The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 07, 2021

Filed:

Apr. 20, 2020
Applicant:

The Johns Hopkins University, Baltimore, MD (US);

Inventors:

Barbara S. Slusher, Baltimore, MD (US);

Anne Le, Baltimore, MD (US);

Takashi Tsukamoto, Ellicott City, MD (US);

Assignee:

THE JOHNS HOPKINS UNIVERSITY, Baltimore, MD (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 417/12 (2006.01); C07D 417/14 (2006.01); C07D 285/135 (2006.01); A61K 9/51 (2006.01); A61K 9/00 (2006.01); A61K 31/433 (2006.01); A61K 45/06 (2006.01); A61K 31/337 (2006.01);
U.S. Cl.
CPC ...
A61K 9/5153 (2013.01); A61K 9/0019 (2013.01); A61K 9/5146 (2013.01); A61K 31/337 (2013.01); A61K 31/433 (2013.01); A61K 45/06 (2013.01); C07D 285/135 (2013.01); C07D 417/12 (2013.01); C07D 417/14 (2013.01);
Abstract

Currently available glutaminase inhibitors are generally poorly soluble, metabolically unstable, and/or require high doses, which together reduce their efficacy and therapeutic index. These can be formulated into nanoparticles and delivered safely and effectively for treatment of pancreatic cancer and other glutamine addicted cancers. Studies demonstrate that nanoparticle delivery of BPTES, relative to use of BPTES alone, can be safely administered and provides dramatically improved tumor drug exposure, resulting in greater efficacy. GLS inhibitors can be administered in higher concentrations with sub-100 nm nanoparticles, since the nanoparticles package the drug into 'soluble' colloidal nanoparticles, and the nanoparticles deliver higher drug exposure selectively to the tumors due to the enhanced permeability and retention (EPR) effect. These factors result in sustained drug levels above the IC50 within the tumors for days, providing significantly enhanced efficacy compared to unencapsulated drug.


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