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

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