Calcium Channel Modulator
Summary:
Cells require certain levels of calcium to function properly. If calcium levels
are too high, cell death can result. Calcium channel modulators are able to
regulate intracellular calcium levels that are too high so they go back to
normal levels and restore proper cellular functioning. This modulation also
protects neurons from calcium overload.[1]
Calcium channel blockers have had positive results in clinical trials for
Parkinson’s disease, restless leg syndrome, and Alzheimer’s disease. A phase III
clinical trial is on-going in Europe using calcium channel blockers as a
treatment for Parkinson’s disease.
Potential benefits:
- Neurons remain more responsive to incoming signals.
-
Inhibits dopamine uptake.
-
Potential neuroprotective activity due to multiple mechanisms of action.
-
Reversible MAO-B inhibition leading to a favorable side effect profile.
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Absence of MAO-A activity in humans, therefore, no cheese effect.[2] (The
cheese effect is generally defined as hypertension during treatment with
MAO inhibitors or similar medications, usually caused by eating tyramine-rich
foods like aged cheese.)
Current
research:
Newron – Safinamide for Parkinson’s
Newron Phameceuticals has initiated an 18-month, double-blind,
placebo-controlled phase III clinical trial designed to compare two dose
ranges of safinamide versus placebo. In this multi-center, multi-national
study, people with early stage Parkinson’s disease will take safinamide as
add-on therapy to a stable dose of a single dopamine agonist. The primary
measure of effectiveness will be the number of patients who show improvement
as rated by the Unified Parkinson’s Disease Rating Scale (UPDRS).
In phase II trials in patients with Parkinson’s disease, safinamide was
co-administered with a dopamine agonist, and the result was a significant
reduction in UPDRS motor scores. So far safinamide has been found to be
safe.[3]
Newron – Safinamide for Restless Legs Syndrome
In a phase II, open label trial of safinamide, participants with
Restless Legs Syndrome (RLS) showed a significant improvement in all
measurable parameters studied. Additionally safinamide was found to be
well tolerated.[4]
Memory Pharmaceuticals - MEM 1003 for Alzheimer’s
MEM 1003 is an L-Type Calcium Channel Modulator – a new-generation drug
candidate to treat Alzheimer’s disease, and potentially mild cognitive
impairment and vascular dementia. The compound lowers intracellular
calcium, preventing the harmful consequences of excessive calcium
levels. A benefit of this ability to modulate calcium layers is that
neurons remain more responsive to incoming signals. This counteracts the
reduced activity that normally occurs during the aging process. This
drug candidate has completed Phase I clinical trials.[5]
[1]
Memory Pharmaceuticals Acquires Rights from Bayer to a Promising Drug
Candidate for Dementia; September 11, 2001
[2] Safinamide in Parkinson’s Disease; Date retrieved: March 13, 2005
[3]
Newron initiates Parkinson's disease Phase III trial with
Safinamide,
September 13, 2004
[4]
Newron Pharmaceuticals Successfully Completes Pilot Study of Safinamide
in Restless Legs Syndrome; Milan, Italy; January 11, 2005; Newron
Pharmaceuticals SpA
[5]
MEM 1003; Date retrieved: March 13, 2005
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