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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 Parkinsonís disease, restless leg syndrome, and Alzheimerís disease. A phase III clinical trial is on-going in Europe using calcium channel blockers as a treatment for Parkinsonís 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.

  • 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 Ė Safinamide for Parkinsonís

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 Parkinsonís 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 Parkinsonís Disease Rating Scale (UPDRS).

In phase II trials in patients with Parkinsonís 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 Ė 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 Alzheimerís

MEM 1003 is an L-Type Calcium Channel Modulator Ė a new-generation drug candidate to treat Alzheimerís 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 Parkinsonís 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

 

Copyright© 2012 Pipeline Project

All rights reserved. Revised: 01/26/12.