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Hi All, The current thread on rasagiline (and confusion with selegeline) begs the question..... What is Rasagiline Mesylate? And... is it FDA approved yet?? Rasagiline is a MAO type B inhibitor and is "similar" to the drug selegiline (Eldepryl®) in that respect. Rasagiline is a selective MAO-B inhibitor that is expected to have a favourable effect in Parkinson's patients in the early stages of the disease. http://www.lundbeck.com/IR/Pipeline/pipeline_info/rasagiline.htm Rasagiline Mesylate is a MAO-B Inhibitor developed by Teva Pharmaceutical Industries Limited. Teva Pharmaceutical Industries Limited P.O. Box 1142 Petach Tikva, Jersusalem 91010 Israel Phone: 972-2-589-2840 or 003-926-7267 Fax: 972-2-589-2839 E-Mail: [log in to unmask] TEVA Pharmaceuticals USA 650 Cathill Road P.O. Box 904 Sellersville, Pennsylvania 18960 U.S.A. Phone: n/a Fax: 215-721-9669 Ownership: Public Symbol: TEVA (NASDAQ) Parkinson's Disease (PD) Rasagiline mesylate (TVP-1012) Rasagiline mesylate is a novel, selective and potent irreversible monoamine oxidase type B (MAO-B) inhibitor for the treatment of PD patients (both as monotherapy and adjunctive therapy to levodopa). Teva has completed two successful double-blind phase II studies in the United States, Israel and Hungary. A pivotal double-blind, placebo-controlled study in 404 de novo Parkinsonian patients in the U.S. and Canada was completed. Rasagiline at dosages of 1 mg/day and 2 mg/day produced beneficial antiparkinsonian effects as monotherapy in these patients. Pivotal studies with rasagiline as adjunctive therapy to levodopa started in 2000 in North-America and in Europe. Unlike deprenyl, an established drug for PD with a similar mechanism of action, rasagiline is not metabolized to amphetamine derivatives. Its main metabolite, aminoindane, improves motor and cognitive functions in experimental models, and may thus contribute to the overall beneficial pharmacological profile of the drug. The drug is administered orally, once daily and does not require any titration. Rasagiline has demonstrated neuroprotective activity in various in vitro and in vivo pre-clinical models. Furthermore, it has shown activity in pre- clinical in-vivo models relevant for depression, stroke, head trauma, hyperactivity syndrome, amyotrophic lateral sclerosis and other neurological diseases. Teva has acquired the exclusive license to all intellectual property related to rasagiline from the Technion Research and Development Foundation Ltd., Haifa, Israel. The drug has a strong worldwide patent protection through 2014. Teva signed an agreement for the joint development and marketing of rasagiline for PD with the Danish pharmaceutical Company, H. Lundbeck A/S at the end of 1999. http://www.tevapharm.com/fs_gen.asp?sector=research_development_p Protection of neurons in ageing and neurodegenerative disorders by rasagiline (-)Deprenyl is a potent inhibitor of type B monoamine oxidase and, independent of this, is also known to protect or rescue dying neurons. Maruyama and colleagues examined the anti-apoptotic effects of rasagiline, which is a propargylamine structurally related to (-)deprenyl. Using human dopaminergic neuroblastoma SH-SY5Y cells, in vitro, rasagiline was found to protect dopamine cells from apoptosis induced by oxidative stress or neurotoxins. Furthermore, rasagiline prevented the disruption of mitochondrial membrane potential, the initial step to apoptosis. In addition, following long-term administration to rodents, rasagiline has been observed to increase the activities of anti-oxidative enzymes, superoxide dismutase and catalase. The results of this study suggest that rasagiline may interact with a specific molecule in the mitochondria and suppress signal transduction death. By its anti-apoptotic function, rasagiline may rescue or protect declining neurons in ageing and neurodegenerative disorders, such as Parkinson's disease. http://www.parkinsonsdisease.com/NEWS/NEWS101.HTM This from Pharma Licencing - 11 Nov 1999 Rasagiline - is currently in phase III clinical trials. Rasagiline is a potent, irreversible and selective inhibitor of the enzyme, monoamine oxide type B (MAO-B) that contributes to the breakdown of dopamine. Rasagiline has shown encouraging effects in phase II clinical trials in Parkinson's Disease (both as mono and adjunct therapy). http://www.pharmalicensing.com/news/adisp/942268680_3829e108e7c92 Successful Completion of a Phase III Trial - Israel, April 7, 2000 http://www.tevapharm.com/pr/2000/pr_236.html Clinical Trials in Parkinson's Disease - UAMS - Feb. 2001 Rasagiline in Levodopa treated Parkinson’s Disease Patients with Motor Fluctuations Phase III, multicenter, double-blind, randomized, placebo-controlled At least 2.5 hours "off" (when medications are not effective) state per day No Selegiline (EldeprylÒ) within the last 90 days In connection with PSG (Parkinson Study Group) Recruiting patients now! http://www.uams.edu/movementdisorders/Clinicaltrials.htm Sooo... What is a MAO-B Inhibitor?? Monoamine oxidase: from genes to behavior http://www.biopsychiatry.com/mao.html On the functions of monoamine oxidase, the emotions, and adaptation to stress http://www.biopsychiatry.com/mao.htm Inhibitory monoamine oxidases of the new generation http://www.biopsychiatry.com/rimah.html Metabolism of monoamine oxidase inhibitors http://www.biopsychiatry.com/maoi.htm Irreversible monoamine oxidase inhibitors.... from Psycho Babble http://www.dr-bob.org/babble/19991108/msgs/14781.html Selegiline (Eldepryl®): FDA approved; yet did not slow disease progression in an 800 subject study called DATATOP, but did improve PD symptoms Rasagiline: Under investigation for its protective and symptomatic benefit http://www.clinical-services.med.umn.edu/movement-disorders/tuite- talk.htm Effects of N-propargyl-1-(R)aminoindan (rasagiline) in models of motor and cognition disorders http://www.biopsychiatry.com/rasagiline.htm Selegiline, also known as l-deprenyl, is an irreversible and (relatively) selective MAO-B inhibitor. http://www.selegiline.com/ Effect of low-dose treatment with selegiline on dopamine transporter (DAT) expression and amphetamine-induced dopamine release in vivo http://www.selegiline.com/doptran.html Increased survival of dopaminergic neurons by rasagiline, a monoamine oxidase B inhibitor http://www.biopsychiatry.com/rasag.htm This mini study has helped me understand a little better.... how 'bout yoo? Cheers ..... murray [log in to unmask] ---------------------------------------------------------------------- To sign-off Parkinsn send a message to: mailto:[log in to unmask] In the body of the message put: signoff parkinsn