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October 14, 2002
New Medications To Treat Memory Disorders By Ruth Winter, MS
A new type of medication to treat memory disorders, Parkinson's Disease, Schizophrenia and perhaps other such ills seems to be progressing well. Ampakines are organic chemical molecules that can be taken by mouth and which rapidly enter the brain.
The current medications, such as Aricept® to treat Alzheimer's and Mild Cognitive Impairment (MCI) help reduce the destruction of acetylcholine---a nerve messenger in the brain involved in memory. Ampakines stimulate nerve endings to enhance the transmission of nerve messages involved in memory and reportedly encourage the production of nerve growth factor (NGF) and neurotrophic factor (BDNF)---two proteins required for healthy nerve cells. These proteins may also play a critical role in treating Huntington's disease; Parkinson's Disease; patients recovering from stroke or brain trauma and may possibly be useful in treating schizophrenia. There are reportedly 250 active compounds in the Ampakine library. In animal studies, rats given Ampakines were found to enhanced learning through smell and improved short-term memory in age- associated memory loss.
Human trials are now underway with AMPAKINE CX516 under a collaboration between Cortex Pharmaceuticals of Irvine, CA., and Les Laboratoires Servier of Paris, France. Early reports look promising. In the first phase of human trials, CX516 was apparently well-tolerated with minimal toxicity and researchers noted enhanced learning and memory in small groups of healthy young and elderly adults. In phase two clinical trials, researchers are assessing CX516 for safety and efficacy in improving cognition in individuals diagnosed with Mild Cognitive Impairment (MCI). This is the first cross-national study of Amapakine compounds designed to show memory enhancement in patients with MCI. It involves 160 patients between the ages of 55 and 85 years. Enrollment in the study started during the first quarter of 2002 and it is anticipated that the preliminary evaluation will be completed during the second quarter of 2003.
Christine Gall, Ph.D., professor of anatomy and neurobiology at UCI, has conducted studies on rats and mice, including studies of Ampakines' effects on brain neurochemistry. She says it is quite likely current drugs now in use that reduce destruction of acetylcholine such as Aricept® and the Amapkines which increase transmission might be useful together since they target distinct aspects of the brain.
For those interested in clinical trials, check with National Institute of Neurological Disorders and Stroke (NINDS), 9000 Rockville Pike Bethesda, Maryland, 20892, United States; Recruiting Patient Recruitment and Public Liaison Office 1-800-411-1222 prpl@mail.cc.nih.gov TTY 1-866-411-1010
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A TROJAN HORSE NAMED "FOLATE "AGAINST CANCER
The Ancient Greeks fooled their enemies, the Trojans, by using a wooden horse outside the city with concealed soldiers in its belly. When the Trojans opened the city gates and dragged in the horse, the Greeks jumped out and killed the Trojans. Human trials will begin in November with folate acting as a "Trojan Horse.". Many types of cancer cells have a great affinity for folate -- a form of water-soluble B vitamin -- because they need the nutrient in order to grow and divide. In fact, cancer cells have evolved a mechanism to capture folate more effectively than normal cells. Making use of this selectivity, researchers have developed a way to trick cancer cells into attracting and even ingesting anticancer agents that are attached to folate molecules. As a result, these chemotherapeutic agents can be delivered more specifically to cancer cells while leaving the surrounding normal tissue unharmed.
Endocyte Inc. and Indiana's Purdue University researchers have developed a form of this "Trojan Horse" therapeutic approach (folate-targeted immunotherapy) that was used to successfully treat more than 200 mice with late-stage metastatic disease. The results of these studies were published in a recent issue of The Journal of Cancer Immunology and Immunotherapy.
"It's using cancer's nutritional needs against itself," said Philip Low, Purdue's Professor of Chemistry who led the research team that discovered this diagnostic and treatment method. "We are essentially slipping medicine in with cancer's favorite food."
The discovery has thus far yielded two different but complementary treatment methods that involve attaching various markers (folate-targeted immunotherapy) or anticancer agents (folate-targeted chemotherapy) to the vitamin. The treatment method that "marks" cancer will be tested in Phase I Food and Drug Administration-regulated human clinical trials beginning in November. The objective of this method is to force the body's immune system to fight the disease, said Christopher Leamon, Endocyte's vice president of research.
"There's no better drug than your own immune system, which consequently is capable of getting rid of every last bacterium, every last virus or every last fungus in the body. Today's drugs can't do that," Leamon said. "Unfortunately, many cancers develop ways to evade immune surveillance. But we've found a way to redirect a patient's immune system to kill those resistant cancer cells by using our folate-targeted approach."
Researchers have found that certain cancers -- among them ovarian cancer and renal cell carcinoma -- have high levels of folate receptors. These receptors are located on the surfaces of cancer cells and are responsible for binding folate in a very specific manner, similar to the way a key is inserted into a lock. Cancer cells that are receptive to folate often express more folate receptors in metastasized sites formed once the cancer becomes widely disseminated throughout the body.
Researchers hoped to bypass normal, healthy cells by delivering folate linked to an anticancer agent directly into the cancer. They discovered, however, that cancer cells don't take in all of the folate at once, but rather wear the excess folate on their cell surfaces, storing it for future use. Some of the drugs they attach to folate, consequently, also are stored on the cancer cell surfaces. .Founded in 1996, Endocyte is located in the Purdue Research Park. For more information, check: Endocyte: http://www.endocyte.com
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ARMING UNDERARM DEODORANTS
Americans have been made self-conscious about body odor and underarm deodorants are big business. Europeans and Asians are also being convinced that that really do need something to cover up or prevent underarm odor.
Most underarm deodorant products are designed to eliminate the perception of odor, but ability of the fragrance and the preference for a fragrance varies.
An antiperspirant, on the other hand ---or is it the other underarm---affects the biological activity of sweat production from the sweat glands. In some countries, antiperspirants are regulated as drugs. The US FDA has published a tentative final monograph outlining what is an acceptable antiperspirant, how it should be used and what tests must be performed to substantiate the claim.
Deodorant sticks, roll-ons, aerosols, and creams have been around for a long time. The newest method of is the "extrudable" with white creams or clear gels that extrude from holes. Towlettes introduced in Europe are now entering the United States, and are "sold" as instant fresheners. Japan and Europe are also testing a compact spray that is convenient to carry.
One of the most popular antimicrobials used in deodorants is triclosan. Other ingredient popular in Europe and starting to enter the US are acyclic sesquiterpene alcohols, ethyhexyl oxyglycerin, pentylene glycol, C12-13 alkyl lactate and a number of botanical extracts. Check A Consumer's Dictionary of Cosmetic Ingredients.
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