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Technology | Programs | Pipeline | Collaborations | About Us | Contact Us |
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Inflammation
Inflammation
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Non-steroidal Anti-inflammatory |
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Unmet Need - Inflammation
has been implicated in myalgia, arthralgia, tendonitis, and dental/bone
irritation and reduction of inflammation resolves the corresponding pain
condition. Anti-inflammatory agents like
non-steroidal anti-inflammatory drugs (NSAIDS) are based on cyclooxygenase-1 (COX-1)/cyclooxygenase-2
(COX-2) inhibition and result in gastrointestinal (GI) distress. Hence, selective COX-2 inhibitors were
developed yet the cardiovascular protective effects of NSAIDs mediated through
COX-1 inhibition are lost. Emerging data regarding the role of the 5-lipoxygenase
(5-LO) pathway suggests its inhibition indirectly reduces TNF-a expression. Considering the influence of COX-2/5-LO pathway,
drugs able to block both pathways (dual inhibitors), should present a superior
anti-inflammatory profile than individual selective COX-2/5-LOX inhibitors.
Our Approach - Medisyn’s
approach is to use molecular topology (MT) to identify novel anti-inflammatory
agents without adverse effects to the GI system or increase in cardiovascular
risks based on dual inhibition of COX-2/5-LO activity. Separate individual
inhibitory (COX-1, COX-2, 5-LO and COX-2/5-LO) activity profiles were created to
define the molecular topological signature responsible for dual inhibition of
COX-2/5-LO activity with minimal COX-1 inhibition since it is unclear the
extent to which COX-1 inhibition is required to minimize cardiovascular risk.
Pipeline Highlights:
Multiple compounds in new chemical
classes inhibiting both COX-2 and 5-LO |
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