Agilect/Azilect has recently been approved in Europe as a new treatment for Parkinson’s disease.
Agilect helps to prevent the breakdown of dopamine, the neurotransmitter most affected in Parkinson’s disease. It achieves this by inhibiting an enzyme called monoamine oxidase B, (or MAO-B). The only other drug known to be as specific as this specific is Deprenyl (Selegiline), however Agilect is believed to be 5 to 10 times more potent.
Also, unlike Deprenyl (for which a tiny amount is converted into the by-product of amphetamine), Agilect is bio-transformed to aminoindan, a non-amphetamine compound. Aminoindan, by-itself appears to have some neuroprotective qualities.
Agilect is likely to also act beneficially through its ability to act as an anti-oxidant and an anti-apoptotic agent.
In clinical trials, Agilect has been found to be effective as a monotherapy (i.e. taken on its own), or when taken together with Levodopa (Sinemet), for both early and late stage Parkinson’s disease.
Agilect has shown itself to have no more side effects than those taking placebo and there has been no sign of any of the so-called “cheese” effects; a condition which reacts with tyrosine-containing foods such as dairy produce. In one trial of 404 subjects treated with 1 mg. or 2 mg. of Agilect daily for 1-year, showed less functional decline than those given placebo. Another 26-week double-blind study concluded that Agilect was effective at 1 mg. or 2 mg. daily for early Parkinson symptoms.
Agilect is also believed to offer protection against dementias, through its MAO-B inhibiting activity, anti-oxidant and anti-apoptotic properties, as well as its propargylamine moiety. This protects mitochondrial viability, activating Bc1-2 genes and down regulating the Bax family of proteins. This is turn processes amyloid precursors protein (which would otherwise lead to the formation of plagues) and increases nerve growth factor. Because of these reasons, Agilect is now also in clinical trials to study its efficacy in Alzheimer’s disease.
Further clinical trials on Agilect
New data presented in an oral presentation session, at the 9th congress of the European Federation of Neurological Societies, showed that treatment with Agilect (Rasagiline 1 mg) once daily can provide significant additional benefits to levodopa treated patients with moderate to advanced Parkinson's disease (PD). These benefits were seen regardless of whether patients were receiving additional, optimized treatment with a dopamine agonist.
The new sub-analysis of the LARGO trial (Lasting effect in Adjunct therapy with Rasagiline Given Once daily), found that giving Agilect to patients already optimized on levodopa, with or without concomitant dopamine agonist (DA) treatment, significantly reduced daily “OFF” time (when the effects of medication wear off and PD symptoms return) by an average of 1.2 hours when compared to placebo, resulting in a clinically meaningful improvement in daily function for patients, without a related increase in dopaminergic adverse events. Patients experienced a corresponding increase in “ON” time (when medication is working) without troublesome dyskinesias, the involuntary movement’s characteristic of long-term PD therapy.
Principle investigator, Professor Olivier Rascol, of University Hospital Toulouse, France, commented: “This data shows that people with Parkinson's disease can achieve additional symptom benefits with Agilect, even when already receiving optimized levodopa treatment and irrespective of whether they are also receiving a dopamine agonist.”
The significant improvements in functioning demonstrated by Agilect, on top of DA treatment, were also shown with all additional end points, such as Clinical Global Impressions measures during “ON” time, UPDRS-motor during "ON" time (symptoms of tremor, slowness of movement, stability and rigidity), and UPDRS-Activities of Daily Living scores during “OFF” time, (measuring the ability of patients to walk, speak, swallow, dress and get out of bed.)
The active comparator in the study, entacapone, demonstrated comparable reductions in daily "OFF" time, but results for some of the additional measures mentioned above did not achieve significance.
The LARGO study investigated the response to treatment in 687 levodopa treated patients who were randomized to receive Agilect, entacapone or placebo. Two thirds of patients in each arm were also receiving DA therapy, allowing for comparison of the effectiveness of Agilect given alone or on top of a dopamine agonist.
