治疗中风的新药对实验鼠有效
http://www.100md.com
2001年4月3日
NEW YORK (Reuters Health) - A brand-new drug compound nearing final testing in humans helped prevent tissue damage from stroke in animals, researchers at Bristol-Myers Squibb report in preclinical findings published in the journal Nature Medicine.
``On average, we see a 20% to 30% reduction in the volume of tissue destroyed when the drug is given 1 to 2 hours after stroke,'' lead author Dr. Valentin K. Gribkoff told Reuters Health. ``It bolstered our confidence this drug has a chance to impact stroke within a time that is realistic.''
, 百拇医药
Gribkoff is a senior principal scientist of neuroscience drug discovery for the Bristol-Myers Squibb Pharmaceutical Research Institute in Wallingford, Connecticut.
The company is currently investigating the new compound, known as MaxiPost, which is designed to block further damage of nerve cells in stroke-affected areas. Damage to these cells can result in brain damage and the loss of the ability to move certain parts of the body.
, 百拇医药
Researchers believe the drug prevents a cascade of events that occur when blood is blocked from reaching the brain by a blood clot or narrowed artery, causing what is known as acute ischemic stroke.
The blockage of blood deprives cells of oxygen, setting off a chain of events, which eventually results in an excess of calcium released around the neurons. If too much calcium enters the brain cells, the cells can self-destruct.
MaxiPost attacks one aspect of that process. Known as a ''maxi-K'' potassium channel opener, it opens potassium channels in the cell wall and pumps potassium out of the cell, which prevents calcium from flooding the cells.
, 百拇医药
``Neuroprotective drugs hope to intervene and keep those cells viable,'' Gribkoff said. ``It gives them a chance to recover from the insult.''
In this first study to publish full results on the new drug, scientists induced blockage of the cerebral artery in rats, then administered the drug intravenously 1 to 2 hours later. The drug was chosen, in part, because of its ability to easily reach and enter the brain.
Because the drug is highly site-specific, it has caused no documented adverse side effects on blood pressure, heart rate or cerebral blood flow in either animals or humans, Gribkoff noted.
, http://www.100md.com
Bristol-Myers is currently conducting the second of two Phase III clinical trials looking at the drug's effect on around 3,000 stroke victims, Gribkoff explained. The first Phase III study in humans reportedly showed no significant result.
``We'll have to wait and see what the data are in humans,'' Gribkoff said. ``We think the hypothesis is valid, not only of this compound, but of the idea of neuroprotective intervention in stroke, but we just don't know at this point.''
, 百拇医药
If the drug were to be proved effective and eventually approved for use, it would be only the second form of treatment available for the thousands of people affected annually by ischemic stroke in the United States, Gribkoff said. ``It's a hugely unmet medical need worldwide,'' Gribkoff said.
But Dr. Mark J. Alberts, professor of neurology and head of the stroke program at Northwestern University Medical School in Chicago, Illinois, said that dozens of promising neuroprotective drugs have worked in animal studies but then failed to be proven safe and effective in humans. ``It's one of the big conundrums in stroke research,'' he said.
SOURCE: Nature Medicine 2001;7:471-477., 百拇医药
``On average, we see a 20% to 30% reduction in the volume of tissue destroyed when the drug is given 1 to 2 hours after stroke,'' lead author Dr. Valentin K. Gribkoff told Reuters Health. ``It bolstered our confidence this drug has a chance to impact stroke within a time that is realistic.''
, 百拇医药
Gribkoff is a senior principal scientist of neuroscience drug discovery for the Bristol-Myers Squibb Pharmaceutical Research Institute in Wallingford, Connecticut.
The company is currently investigating the new compound, known as MaxiPost, which is designed to block further damage of nerve cells in stroke-affected areas. Damage to these cells can result in brain damage and the loss of the ability to move certain parts of the body.
, 百拇医药
Researchers believe the drug prevents a cascade of events that occur when blood is blocked from reaching the brain by a blood clot or narrowed artery, causing what is known as acute ischemic stroke.
The blockage of blood deprives cells of oxygen, setting off a chain of events, which eventually results in an excess of calcium released around the neurons. If too much calcium enters the brain cells, the cells can self-destruct.
MaxiPost attacks one aspect of that process. Known as a ''maxi-K'' potassium channel opener, it opens potassium channels in the cell wall and pumps potassium out of the cell, which prevents calcium from flooding the cells.
, 百拇医药
``Neuroprotective drugs hope to intervene and keep those cells viable,'' Gribkoff said. ``It gives them a chance to recover from the insult.''
In this first study to publish full results on the new drug, scientists induced blockage of the cerebral artery in rats, then administered the drug intravenously 1 to 2 hours later. The drug was chosen, in part, because of its ability to easily reach and enter the brain.
Because the drug is highly site-specific, it has caused no documented adverse side effects on blood pressure, heart rate or cerebral blood flow in either animals or humans, Gribkoff noted.
, http://www.100md.com
Bristol-Myers is currently conducting the second of two Phase III clinical trials looking at the drug's effect on around 3,000 stroke victims, Gribkoff explained. The first Phase III study in humans reportedly showed no significant result.
``We'll have to wait and see what the data are in humans,'' Gribkoff said. ``We think the hypothesis is valid, not only of this compound, but of the idea of neuroprotective intervention in stroke, but we just don't know at this point.''
, 百拇医药
If the drug were to be proved effective and eventually approved for use, it would be only the second form of treatment available for the thousands of people affected annually by ischemic stroke in the United States, Gribkoff said. ``It's a hugely unmet medical need worldwide,'' Gribkoff said.
But Dr. Mark J. Alberts, professor of neurology and head of the stroke program at Northwestern University Medical School in Chicago, Illinois, said that dozens of promising neuroprotective drugs have worked in animal studies but then failed to be proven safe and effective in humans. ``It's one of the big conundrums in stroke research,'' he said.
SOURCE: Nature Medicine 2001;7:471-477., 百拇医药