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Spasticity or muscular hypertonicity is a disorder of the body motor system, and especially the central nervous system (CNS), in which certain muscles
are continuously contracted. During the development of spasticity, the spinal cord undergoes neurophysiologic changes in the excitability of motor neurons, interneuronal connections, and local reflex pathways. |
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Spasticity is associated with neurological disorders like multiple sclerosis, stroke, cerebral palsy, spinal cord and brain injuries, and neurodegenerative diseases. |
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The pathophysiologic mechanisms causing the increase in stretch
reflexes in spasticity also are not well understood. This contraction causes stiffness or tightness of the muscles and may interfere with gait,
movement, and speech. |
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Antispasticity agents such as baclofen, tizanidine, dantrolene, and diazepam are used to improve muscle hypertonicity and involuntary jerks. |
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Baclofen is a gamma aminobutyric acid (GABA) derivative with central nervous system action. It inhibits transmission at spinal level and also depresses the central nervous system. |
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Baclofen is given orally with variable effects. In severely affected children, the oral dose is so high that side effects appear and the treatment
loses its benefit. Baclofen is rapidly and almost completely absorbed
from the gastrointestinal tract, but the rate and extent of absorption
vary between patients. |
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SUN-09 is a prodrug, a modified form of a drug used widely in the
treatment of spasticity. The modification in the structure increases the extent and rate of absorption significantly. The prodrug metabolises
into the active drug in circulation. Since absorption is consistent, there is better control over symptoms. |
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Animal studies and extensive tests to study the safety of SUN-09 in animal models have now been completed. In animal models of ataxia, SUN-09 showed reduction in fall off latency and fast onset of action compared to the marketed drug given orally and by intrarectal administration. In repeat dose toxicity, the drug showed a good safety profile. |
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SUN-09 will be developed for use as an injectable as well as a
once-a-day tablet or capsule. |
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