This data from the LARGO study adds to the growing body of evidence for Agilect as an effective and well-tolerated treatment for Parkinson's disease. The findings from LARGO are consistent with the recently published study PRESTO, which also demonstrated that once daily Agilect, as an adjunctive therapy, significantly increases daily “ON” time and improves the cardinal symptoms of Parkinson's disease.
In addition, data from the TEMPO trial, a study of Agilect as monotherapy, demonstrated that Agilect is an effective and well-tolerated treatment in early disease and can significantly delay the progression of PD symptoms.
Agilect is a novel, potent, second-generation, selective, irreversible monoamine oxidase type-B (MAO-B) inhibitor that blocks the breakdown of dopamine, a neurotransmitter that is critical for the regulation and coordination of movement.
Parkinson's Disease
Parkinson's disease is a progressive neurodegenerative, chronic disruption of the central nervous system. Symptoms include tremor, slowness of movement, stiffness, gait and posture problems.
As the disease progresses, symptoms worsen and the patient is likely to experience motor complications, including a fluctuating response to treatment. During “ON” states, medication works effectively, but during “OFF” states, which correspond to the medication wearing off between doses, patients experience relatively poor function and mobility.
Parkinson's disease affects men and women equally, and an estimated four million people worldwide are affected by the disease, which typically occurs at a late age. Approximately 1.6% of the population over the age of 65 suffer from Parkinson's disease. It is estimated that well over one million people in the EU suffer from Parkinson's disease. In 2003, the worldwide market for Parkinson's disease drugs was valued at USD 2.5 billion with approximately 40% of this in Europe.
Dopaminergic adverse events are often seen with levodopa and dopamine agonist treatment and include sudden daytime sleepiness, hypotension, vomiting, diarrhoea, constipation and hallucinations.
LARGO: The LARGO trial was published in March 2005 in The Lancet. Findings showed that additional Agilect treatment significantly improves Parkinson's disease symptoms when compared with placebo in patients optimised on levodopa and concomitant Parkinson's disease medications. Agilect also demonstrated significant improvement compared to entacapone in gait, postural instability and “freezing” (when walking) - symptoms that are generally considered poorly responsive to levodopa therapy.
Global scales used to measure Parkinson's disease symptoms include:
UPDRS - The Unified Parkinson's Disease Rating Scale, a research tool commonly used to measure a patient's ability to perform mental and motor tasks and activities of daily life
CGI - the Clinical Global Impressions scale, a global measure of function improvement.
Dosage: Typically dosages for dementia are 1 mg. daily, maximum 2 mg. daily, although persons using it for preventative measures may want to consider 0.25 mg. to 0.5 mg. (dependant upon need). It is known that at dosages greater than 2 mg. daily Agilect can also become a MAO-A inhibitor and therefore will interfere more readily with other drugs such as SSRI anti-depressants etc. Unless under the guidance of a health professional, the concurrent use of any other MAO inhibiting products, such as Deprenyl, Gerovital, St. John’s Wort, as well as other anti-depressants, particularly SSRI’s such as Paxil and Prozac etc., should be avoided.
Safety: The effect of a long-term regimen of Agilect on human lifespan is unknown, yet since Deprenyl has increased both life-expectancy and maximum lifespan in animal studies, it is possible, and that Agilect’s metabolic profile may have similar advantages for antiaging. For those with Parkinson’s disease, particularly who are undergoing a multi-approach therapy, Agilect may well be the drug of choice.
Persons taking prescription medication and pregnant or lactating women should consult a physician before using this product. Long-term use of this product should be supervised and monitored by a health care professional.
Disclaimer: This product and its statements have not been evaluated by the FDA. This product is not intended to treat, cure or prevent any disease. The above information is provided under the supplying company's terms and conditions and should not replace the advice of your personal physician.
Restrictions: This product is not available for shipment to the EU
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