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Gabapentin is one of the most commonly prescribed anti epileptics in the world. Gabapentin is primarily used to treat seizures, it also finds use in the management of neuropathy or nerve pain, post- herpetic pain, and is being investigated for use in psychiatric ailments such as bipolar mood disorders. |
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A seizure or convulsion reflects an imbalance between excitatory and inhibitory activity in the brain, with an increment of excitation over inhibition. The most important inhibitory neurotransmitter in the brain is GABA. Gabapentin has a structure similar to GABA. |
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| However, gabapentin is poorly absorbed, less than 60% of the administered dose reaches circulation. Bioavailability is affected mainly by variable absorption, which depends on active transport across the gastrointestinal tract by a mechanism called an large amino acid transporter. Absorption may be impaired in some clinical situations in which active transport does not function as well as it ought to. In addition, with single doses of gabapentin greater than 1200 mg, the bioavailability reduces to 35%. |
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| The molecule we are working on, SUN-44, is a prodrug of gabapentin having significantly higher bioavailablity, i.e., better absorption profile. A prodrug is an inactive precursor of a given drug, that once it is taken, is converted by enzymatic action into an active form. |
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Extensive animal studies have been carried out on SUN-44 so far. SUN-44 shows much better absorption, compared to gabapentin. In seizure and neuropathtic pain models, SUN-44 showed improved efficacy compared to gabapentin and competitor’s molecule which is currently in Phase III trials.
In repeat dose toxicity studies our compound showed good safety profile. |
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Current data about its profile indicates that it should be possible to administer SUN-44 as a once a day drug. |
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