The active ingredient aleplasinin is currently being used to develop a drug that will be used in the therapy of Alzheimer’s disease patients. The drug is intended to prevent the formation of deposits that cause brain cells to die, thereby worsening the disease.
What is aleplasinin?
The active ingredient aleplasinin is currently being developed into a drug that will be used in the treatment of Alzheimer’s disease patients. Aleplasinin is a selective inhibitor designed to act on the plasminogen activator inhibitor PAI-1. These are proteins found in the blood that play an important role in blood clotting. The inhibitor PAI-1 has the task of breaking down the fibrin polymers that act as a kind of glue in blood clotting, so that they can be broken down in the organism. In rare cases, PAI-1 deficiency can occur within the human body if there is a mutation in the SERPINE1 gene. The drug PAZ-417 is currently being developed from this active ingredient by the US pharmaceutical company Wyeth. This company also has a site in Germany, where medical research is a significant focus. Once the drug is tested and approved for commercial use, it will be used in the therapy of Alzheimer’s disease.
Pharmacological action
In patients suffering from Alzheimer’s disease, so-called senile plaques accumulate on neurons in the gray matter of the brain. These plaques are misfolded amino acids and protein structures that accumulate in neurons. These accumulations ultimately lead to the death of the affected neurons. These are primarily the peptides beta-amyloid, which are continuously produced in a healthy organism but are not usually deposited. Recent research has shown that these peptides play a key role in the processing of information in the brain. Normally, the beta-amyloid peptide activates plasminogen activator, which in turn activates other enzymes that eventually degrade the beta-amyloid peptide. In patients suffering from Alzheimer’s disease, this mechanism is massively destroyed. Aleplasinin corrects this dysfunction insofar as PAI-1 is inhibited and increased degradation of the beta-amyloid peptide can occur. Because this prevents the peptides from being deposited in the gray matter of the brain, neuronal cell death in the affected regions is prevented.
Medical application and use
The active ingredient aleplasinin is thought to act in the therapy of Alzheimer’s disease. This disease belongs to the group of neurodegenerative diseases that occurs mainly in patients who have passed the age of 65. Alzheimer’s disease is considered to be the cause of about 60 percent of all dementias, affecting about 24 million people worldwide. Alzheimer’s disease is called primary dementia because the cause of the disease is a change in the structure of the brain. In secondary dementias, the disease has other causes such as deficiency symptoms, poisoning or injuries. While secondary dementias can be at least partially cured, Alzheimer’s dementia is not considered reversible. The typical characteristic of Alzheimer’s disease is a clear and growing deterioration of cognitive abilities. In addition, those affected often no longer manage to cope with their daily lives. The plaques that are to be eliminated by aleplasinin often form years before the first symptoms of Alzheimer’s disease become visible. Because treatment becomes more difficult the more advanced the Alzheimer’s disease, the U.S. National Institute on Aging has defined seven warning signs that may indicate the presence of the disease, which those affected or their immediate environment should seek medical attention for. The following warning signs indicate a possible disease: The affected person constantly repeats the same question or tells the same story over and over again. The affected person can no longer do everyday tasks such as cooking or operating appliances and can no longer handle money safely. The affected person can no longer find numerous objects or puts them in unusual places, whereupon he or she suspects other people of having taken the object away. The exterior is neglected, but the affected person denies this.And, sufferers respond to questions by repeating the question.
Risks and side effects
Because the drug is still in the development phase, no side effects are yet known.
