Long Acting Therapeutic Conjugates with Evans Blue

This invention is a platform technology that pertains to the advantages of conjugating therapeutics to Evans Blue thus providing long lasting pharmacokinetic profiles by complexing with albumin. Notably, albumin bound therapeutic- or prodrug-Evans Blue conjugates provide a complex with a total molecular size above 60 kDa thus eliminating the risk for renal clearance. Interestingly, since albumin also crosses the blood-brain barrier and since all circulating Evans Blue is bound to albumin, Evans Blue bound therapeutics or prodrugs can also cross the blood-brain barrier. By way for example but not limitation, Evans Blue can be conjugated to insulin, GLP-1, exendin-4, exendin (9-39), octreotide, bombesin, RGD peptide (arginylglycylaspartic acid), vascular endothelial growth factor (VEGF), interferon (IFN), tumor necrosis factor (TNF), asparaginase, or adenosine deaminase, exenatide, dipeptidyl peptidase-4 inhibitors, neuropilin, epidermal growth factor, islet neogenesis associated protein, alpha-1 antitrypsin, anti-inflammatory agents, glulisine, glucagons, local cytokines, modulators of cytokines, anti-apoptotic molecules, aptamers, asparaginase, adenosine deaminase, interferon alpha2a, interferon alpha2b, granulocyte colony stimulating factor, growth hormone receptor antagonists, doxorubicin, paclitaxel, gemcitabine, camptothecin, and temozolomide. Evans Blue conjugates according to this invention can additionally include radionuclides like 18F, 76Br, 124I, 125I, or 131I, or 117mSn for tracking or use in diagnostics.

Potential Commercial Applications: Competitive Advantages:
  • Diabetes therapeutics
  • Cancer therapeutics
  • CNS therapeutics
  • Pharmacokinetic/distribution studies
  • Long pharmacokinetic profile
  • No renal clearance of circulating drug

Development Stage:



Xiaoyuan Chen (NIBIB)  ➽ more inventions...

Lixin Lang (NIBIB)  ➽ more inventions...

Gang NIU (NIBIB)  ➽ more inventions...

Intellectual Property:
US Pat: 10,709,790 issued 2020-07-14
PCT Application No. PCT/US2016/038475 filed on 2016-06-21
US Application No. 62/182,694 filed on 2015-06-22

Licensing Contact:
Michael Shmilovich, J.D.
Email: shmilovm@mail.nih.gov
Phone: 301-435-5019

OTT Reference No: E-143-2015-0
Updated: Jun 27, 2016