Cancer Treatment Using Inhibitors of Tyrosyl-Dna Phosphodiesterase (Tdp1)

Background:
The National Cancer Institute's Laboratory of Molecular Pharmacology is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize inhibitors of Tyrosyl-DNA phosphodiesterase (Tdp1). The technology is also available for exclusive and non-exclusive licensing.

Technology:
Tyrosyl-DNA phosphodiesterase (Tdp1) is an enzyme that repairs topoisomerase I (Top1)-mediated DNA damage induced by chemotherapeutic agents and ubiquitous DNA lesions that interfere with transcription. The current technology involves steroid derivatives that inhibit Tdp1.

Currently, there are various types of Top1 inhibitors used in chemotherapy. However, Tdp1 inhibitors are expected to be effective in combination therapy with Top1 inhibitors for the treatment of cancers.

R&D Status:
Pre-clinical (discovery)

IP Status:
U.S. Provisional Application No. 60/921,980 filed 05 Apr 2007

Value Proposition:

• Combining Tdp1 inhibitors with Top1 inhibitors would allow Tdp1 to potentiate the anti-proliferative activity of Top1 inhibitors
• May have selective activity towards tumor tissues
• Tdp1 inhibitors can also exhibit antitumor activity independently, as tumors are shown to have excess free radicals, and Tdp1 repairs DNA damage by oxygen radicals.

Contact Information:
John D. Hewes, Ph.D., NCI Technology Transfer Center
Phone: 301-435-3121
E-mail: Hewesj@mail.nih.gov

Reference:  #588 LF

Posted on 12/06/2007