|Company Name:||J & K SCIENTIFIC LTD. |
|Product Categories:||Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitors|
|Pimavanserin Chemical Properties|
|Pimavanserin Usage And Synthesis|
|Parkinson's treatment||Pimavanserin is a kind of novel oral administrated drug for treatment of Parkinson’s psychosis developed by Acadia pharmaceutical Company (US) with the trade name being Pimavanserin. In September 3rd 2014, it has been granted by the US Food and Drug Administration (FDA) for breakthrough therapy certification. Breakthrough therapy certification is created by the FDA for accelerating the development and review of new drugs for treatment of serious or life-threatening diseases. |
Currently there are about seven millions to ten million of patients of Parkinson's disease worldwide with China contributing 2.6 million, ranking first in the world with 100,000 new patients emerging every year. More than 50% of patients of Parkinson's disease have had psychiatric symptoms (PDP). These psychiatric symptoms are mainly manifested as hallucinations and delusions, bringing greater challenge to the treatment and care for patients of Parkinson's disease. Dopamine is the primary target for the treatment of Parkinson's disease because most antipsychotics drugs will block the dopamine in the brain of the patients of Parkinson’s disease, making their situation of motor dysfunction be even worse, and thus currently not being suitable for these patients.
Parkinson's disease psychosis is the major reason why patients of Parkinson disease enter into the elderly-care apartment. There is currently no other drugs except low-dose clozapine (Clozaril) that have been approved for the treatment of Parkinson's disease psychosis. So once approved, the drug should be able to significantly improve the standard therapy. Clozapine has serious security risks that can lead to a dangerous decline in the number of white blood cells and also has another side effect of causing drowsiness.
Pimavanserin is a novel first-line drug of antipsychotic symptoms belongs to non-dopaminergic neurotransmitters with the drug targets being serotonin 2A receptor (5-HT2A), which can selectively block the 5 -HT 2A receptor without affecting the action of dopamine with the routine administration being treatment via oral administration once daily. There are evidences showing that the drug is quite effective in the treatment of Parkinson's disease psychosis with well tolerance. Moreover, it does not block the dopamine receptors, and therefore does not lead to worsening of symptoms of Parkinson's disease. A 6-week-lasting randomized, double-blind, placebo-controlled trial has included 199 patients and evaluated the safety and efficacy of pimavanserin.
Patients in the pimavanserin group, in the Parkinson's disease-adapted scale for assessment of positive symptoms (SAPS-PD) for evaluating the positive symptom, have their average scores drop by 5.79 points while the placebo group have the average score drop only by 2.73 points, the difference between these two groups was statistically significant (P = 0.001). In addition, pimavanserin group also have greater improvement in the Clinical Global Impression Scale and caregiver burden scale. Pimavanserin can be well tolerated and does not aggravate the symptoms of motion.
The secondary endpoints for the study is the exercise tolerance in patients, it is through the assessment of the second part and third part of the unified Parkinson's disease rating scale (UPDRS). From this perspective, pimavanserin treatment enables the patient to receive a significant therapeutic benefit. In the improvement aspect on the Clinical Global Impression Scale scores, patients in the group of the Clinical Global Impression Scale have been also significantly improved. In some exploratory detection indicators, patients in the pimavanserin treatment group had also obtained significant improvement such as night sleep time, wake time during the day, and the total cost of care and so on.
During the course of treatment, the most common adverse events are urinary tract infection (11.7% in the placebo group, 13.5% in the pimavanserin group) and falls (8.5% in the placebo group; 10.6% in the pimavanserin group), but the vast majority are mild to moderate adverse reactions. Moreover, for patients who have been subject to completion of all tests and treatment benefit, 90% are chosen to participate in the further pimavanserin extension study.
Figure 1 the chemical structure formula of Pimavanserin
The above information is edited by the Chemicalbook of Dai Xiongfeng.
|Uses||Drug used in the treatment of Parkinson disease psychosis.
|Chemical Properties||Yellow Solid|
|Usage||Drug used in the treatment of Parkinson’s disease psychosis.|
|Definition||ChEBI: A member of the class of ureas in which three of the four hydrogens are replaced by 4-fluorobenzyl, 1-methylpiperidin-4-yl, and 4-(isopropyloxy)benzyl groups. An atypical antipsychotic that is used (in the form of its tartrate salt) for treatment of halluc
nations and delusions associated with Parkinson's disease.|
|Pimavanserin Preparation Products And Raw materials|