A patent application has been submitted by Yale for 2',3'-Didehydro-3'-Deoxy-4'-Ethynylthymidine, or Ed4T, a compound with a new and potentially effective anti-HIV clinical treatment.
Ed4T is a thymidine analogue that blocks HIV-1 reverse transcriptase, the enzyme that is essential for viral replication. The compound was discovered and developed jointly by Professor Masanori Baba of Kagoshima University and Professor Hiromichi Tanaka of Showa University in Japan, and Yung-Chi Cheng, the Henry Bronson Professor of Pharmacology at Yale University School of Medicine.
An estimated 20 million people worldwide have died from AIDS and 40.3 million are infected with the virus. In 2004, a reported 1,000 patients in Japan were infected -- and the numbers are rapidly increasing.
"Yale is very proud of the contribution it makes to fighting the HIV pandemic though discovery of novel antiviral drugs," stated E. Jonathan Soderstrom, Managing Director of the Yale Office of Cooperative Research, which is responsible for licensing technologies on behalf of Yale inventors and their academic partners. "We are very pleased to be working in partnership with Oncolys Biopharma to commercialize Ed4T."
Since 1985, when AZT was introduced into clinical practice, 18 products have been approved and commercialized worldwide as anti-HIV-1 treatment. The drugs are in four categories, according to their various modes of action and chemical structures. Of the available drugs, seven are Nucleoside-analogue Reverse Transcriptase Inhibitors (NRTIs), three are Non NRTIs (NNRTI), seven are Protease Inhibitors, and one is a Fusion Inhibitor.
The current standard treatment for AIDS is HAART (Highly Active Anti-Retroviral Therapy), a combination regimen including drugs with different modes of action. HAART has two standard regimens: either treatment with two NRTIs plus one or two Protease Inhibitor(s), or treatment with two NRTIs plus one NNRTI.
However, during long-term treatment with anti-HIV-1 drugs, patients can develop a resistant strain of the virus, and require a new drug to counter the mutation.
Pharmacological studies have demonstrated that Ed4T has more potent anti-HIV activity than the existing NRTI and is active against those viruses that are resistant to the existing NRTI and NNRTI drugs. Further, Ed4T does not affect DNA synthesis in mitochondria, a toxic side effect of some nucleotide analogues. These findings suggested that Ed4T might offer unique therapeutic advantages over existing anti-HIV drugs.
Oncolys BioPharma Inc. was founded in March 2004 to develop and commercialize Telomelysin, an engineered virus that infects and destroys cancer cells. In March 2006, the company applied to the FDA for approval of a Clinical Study in patients with cancer. The company has recently added infectious disease as a strategic target. Further information on the company, headquartered in Tokyo, is available by contacting the company at +81-3-5575-3378 or firstname.lastname@example.org and online at http://www.oncolys.com.
The Yale University Office of Cooperative Research manages intellectual assets created at Yale. Further information on licensing agreements is available through email@example.com or at http://www.yale.edu/ocr/ online.
Antimicrob Agents Chemother. 48(5):1640-6 (May 2004). Novel 4'-Substituted Stavudine Analog with Improved
Anti-Human Immunodeficiency Virus Activity and Decreased Cytotoxicity
Antimicrob Agents Chemother. 49(8):3355-60 (Aug2005). Anti-human immunodeficiency virus type 1 activity and resistance profile of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine in vitro.
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