Unmet Need
Sorafenib, a kinase inhibitor, has been the gold-standard treatment for most individuals with hepatocellular carcinoma (HCC); however, studies suggest survival after treatment remains less than 15% (Raoul et al. 2019). Additionally, side effects, including hand-foot skin reactions and diarrhea, are prevalent in almost half of patients being treated for HCC, diminishing their overall comfort (Pang et al. 2022). Therefore, there exists a need for a multi-approach therapy to more efficiently stunt tumor growth and prolong the average survival rate.
Technology Description
Researchers at Johns Hopkins have developed a technology improving upon terameprocol, a synthetic derivative of nordihydroguaiaretic acid, that has been described as an anti-cancer treatment due to its similarities with transcription factor Sp1 (Smolewski et al. 2008). Optimization via the addition of two specific moieties (poly(ethylene glycol)and nitroimidazole), the researchers developed a novel drug that seeks unique tumor-specific microenvironments during HCC development, while enhancing overall solubility, to increase overall potency.
Value Proposition
· Increased bioavailability, with new moieties causing a 6.5-11.2-fold increase in solubility
· Preferentially bioactivated in HCC regions, releasing reactive radicals to eliminate cancer cells
· Maintains IC50 in the 10-15 μM range, only two-fold greater than sorafenib (Preuss et al. 2015)
Stage of Development
· Extensive characterization has confirmed chemical structure and regional makeup of the novel cancer-targeting compound, with excellent yield rates (> 80%)
· In vitro analysis confirms growth inhibition of cell cultures
Data Availability: Data available upon request, and in the publications below.
Publications
1. Hsu, M-H. et al., ChemMedChem (2014).
2. Gnabre, J. et al., J. of Trad. and Complementary Med. (2015).
3. Park, R. et al., Clin. Cancer Res. (2005).
Patent Information
1. Huang, R. et al. US20050267208A1
2. Chang, C-C. et al. AU2005294432A1
