nuclear export protein, XPO1, leading to the accumulation of tumor suppressor proteins in the cell nucleus. This reinitiates and amplifies their tumor suppressor function and is believed to lead to the selective induction of apoptosis in cancer cells, while largely sparing normal cells.
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 we are evaluating its safety, tolerability and efficacy in ongoing clinical studies.
Eltanexor is an investigational medicine and has not been approved by The United States Food and Drug Administration (FDA), Health Canada, the European Medicines Agency (EMA), nor any other regulatory agency.
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.