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"New DRug stirs sceintists' hopes of halting AIDS" star ledger3/1/07, page two


motherinneed: - News - Star-Ledger - New drug stirs scientists' hopes of halting AIDS
An experimental AIDS drug, years in the making by scientists from Johnson & Johnson and Rutgers University, is part of an assortment of startlingly effective new treatments shown to zap resistant strains of HIV. Scientists from J&J's Tibot...
- NJ: Star-Ledger (Article) : Read More

New drug stirs scientists' hopes of halting AIDS
Thursday, March 01, 2007
Star-Ledger Staff
An experimental AIDS drug, years in the making by scientists from Johnson & Johnson and Rutgers University, is part of an assortment of startlingly effective new treatments shown to zap resistant strains of HIV.

Scientists from J&J's Tibotec division reported the results yesterday at the end of a major AIDS conference in Los Angeles. The drug, TMC-278, has long been viewed as the most promising of a family of revolutionary AIDS compounds called "DAPY" (rhymes with "happy') being developed by the New Brunswick drug giant.
"Right now, it looks as if this could be a home run for patients," said Roger Pomerantz, president of J&J's Tibotec Pharma Ltd. in Yardley, Pa., minutes after a presentation before a standing-room-only crowd of 4,000. "I am very jazzed about this. It's going to have a huge impact."

The J&J AIDS presentation followed a equally riveting talk by scientists from Gilead Sciences Inc. in California on their treatment advances, as well as announcements on Tuesday by Merck & Co. of Whitehouse and Pfizer of New York of major strides in AIDS treatment. All of the new drugs attack difficult-to-treat "resistant" strains of the virus and that news has energized the AIDS community.

"It's a brand-new day," said Stephen Smith, a physician-scientist who directs the department of infectious disease at Saint Michael's Medical Center in Newark. "This means that no one in the developed world should be walking around anymore with any detectable levels of virus in their blood. These drugs are just blowing me away."

The announcements made at the 14th annual Conference on Retroviruses and Opportunistic Infections, according to Smith and other experts, are as revolutionary as the breakthroughs of the mid-1990s when scientists developed drug cocktails to stop AIDS.

Merck's drug, MK-0518, blocks an enzyme called integrase that helps the virus replicate. The company plans to seek federal approval before July 1 to use the drug against resistant HIV, the deadly virus that causes AIDS. Gilead also presented promising results from tests on its integrase inhibitor, GS-9137, which is in second-stage testing.

Pfizer's HIV pill, named maraviroc, is the first of a new class of medicines called CCR5 inhibitors that block a chemical doorway used by the virus to infect cells. A chemical cocktail that included maraviroc suppressed the drug in patients who do not respond to older treatments, scientists reported.

Resistant strains, caused when the quick-change artist that is HIV morphs its shape and structure to survive lethal drug attacks, is a huge and growing medical problem. About 10 percent of new HIV patients are infected with a virus resistant to at least one type of AIDS drug, according to a study released earlier this week by the federal Centers for Disease Control and Prevention in Atlanta. And five people in 1,000, according to the study, suffer from a form that evades all three major AIDS therapies currently available.

TMC-278 ("Tibotec medical compound") is a non-nucleoside reverse transcriptase inhibitor. Like other drugs in this category, it jams the machinery of reverse transcriptase, one of the prime proteins responsible for the reproduction of HIV.

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But 278 is a DAPY compound, so it is special, according to its designers. So named because they have diarylpyrimidine at their core, these drugs are made of flexible molecules that find ways to fit into portals on the surface of proteins, like a master key adjusting to many locks.

"This drug sort of bobs and weaves, if you will, and stays in the pocket," said Pomerantz of Tibotec.


In data presented at the conference, Tibotec scientists said the drug was as effective at lowering HIV levels in newly diagnosed patients as Bristol-Myers Squibb's popular Sustiva.

Anton Pozniak, managing director of St. Stephen's AIDS Trust in London, who led the study, said drug combinations that included TMC-278 at three different dose levels lowered the amount of HIV as much as standard doses of Sustiva used in similar combinations.

The drug can be easily combined with others to form a single pill, company officials said, and causes fewer side effects than others on the market. In addition, the drug appears to be non-toxic to pregnant women and their fetuses, which could be an enormous benefit in the developing world where so many of the newly infected patients are women.

Two other Tibotec drugs, also DAPY compounds, are making steady progress, Pomerantz said. TMC-125, which does not combine as well into a single pill but is potent against the virus, has moved through clinical trials and is close to FDA approval. TMC-120 is being studied for its use as a microbicide (an AIDS cream) and has passed initial safety tests, he said.

Research teams at the Center for Advanced Biotechnology and Medicine on Rutgers' Busch campus have studied reverse transcriptase as well as the DAPY compounds for more than a decade. Over the past year, Rutgers researcher Joseph Bauman created a detailed image of TMC-278 through crystallography, technology that reveals the atomic structures of compounds. He then interlocked TMC-278 with reverse transcriptase, an advance expected to lead to new drugs made from DAPY compounds.

"Any time that basic science can lead to new, ideal options for patients with dreadful disease, that's a triumph of enormous magnitude," said Eddy Arnold of Rutgers University, an AIDS expert who supervised Bauman and has long investigated the intricacies of reverse transcriptase.

Kitta MacPherson may be reached at

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Yes - this is Tibotec's new NNRTI. I just hope it's more robust than the others... about time we had a "second generation" of NNRTI drugs.


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