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Dr. Bob is Robert Hsiung, MD,
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Posted by ed_uk on January 2, 2006, at 5:11:28
I POSTED THIS ABOVE BUT I WANTED TO RE-POST IT BECAUSE THE ORIGINAL THREAD GOT SIDE-TRACKED. I HOPE YOU DON'T MIND DR. BOB. I THOUGHT PEOPLE MIGHT BE INTERESTED IN LADOSTIGIL.
Hi all,
OK, I've just consumed (more than) a few units of alcohol so this might not be as coherent and it could have been. Anyway, I'm sure you'll let me off given the circumstances :-)
LADOSTIGIL is a *very* interesting drug. It's currently in phase II trials for Alzheimer's disease. It was created by 'blending' the molecular characteristics of rivastigmine (Exelon) with those of rasagiline (Azilect). Rivastigmine (Exelon) is a cholinesterase inhibitor which is used to treat Alzheimer's disease. Rasagiline is an MAO-B inhibitor which is used to treat Parkinson's disease. Rasagiline was recently approved in Europe. It is believed to be neuroprotective as well as offering symptomatic relief.
The result, ladostigil, is a 'brain selective' MAOI and cholinesterase inhibitor. At therapeutic doses, it inhibits both MAO-A and MAO-B in the brain. Inhibition of both forms of MAO is probably necessary to gain a 'robust' antidepressant effect. Ladostigil is particularly interesting because of its alleged 'brain selectivity'. Unlike the classical MAOIs ie. Nardil and Parnate, ladostigil has relatively little effect on the MAO enzymes in the liver and gut. As a result, the risk of a tyramine-induced hypertensive crisis should be much reduced. Although ladostigil *does* potentiate the pressor effect of tyramine, the effect it minimal and no greater than that observed with moclobemide (Manerix/Aurorix). A strict low-tyramine diet is not necessary with moclobemide.
As well as inhibiting MAO-A and MAO-B, ladostigil is a cholinesterase inhibitor (think Aricept). Cholinesterase inhibitors are used in the treatment of Alzheimer's disease to enhance cognition and memory. Unfortunately, they do at times aggravate depression. Ladostigil is not expected to aggravate depression. Even so, if ladostigil was being used 'off label' as an antidepressant, as opposed to a treatment for Alzheimer's disease, it might be necessary (in some cases) to combine it with an anticholinergic - to offset the effects of potentially excessive synaptic levels of acetylcholine. There are many anticholinergics to choose from eg. Cogentin, Artane, Akineton, Kemadrin etc.
Ed
Posted by ed_uk on January 2, 2006, at 6:24:20
In reply to A new MAOI, posted by ed_uk on January 2, 2006, at 5:11:28
Ladostigil is currently in phase II clinical trials for Alzheimer's disease. Of interest to us, ladostigil might in future be prescribed 'off label' in the treatment of depression, anxiety and cognitive disorders.
From the TEVA website......
'Ladostigil Tartrate (TV-3326) for Alzheimer's Disease
Ladostigil tartrate (TV-3326) is a novel compound developed for the treatment of Alzheimer's disease (AD) and other forms of dementia. It combines in one molecule three mechanisms of action: MAO-inhibition, cholinesterase inhibition and neuroprotective activity. The combination of these three activities in a single entity gives the molecule a unique profile: It targets both the cognitive impairment and the problematic behavioral disturbances, such as depression and anxiety, prevalent in AD, and also potentially modifies the course of the disease via its neuroprotective mechanism. The development of ladostigil tartrate is based on original research done in the Technion & the Hebrew University, in Israel.
Teva has acquired the exclusive world-wide license to all intellectual property related to.
The product Phase I studies with ladostigil have been completed and a phase IIa study has been recently initiated in Europe.'Ed
Posted by tepiaca on January 3, 2006, at 0:47:44
In reply to Development of ladostigil by Teva, posted by ed_uk on January 2, 2006, at 6:24:20
Hi eddy
If is in Phase 2 , when it is suposed to be on
the market?
I have no idea how much time last the trialsTep
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