On October 27, 2022 Salarius Pharmaceuticals, Inc. (NASDAQ: SLRX), a clinical-stage biopharmaceutical company using protein inhibition and protein degradation to develop cancer therapies for patients in need of new treatment options, reported favorable preclinical data that support continued development of the company’s Targeted Protein Degrader (TPD), SP-3164 (Press release, Salarius Pharmaceuticals, OCT 27, 2022, View Source [SID1234622551]). The data were presented on October 26 at the 5th 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.
Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:
Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing
Schedule Your 30 min Free Demo!
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 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 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 in vivo studies including statistically significant improvement over the approved immunomodulatory drugs lenalidomide (Revlimid) and pomalidomide (Pomalyst) 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.
"We are delighted by the reception Dr. Santiesteban’s presentation received," said David Arthur, chief executive officer of Salarius. "These initial data explain why we believe SP-3164 is so exciting, with the potential to make a positive difference in the treatment of hematologic cancers. Our near-term plans for SP-3164 include research in multiple blood cancers, additional pharmacokinetic and pharmacodynamic work to better understand potential clinical dosing advantages and additional studies to explore immuno-oncology effects and potential combinations for SP-3164.
"We are looking forward to providing additional preclinical information at the upcoming American Society of Hematology (ASH) (Free ASH Whitepaper) annual meeting later this year, completing our Investigational New Drug (IND)-enabling studies, submitting the SP-3164 IND to the U.S. Food and Drug Administration in the first half of 2023 and beginning clinical trials shortly thereafter," Mr. Arthur added.