U.S. patent on 3TC awarded to Emory University.

ATLANTA--(HealthWire)--July 23, 1996--The U.S. Patent and Trademark Office today awarded the patent on the antiviral drug 3TC (also known as Epivir[TM] or lamivudine) to Emory University in Atlanta, Ga.

3TC is an important component of the new AIDS "cocktail" therapies, in which two or more drugs which exert different kinds of selective pressures on the virus are administered together.

3TC was approved by the U.S. Food and Drug Administration for marketing and sale on Nov. 17, 1995, in combination with AZT for the treatment of HIV infection and AIDS as a "first line" therapy. Since its approval, the drug has obtained an impressive share of the HIV market. It is estimated that first year sales in this country may reach $300 million for the treatment of HIV. Some analysts estimate that worldwide sales of the drug could reach $1 billion per year or more for HIV treatment.

3TC also is now in clinical trials for the treatment of hepatitis B virus in the United States, Japan, China and other important markets. Approval of 3TC for the treatment of hepatitis B virus will significantly increase the sales of this drug over the HIV sales estimates.

"We are delighted," said Vince La Terza, director of Patents and Licensing for Emory. "Emory's 3TC patent is tangible evidence of the strength of Emory's antiviral research program and Emory's commitment to protecting important research results. Our portfolio of 3TC patent rights will significantly improve our ability to continue to fund this cutting edge and vital research effort."

Emory has been represented in this matter by Sherry Knowles Zalesky of Kilpatrick and Cody in Atlanta. According to Zalesky, Emory's patent claims on 3TC also have been allowed by the patent offices in Australia and Japan, and Emory expects to obtain similar coverage in other countries.

3TC is currently marketed in the United States by Glaxo Wellcome, Inc., a subsidiary of Glaxo Wellcome plc, a British corporation, under a license from BioChem Pharma, Inc., a Canadian corporation. 3TC is one of the two components of BCH-189, which originally was discovered by Dr. Bernard Belleau at BioChem Pharma. In technical terms, BCH-189 is a "racemate," which means that it is a mixture of two compounds that are mirror images of each other (called "optical isomers," or "enantiomers"). Dr. Belleau and Nghe Nguyen-Ba filed a patent application in the United States on Feb. 8, 1989, that disclosed how to obtain the mixture (BCH-189), but not the individual optical isomer which is being marketed as Epivir (3TC). This patent issued in the United States on Sept. 10, 1991, as U.S. Patent No. 5,047,407.

Dr. Dennis Liotta and Dr. Woo-Baeg Choi, Emory University, discovered a process to separate the mirror image compounds of BCH-189 using certain enzymes, and filed a patent application that described this invention on Feb. 1, 1990. A continuation of this application issued today as U.S. Patent No. 5,539,116. Dr. Liotta, formerly the chair of the Department of Chemistry at Emory, is now the vice president for research at Emory. Dr. Choi currently is a research fellow at Merck, Inc.

Another scientist at Emory who has been closely involved with the 3TC discovery and subsequent events is Dr. Raymond Schinazi. Dr. Schinazi is a professor of pediatrics at Emory, and director of the Laboratory of Biochemical Pharmacology and a research career scientist at the Veterans Affairs Medical Center in Atlanta. Dr. Schinazi recently served on the President's Commission on AIDS.

According to Dr. Schinazi, "3TC is one of the most exciting drugs resulting from the collaborative research efforts between scientists in Georgia. Its true potential will become apparent when it is approved for the treatment of hepatitis B virus."

Mr. La Terza indicated that this is a culmination of the major scientific contributions provided by Emory faculty in the discovery and development of 3TC and related drugs over the last 20 years.

"Emory University scientists have published some of the key papers on 3TC, including the discovery of the 184 point mutation caused by 3TC critical for the virus survival, which contributes to AZT's sustained effect in combination with 3TC in people infected with HIV," Mr. La Terza said. "This cocktail of antiviral drugs appears to completely suppress HIV in many patients, especially when administered with the new protease inhibitors."

CONTACT: Emory University News

Sarah Goodwin, 404/727-5686