Company Press Release
SOURCE: Vertex Pharmaceuticals Incorporated
Vertex Neurophilin Ligands Demonstrate Neuroprotective Effect in Models
of Parkinson's Disease
- Results suggest neurotrophic pathway independent of FKBP-12 -
VANCOUVER, BC, July 29, 1999 /PRNewswire/ -- Orally administered
neurophilin compounds discovered at Vertex Pharmaceuticals Incorporated
(Nasdaq: VRTX - news), including compounds that do not interact with
FKBP-12, significantly improve outcome in two different preclinical
models of Parkinson's disease, according to results presented this week
at the International Congress on Parkinson's Disease in Vancouver,
British Columbia. The results presented were from studies conducted in
the laboratory of Dr. Ole Isacson, Associate Professor of Neurology at
Harvard Medical School and Director, Neuroregeneration Laboratory at
McLean Hospital.
Neurophilin ligands are orally bioavailable small molecules that have
the potential to promote neurite outgrowth, prevent nerve damage, and
accelerate recovery following nerve injury. In the past, some
investigators have suggested that inhibition of the enzyme FKBP-12 is
required for these neural activities. Earlier this month, however,
Vertex reported for the first time that compounds that do not interact
with FKBP-12 can improve outcomes in animal models of peripheral
neuropathies. The results reported in Vancouver show that central
nervous system activities of these compounds also do not require FKBP-12
interaction.
In one set of experiments, the neurophilin compounds V-10,367 and
V-13,661 were administered orally to mice exposed to MPTP, a neurotoxin
selective for dopamine-producing neurons in the brain. Both neurophilin
compounds prevented the loss of striatal tyrosine hydroxylase, a marker
for dopamine, compared to control. V-10,367 is known to bind to the
enzyme FKBP-12. These new results extend earlier findings with V-10,367,
and show a comparable potent neuroprotective effect for V-13,661, a
compound which does not bind to FKBP- 12. V-13,661 is structurally
similar to timcodar dimesylate, a neurophilin compound currently being
tested by Vertex in a Phase II clinical trial in patients with diabetic
neuropathy.
``Through our extensive research program, we have produced neurophilin
compounds that are orally bioavailable and penetrate the brain. Our data
demonstrate that these compounds prevent neurological damage and improve
functional outcome in a range of neurological disease models,'' said Dr.
Joshua Boger, Chairman, President and CEO of Vertex. ``Importantly, we
have found that FKBP binding is not required for these activities. We
are excited by these findings and expect to substantially increase our
biological understanding of these effects.''
Results were also presented for the compound V-10,367 in a rat model of
progressive and extended neurological damage. In this experiment, the
neurotoxin 6-hydroxydopamine was injected in the striatum of rats, and
oral administration of V-10,367 significantly protected against
degeneration of striatal dopamine innervation and nigral dopamine
neurons with indications of functional improvement.
``Progressive neural degeneration is the fundamental source of the
physical and behavioral deterioration in patients with Parkinson's
disease,'' said Douglas Cole, M.D., Neurophilin Program Executive at
Vertex. ``Therapeutic strategies designed to slow or reverse damage to
the neuronal circuitry represent a significant potential breakthrough
for this debilitating disease.''
Vertex's press releases are also available by fax-on-demand at (800)
758- 5804 -- Code: 938395
SOURCE: Vertex Pharmaceuticals Incorporated
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More Quotes and News: Vertex Pharmaceuticals Inc (Nasdaq:VRTX - news)
Related News Categories: biotech, medical/pharmaceutical
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