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Potent, Easy to Use Targeted Toxins as Anti-Tumor Agents

Posted Jun 15 2010 5:00pm

Description of Invention:
The invention discloses synthesis and use of novel derivatives of 2-[2'-(2-aminoethyl)-2-methyl-ethyl]-l,2-dihydro-6-methoxy-3H-dibenz-[de,h]isoquinoline-l,3-dione as targeted anti-tumor agents. The use of targeted toxin conjugates with anti-cancer antibodies, such as herceptin, is increasing. Based on a comparison with the structurally complex toxins, such as DM1, available in the market, these novel toxins are more stable in circulation, thus making the toxin-conjugates more tumor-selective and less toxic. As such, these compounds are superior alternatives to the existing toxins.

The invention describes a potent and easy to synthesize toxin that can be used for generating a variety of prodrugs. These compounds can be attached to a ligand that recognizes a receptor on cancer cells, or to a peptide that is cleaved by tumor-specific proteases. The compounds are topoisomerase inhibitors and are mechanistically different from DM1 that targets tubulin.

The structure of the toxin allows it to be modified with a peptide linker that is stable, but rapidly cleaved in lysosomes after the compound is specifically taken up by cancer cells.

The compounds can be used for preparation of a variety of potent anti-cancer agents with low systemic toxicity.

  • Easy to prepare
  • Structural features make these compounds more stable in circulation
  • Toxin conjugates are more tumor-selective and less toxic

Development Status:
In vitro studies are completed and in vivo animal model studies are ongoing.

Nadya I Tarasova (NCI)
Marcin D Dyba (NCI)
Christophr J Michejda (NCI)

Patent Status:
HHS, Reference No. E-160-2006/0
PCT, Application No. PCT/US2007/078233 filed 12 Sep 2007
US, Application No. 12/441,029 filed 12 Mar 2009

Cancer - Therapeutics
In-vivo Data
In-vitro Data

For Additional Information Please Contact:
Jennifer Wong
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-435-4633
Fax: 301-402-0220

Ref No: 1570

Updated: 06/2010

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