Advertisement

Topics

BODIPY-FL Nilotinib (Tasigna) for Use in Cancer Research

14:37 EDT 12 Jul 2018 | NIH

The National Cancer Institute''s Laboratory of Cell Biology is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize bodipy conjugated tyrosine kinase inhibitors that are currently used in the clinic for the treatment of CML or gastric cancers. We are also interested in evaluating third generation tyrosine kinase inhibitor derivatives as modulators of ABC drug transporters to improve the efficiency of chemotherapy in animal (mouse) model system. In addition, we can identify possible pharmacokinetic interactions of the novel kinase inhibitors with ABC drug transporters.

Investigators at the National Institutes of Health have produced a fluorescently labeled derivative of the clinically-approved, tyrosine kinase inhibitor (TKI) nilotinib (Tasigna) for use in research.  This was accomplished by conjugating the fluorescent dye BODIPY-FL to nilotinib.

The TKI imatinib (Gleevec) is the first targeted therapeutic developed and is used as first line treatment of Philadelphia chromosome-positive (Ph+) cancers like chronic myeloid leukemia (CML).  Although imatinib is highly effective, after continued use the cancer cells frequently become resistant to the drug.  Nilotinib is a second generation TKI developed to overcome imatinib resistance, but eventually it can also result in drug resistance.

The fluorescent nilotinib conjugate was developed to study the mechanism by which cancer cells become resistant to nilotinib and better understand its cytotoxic effects.

Development Status:

  • Ready for use
  • Pre-clinical data available 
IC: 
NCI
NIH Ref. No.: 
E-009-2010
Advantages: 
  • Material is ready for use reducing time and effort to duplicate
  • BODIPY-FL dye is compatible with commonly-used fluorescein dye optics and has superior fluorescent properties to fluorescein
  • BODIPY-FL Nilotinib (Tasigna) is compatible and can be used for both in vitro and in vivo studies.
Applications: 
  • Use in monitoring cellular accumulation of nilotinib using flow cytometry, fluorescent microscopy, or other fluorometric techniques
  • Use as an in vivo probe with experimental models and in clinical studies for analyzing drug efficacy, pharmacokinetic profile and drug localization
  • Use for the study of cytotoxic effects of nilotinib in important physiological locations such as the heart and brain
  • Use in identifying other potential targets of nilotinib in different types of cancer
  • Use in in vivo imaging to identify potential physiological barriers to drug penetration into tissues
Development Status: 

Prototype

Updated On: 
May 30, 2018
Provider Classifications: 
Publications: 
Licensing Contacts: 
Lead Inventor: 
Inventor IC: 
NCI
NCI
NCATS
NCI
Inventor Lab URL: 
http://irp.nih.gov/pi/suresh-ambudkar
https://ccr2.cancer.gov/resources/cbl/Scientists/Thomas.aspx
LPM FIrst Name: 
John
LPM Last Name: 
Hewes
Inv Is lead: 
LPM Phone: 
240-276-5515
LPM Suffix: 
Ph.D.
LPM Organization: 
NCI - National Cancer Institute
DTDT Classification: 
Research Materials
DTDT Description: 
Research Materials
Publication Link: 
https://www.ncbi.nlm.nih.gov/pubmed/21630681
Publication Caption: 
PMID 21630681
Publication Title: 

S. Shukla, et al. Synthesis and characterization of a BODIPY conjugate of the BCR-ABL kinase inhibitor Tasigna (nilotinib): evidence for transport of Tasigna and its fluorescent derivative by ABC drug transporters.

Collaboration Sought: 
Yes
Institute or Center: 
Collaboration Opportunity: 

Licensing only

E Number Only: 
E-009-2010
Inventor First Name: 
Suresh
Suneet
Amanda
Craig
Inventor Last Name: 
Ambudkar
Shukla
Skoumbourdis
Thomas

Original Article: BODIPY-FL Nilotinib (Tasigna) for Use in Cancer Research

NEXT ARTICLE

More From BioPortfolio on "BODIPY-FL Nilotinib (Tasigna) for Use in Cancer Research"

Advertisement
Quick Search
Advertisement
Advertisement

 

Relevant Topic

Cancer Disease
Cancer is not just one disease but many diseases. There are more than 100 different types of cancer. Most cancers are named for the organ or type of cell in which they start - for example, cancer that begins in the colon is called colon cancer; cancer th...