Salarius Pharmaceuticals, Inc. announced favorable preclinical data that support continued development of the company's Targeted Protein Degrader (TPD), SP-3164. The data were presented on October 26 at the 5(th) Annual Targeted Protein Degradation Conference by Daniela Santiesteban, Ph.D., Salarius' director of targeted protein degradation development, in a presentation titled "Development of SP-3164, a Cereblon-Binding Molecular Glue The presentation is available for viewing on the company's website here.Dr. Santiesteban's presentation included an overview of SP-3164 development and the therapeutic benefits of a stereoselective molecular glue. SP-3164 was developed to be the deuterium-stabilized, active S-enantiomer, or the preferred enantiomer, of avadomide or CC-122.

Avadomide is a widely studied molecular glue with demonstrated clinical activity and established safety data. in vitro studies, SP-3164 has shown potent cereblon binding, efficient degradation of neosubstrates and induction of cell death in both lymphoma and multiple myeloma cells. in vivo studies, SP-3164 has shown minimal to no interconversion of the preferred S-enantiomer into the unwanted R-enantiomer, indicating successful stabilization.

In addition, SP-3164 showed significant tumor growth inhibition in vivo studies including statistically significant improvement over the approved immunomodulatory drugs lenalidomide (Revlimid(R)) and pomalidomide (Pomalyst(R)) in a multiple myeloma NCI-H929 mouse model. Dr. Santiesteban concluded that by eliminating the unwanted R-enantiomer, SP-3164 may lead to improved activity and safety, as demonstrated by deuterated R-enantiomer's lack of anticancer activity and its potential role in supporting tumor growth.