WP1244 / WP1874 was designed, synthesized and patented at The University of Texas MD Anderson Cancer Center utilizing a "modular" drug design strategy.

This strategy combines intercalation and groove-binding modes into molecules with the requisite chirality and binding-site size to impart meaningful selectivity.

WP1244 and WP1874 (a water soluble mesylate salt of WP1244) represent a novel class of DNA binding agents with unique biological properties incorporating anthracycline and distamycin-based scaffolds to create agents designed to bind selectively extended sequences of DNA.

WP1244 is exceedingly potent with in vitro IC50 values in the subnanomolar range. A previous animal study confirmed the presence of WP1244 in murine brain tissue, thereby demonstrating its ability to cross the blood-brain barrier.



The WP1874 molecule will now be the primary focus of pre-clinical research conducted in this portfolio.

References

  • 1. Zielinski, R., Cardenas-Zuniga, R., Poimenidou M., et al. Neuro-Oncol. 2021; 23 (6):1