- EMA-approved medicine for excessive daytime sleepiness med Ozawade (Pitolisant)
- Pitolisant was developed after decades of research by Bioprojet co-founders Dr. Jeanne-Marie Lecomte and Prof. Jean-Charles Schwartz
The European Medicines Agency (EMA) has approved Bioprojet’s Ozawade (Pitolisant) for the treatment of excessive daytime sleepiness (EDS) associated with obstructive sleep apnoea (OSA) in adults.
Ozawade was evaluated in two Phase III clinical studies in the treatment of EDS in patients suffering from OSA – HAROSA I and HAROSA II. The two studies showed a ‘significant improvement’ in the Epwoth Sleepiness Scale score (ESS) in patients treated with Ozawade, with no notable cardiovascular incidents or significant change in blood pressure/heart rate observed.
Following the EMA approval, Ozawade is indicated to improve wakefulness and reduce EDS in adult patients suffering from OSA, whose EDS has not been treated successfully by a primary treatment for the condition – including continuous positive pressure (CPP) – or for those who do not tolerate CPP.
“With fatigue, excessive daytime sleepiness is the symptom most frequently reported by patients, with a considerable impact on quality of life and on daily safety,” said Jean-Charles Schwartz, scientific director and co-founder of Bioprojet.
“Ozawade provides an effective solution to all patients, whether they are treated by PPC or intolerant of this treatment.”
“The HAROSA I and II studies in particular demonstrated that taking pitolisant had no impact on systolic or diastolic blood pressure and did not increase the risk of hypertension. In fact, the mode of action for Ozawade is distinct from that of psychostimulants which gives it a favourable safety profile, which is essential for a population which often has metabolic and cardiovascular co-morbidities,” he added.
What is Ozawade (pitolisant)?
Pitolisant is a medication for the treatment of excessive daytime sleepiness in adults with narcolepsy. It is a histamine 3 (H3) receptor antagonist/inverse agonist. It represents the first commercially available medication in its class. Pitolisant enhances the activity of histaminergic neurons in the brain that function to improve a person’s wakefulness.
Ozawade is a medicine used to improve wakefulness and reduce excessive daytime sleepiness in adults with obstructive sleep apnoea.
What is Excessive daytime sleepiness?
Excessive daytime sleepiness is one of the most common sleep-related patient symptoms, and it affects an estimated 20 percent of the population. Persons with excessive daytime sleepiness are at risk of motor vehicle and work-related incidents, and have poorer health than comparable adults. The most common causes of excessive daytime sleepiness are sleep deprivation, obstructive sleep apnea, and sedating medications. Other potential causes of excessive daytime sleepiness include certain medical and psychiatric conditions and sleep disorders, such as narcolepsy. Obstructive sleep apnea is a particularly significant cause of excessive daytime sleepiness. An estimated 26 to 32 percent of adults are at risk of or have obstructive sleep apnea, and the prevalence is expected to increase. The evaluation and management of excessive daytime sleepiness is based on the identification and treatment of underlying conditions (particularly obstructive sleep apnea), and the appropriate use of activating medications.
Obstructive sleep apnoea:
Obstructive sleep apnoea is the repeated interruption of breathing during sleep due to airways becoming blocked. Ozawade is used when other treatments, such as continuous positive airway pressure (CPAP, use of a ventilator to keep the airways open) have not satisfactorily improved excessive daytime sleepiness or cannot be tolerated by the patient.
Pitolisant (Wakix) is used in adults for the treatment of excessive daytime sleepiness. Narcolepsy is a sleep problem that is characterized by an irresistible urge to sleep and disturbed nighttime sleep, while cataplexy refers to attacks of severe muscle weakness that cause a person to collapse. Pitolisant (Ozawade) is indicated to improve wakefulness and reduce excessive daytime sleepiness in adults with obstructive sleep apnea.
The most common side effects include insomnia (difficulty sleeping), headache, nausea (feeling sick), anxiety, irritability, dizziness, depression, tremor, sleep disorders, tiredness, vomiting, vertigo (a spinning sensation) and dyspepsia (heartburn).Serious but rare side effects are abnormal loss of weight and spontaneous abortion.
Mechanism of Action (MOA):
The active substance in Ozawade, pitolisant, works by attaching to receptors (targets) in the brain called ‘histamine H3 receptors’. This increases the activity of certain brain cells called ‘histamine neurons’, which are important for keeping the body awake. Pitolisant also increases levels of the neurotransmitters acetylcholine, dopamine and noradrenaline in the brain. Neurotransmitters are chemical messengers that allow nerve cells to communicate with each other. Since these neurotransmitters are involved in maintaining alertness and arousal, increasing their levels may improve wakefulness.
When was Pitolisant approved by USFDA?
Pitolisant was approved by the U.S. Food and Drug Administration (FDA) in August 2019. It was granted orphan drug designation for the treatment of narcolepsy, fast track designation for the treatment of excessive daytime sleepiness and cataplexy in people with narcolepsy, and breakthrough therapy designation for the treatment of cataplexy in people with narcolepsy.
Bioprojet SCR is a research-based pharmaceutical company. Bioprojet is headquartered in Paris, France and its Research Center located in Rennes, France. Its activity is focused on the design, synthesis and development of novel classes of drugs for unmet medical needs.
The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of medicinal products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products or the European Medicines Evaluation Agency (EMEA).
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