Glutaminase Inhibitor Discovery and Nanoparticle-Enhanced Delivery for cancer therapy
JHU REF: C13142
Invention novelty: An improved glutaminase (GLS) inhibitors delivery system to enhance efficacy and prolong glutaminase inhibitor drug levels in tumor for improve treatment of pancreatic cancer.
Value Proposition: Currently available glutaminase inhibitors are generally poorly soluble, metabolically unstable, and/or require high doses, which together reduce their efficacy and therapeutic index. Johns Hopkins researchers have developed more potent inhibitors and tumor-penetrating stealth nanoparticles to more effectively deliver the new potent glutaminase inhibitors. This new delivery system offers the following advantages:
• Inhibitors can be administered safely.
• Provide dramatically improved tumor drug exposure.
• Results in greater efficacy.
Technical Details: Johns Hopkins researchers used the structural information about the binding of BPTES to glutaminase to synthesize modification of BPTES to develop inhibitors with substantially improved potency. Taking advantage of the lipophilic nature the molecule was encapsulated into nanoparticles for sustained drug delivery.
Looking for Partners: To develope and commercialize the glutaminase inhibitors and the nanoparticle formulation for cancer therapy.
Stage of Development: Discovery, Preclinical
Data Availability: Under CDA/NDA
Patent Status: Pending
Publication(s)/Associated Cases: WO 2016/007647
Categories: Therapeutic/drug delivery vehicle
Keywords: Glutaminase inhibitor, Nanoparticle-enhanced delivery, Pancreatic ductal adenocarcinoma, cancer therapy