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CANCER: TURNING THE CORNER
Going after cancer's Achilles' heel

By Richard Saltus, Globe Staff, 08/03/98

They were hailed as biological ''guided missiles'' when they were developed in the 1970s, but monoclonal antibodies fell short of their targets in early tests against cancer and other illnesses.

 

In a remarkable turnaround, however, these biotech weapons are now leading the charge in the early testing of new, highly specific drugs that aim for the genetic Achilles' heels of cancer cells.

 

Already, one monoclonal antibody drug has been approved to treat an immune cancer, lymphoma, with fewer side effects than standard chemo agents. Another, Herceptin, is on a Food and Drug Administration ''fast track'' toward approval after showing encouraging results against metastatic breast cancer in cases where other therapies had failed.

 

Dr. Dennis Slamon, a University of California at Los Angeles scientist whose research led to the development of Herceptin, was in the spotlight at a major cancer meeting this spring.

 

''This is the first time when molecular biology has really paid off,'' he declared, ''where we've identified a genetic alteration, showed its role in a disease process, and then targeted it.''

 

Herceptin is a monoclonal antibody that recognizes and binds to a molecule found on the surface of about 30 percent of breast cancer cells. The molecule, known as the HER-2/neu receptor, acts as an on-off switch. When on, it makes breast cancer especially aggressive and fast-moving. Herceptin keeps the switch turned off.

 

Because the HER-2/neu protein isn't present on normal breast cells, Herceptin selectively attacks the cancer. Results announced in May showed that the drug, combined with the best standard chemotherapy agent, caused tumors to shrink by half or more in 49 percent of women, compared with 32 percent of those on the chemo alone.

 

A year later, 28 percent of women on Herceptin had no evidence of tumor progression, compared with 14 percent in the chemo-only group.

 

Because they're expensive and must be given by injection, monoclonals may not be the ultimate cancer drugs, but they're further along in development than most of the ''small molecule'' drugs that eventually may be more selective and easier to administer.

 

Antibodies are the proteins made by the body's immune system cells to recognize and attack specific foreign invaders, such as infectious germs. The body makes millions of antibodies, each of which has a specific shape to recognize and bind to a foreign molecule.

 

Twenty years ago, scientists discovered how to make large quantities of identical antibodies - hence ''monoclonal'' - in mice. There were high hopes that these would be ''magic bullets'' that could be tailored to identify and latch onto unique structures on cancer cells. The antibodies could then be loaded with toxins or radioactive substances that would destroy the cells.

 

Antibodies can be used against cancer in three ways, says Dr. Mark Kaminski, a researcher at the University of Michigan School of Medicine:

 

They can bind to cancer cells and alert the immune system to attack them.

 

They can latch onto cells and trigger a signal within each one that halts its growth or causes it to commit suicide. Or they can block growth signals from outside the cell and squelch growth that way.

 

They can serve as guided missiles, homing in on cancer cells after scientists attach a molecular warhead, in the form of toxins or drugs, that kills targeted cells.

 

Disappointing start>

 

for antibody approach

 

In spite of all that, antibody treatments were deeply disappointing for the first 10 years or so.

 

''They were the hot technology in the late '80s,'' says Donald Drakeman, president of Medarex, Inc., in New Jersey. ''It was an exciting opportunity, and like with all brand-new technologies, no one figured out the problems. By the early '90s antibodies became almost a dirty word.'"

 

The main problem was that patients' immune systems recognized the proteins from the mice used to make the monoclonals as foreign and attacked them. The drugs were destroyed before they could reach their targets.

 

As researchers learned to ''humanize'' the antibodies by replacing most of the mouse components with human ones, their effectiveness rose.

 

Over the last 10 years we learned more about how to use them and which [molecules] are especially good targets,'' says Drakeman.

 

And now the new drug Herceptin, made by Genentech, Inc., of South San Francisco, has put monoclonal antibodies back in the spotlight with its ability to fight breast cancer. Genentech says it expects FDA approval by the fall and it will be able to supply what is expected to be a large market. (Some clinical trials of Herceptin are still open for women who meet the criteria.)

 

Edith Sooy is a Massachusetts woman who took Herceptin in the company's earlier trials and believes she is alive today because of it.

 

Sooy, 54, of Dover, was treated for breast cancer in 1987, but discovered in 1992 that it had spread to her lungs. The most potent standard drugs, like adriamycin and the relatively new agent, Taxol, failed to help. ''They're dreadful drugs'' because of their side effects, she says, ''and when they don't do anything for you, it's depressing.''

 

Because her tumor was among the 30 percent that carry the HER-2/neu genes, Sooy was able to enroll in a Herceptin study at Boston University Medical Center. In early 1996 she began taking the intravenous agent. Within a few months, her tumors had shrunk by 50 percent of more, and the toxicity was very mild. ''It's heaven - if it keeps your cancer in check,'' she says.

 

Unfortunately, the tumors grew back. Since then, she has been on a series of combinations of chemo drugs and Herceptin. Her disease has progressed, but slowly. ''I think I'm very lucky to be alive and well and doing my gardening. I have to think it has to be due in part to the Herceptin,'' she says.

 

Other monoclonal antibodies have shown effectiveness against non-Hodgkin's lymphoma, an immune-system cancer. In addition to the already approved Rituxan, an experimental monoclonal antibody called Bexxar is undergoing testing at the University of Michigan, where Kaminski has reported a series of promising test results. All of the newly diagnosed patients with advanced low-grade non-Hodgkin's lymphoma have responded to the drug, and 17 of 24 patients followed for at least six months have had a complete remission, Kaminski reported.

 

A trial is now in progress to see whether patients who relapsed after the first round of treatment will respond to a second dose of Bexxar. Thus far, says Kaminski, ''we've gotten the majority of patients back into remission.''

 

That's a huge selling point for patients who have volunteered for trials. ''What you go through in this treatment is so much less [traumatic] than chemotherapy, so if you had to do it again, it wouldn't take as much out of you,'' says Teresa Singh, 39, who chose treatment with Bexxar after being diagnosed in 1996 with lymphoma

 

She was told that with conventional chemotherapy she might be put into remission - free of disease as far as standard tests show - but that she would likely relapse. One expert told her she might live 6 to 9 years after diagnosis; another put it at 10 to 15 years.

 

''I have [plans for] a lot longer than that to live,'' she says.

 

Bexxar seeks out a target protein, called cd20, on the surface of the affected blood cells. To the antibody is attached radioactive iodine, which at close range can kill those cells

 

Singh received the treatment in a special hospital room in which she was shielded by lead slabs and had to take precautions to avoid contaminating others. ''I had to flush the toilet three times'' to ensure that contaminated urine was completely disposed of, she said.

 

Singh and other patients have been astonished to find their swollen lymph glands and other sites of cancer shrink quickly - sometimes within a week or two - after the radioactive assault.

 

''I think oncologists don't raise their hopes too easily,'' says Singh, ''and Dr. Kaminski is still very conservative in the way he talks about this. I can't say I never worry about it coming back, but I'm thankful I have this treatment that isn't grueling... and there is hope for a cure.''

 

 

This story ran on page C01 of the Boston Globe on 08/03/98.
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Copyright 1998 Globe Newspaper Company