אקסלון: התרופה שנלחמת באלצהיימר
המוצר: תרופה לטיפול בחולי אלצהיימר
המפתחת: פרופ' מרטה וינשטוק-רוזין החברה: נוברטיס
תחילת הפיתוח: 1981
Product: A Drug for Treating Alzheimer’s Patients
Developer: Prof. Marta Weinstock-Rosin Company: Novartis
Start of Development: 1981
In 1984, Prof. Marta Weinstock Rosin was working as a researcher in the School of Pharmacy at the Hebrew University, when her mother-in-law was diagnosed with Alzheimer’s. Prof. Weinstock-Rosin witnessed first-hand the disease’s devastating influence on the patient and her family.
Alzheimer’s is a chronic progressive disease characterized by damage to short term memory and gradual loss of functional and cognitive ability. The disease is frequently accompanied by changes in behavior such as apathy or aggressiveness, anxiety, depression and paranoia. Today, 26 million people worldwide are diagnosed with Alzheimer’s.
Prof. Weinstock-Rosin’s personal encounter with the disease occurred during her research into the respiratory depression mechanism of morphine. She discovered that the mechanism is connected to the delayed release of a neurotransmitter in the brain stem called acetylcholine. It became evident that administration of a drug inhibiting the cholinesterase enzyme that prevents the breakup of acetylcholine, reduces the morphine’s depressive influence on respiration. The problem was that the drug was toxic and chemically unstable.
Following this discovery, Prof. Weinstock-Rosin attempted to develop safer and more stable cholinesterase inhibitors at the Hebrew University laboratories and this search gave birth to a new chemical named RA7.
Prof. Weinstock-Rosin then came across a finding that indicated an inverse correlation between the levels of acetylcholine in the cerebral cortex and hippocampus, and the degree of memory impairment in Alzheimer’s patients. The researcher understood that RA7 could provide a solution to memory impairment by prolonging the acetylcholine’s influence in these areas of the brain. The hypothesis was confirmed during trials that were the first step towards a revolutionary new treatment.
Prof. Weinstock-Rosin continued developing the RA7 until 1986, registering it as a patent. The university approached TEVA with the aim of completing the substance’s development as a pharmaceutical drug, however TEVA declined the offer and it was instead sold to the Swiss corporation Sandoz, later Novartis.
Development continued about a decade and in 1987 the drug was first marketed under the tradename Exelon. Trials and studies revealed that Exelon improves cognitive function and behavioral disturbances in nearly 30 percent of Alzheimer’s patients and slows deterioration in approximately 60 percent.
Annual sales of Exelon fluctuated between 500 million-1 billion dollars until the patent’s expiration in 2006.
In 2014, Prof. Weinstock-Rosin won the Israel Prize for medical research.