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Platinum-Acridine Chemotherapeutics That Effectively Kill Cancer Cells (REF # WFU 09-05)
Wake Forest Innovations USA flag USA
Abstract ID:
A new class of chemotherapy fights advanced and resistant cancer malignancies. Structurally unique compound has higher intracellular concentrations and improved DNA binding affinity, enabling it to target and destroy cancer cells at lower overall doses....
Contact Stephen j. Susalka, phd, clp
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Value Proposition

It is estimated that over 1.6 million people in the United States were diagnosed with cancer in 2013 (National Cancer Institute SEER database). New therapies with increased efficacy and lower side effect profiles have enormous market potential. Wake Forest University's cytotoxic platinum–acridine hybrid agent has been shown in preclinical models to effectively kill cancer cells that are inherently resistant to chemotherapy or have developed resistance over time. This includes a wide range of solid tumors, including lung, ovarian, breast and pancreatic cancers, as well as hematological malignancies, such as multiple myeloma.

Invention Summary

Chemists at Wake Forest University have developed a new class of platinum-acridine chemotherapeutics with significant potential for tackling highly advanced and chemoresistant malignancies. Traditional platinum-based chemotherapies are a mainstay of many cancer treatments, but systemic toxicity and various forms of resistance limit their efficacy. Wake Forest's novel platinum-acridine anticancer agent builds on the known efficacy of platinum-based therapies, improving the profile of these compounds by overcoming drug resistance and increasing cancer-killing potency. The structurally unique compound has improved intracellular concentrations and DNA binding affinity, enabling it to target and destroy cancer cells at lower overall doses than existing platinum-based therapies.

Competitive Benefits

• 500 x the cytotoxicity of cisplatin in NCI-H460 cell proliferation assays, with IC50 values in the nanomolar range

• Significantly reduced tumor growth in a highly aggressive H460 mouse xenograft model at doses lower than typical for cisplatin

• Excellent cytotoxic response in cancers resistant to conventional platinum therapy

• Rapid intracellular accumulation in tumor cells and higher DNA adduct levels lead to efficient cancer cell kill

• Excellent chemical versatility for modification with conjugatable functional groups using click chemistry

• Localization of drugs in nucleoli and possibility of targeting “nucleolar rRNA synthesis,” by stabilizing telomeric G-quadruplex DNA structures and inhibition of telomerase enzyme activity

• An emerging target in anticancer drug development

Application Fields

• An effective first- or second-line therapy for many solid tumor malignancies

• Demonstrated efficacy against chemoresistant non-small cell lung cancer (NSCLC)

• Compatible with liposomal nanoencapsulation for safe delivery and co-delivery with targeted antibody and/or chemosensitizing agents in the form of cleavable conjugates

Stage of Development

• Several compounds chemically and biologically fully characterized

• Synthetic procedures optimized; robust and amenable to high-throughput screening

• In vivo study completed and published, with additional in vivo studies underway

• Additional detail can be found in:

o Patent application nos. US 13/125,214;

o PCT/US09/061832 (nationalized in Canada, the European Patent Office, and Japan); and

o PCT/US2012/053189

Background

Traditional platinum-based chemotherapies are a mainstay of many cancer treatments, but systemic toxicity and various forms of resistance limit their efficacy.

Inventor

Ulrich Bierbach, PhD

Professor, Department of Chemistry

Wake Forest University

Key Words

• Platinum-acridine chemotherapeutics

• Platinum-based chemotherapies

Publications

• J. Med. Chem. 2008, 51, 7574-7580

• “Expanding Platinum's Potential. Paradigm Shift.” Nature/SciBx 2008, 1, 1-3

• ACS Med. Chem. Lett., 2011 Sep 8; 2(9): 687-691

• Metallomics, 2012, 4, 645-652

• J. Med. Chem., 2012, 55, 7817-7827

• J. Med. Chem., 2012, 55, 10198-10203
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Type of Business Relationship Sought
Exclusive Licensing Arrangement
Possibility of a parallel Sponsored Research Agreement
FEATURED
Last Updated Feb 2014
Technology Type THERAPEUTIC
Phase of Development PRECLINICAL
CORPORATION