• TRPV1 is non selective ion channel with a preference for Ca2+.
• TRPV1 function as neuronal membrane recognition site for proton, heat, and irritant compounds such as capsaicin (CAP), resiniferatoxin (RTX).
• TRPV1 expressed exclusively by primary sensory neurons involved in nociception and neurogenic inflammation
• By TRPV1 functional modulation, neuropathic pain can be controlled.
• MDFR series compounds from Medifron_DBT have broad range analgesic effect on inflammatory pain through neuropathic pain.
• Also, those compounds showed very low pungency profile.
• It can be developed topical cream and gel formulation of TRPV1 agonist.
• The possible applications are Post Herpetic Neuralgia (PHN), Diabetic Peripheral Neuropathy (DPN) and Chemotherapy Induced Neuropathic Pain (CINP) etc.
• Applicable to broad range analgesics on inflammatory pain through neuropathic pain.
• Topical cream and gel formulation possible.
• Intervention area : Post Herpetic Neuralgia (PHN), Diabetic Peripheral Neuropathy (DPN), post operational pain and Chemotherapy Induced Neuropathic Pain (CINP)
3. Market Feasibility
• Pain market size is huge over 100B US$
• Neuropathic pain market is around 4B US$
• Topical analgesics make 1B US$ market
• Novel analgesics for neuropathic pain can expend market size
4. Technical Advantages
• Non of TRPV1 antagonist come out market place
• Several TRPV1 agonist already existed such as capsaicin cream/ patch, zucapsaicin cream
• Capsaicin patch has strong pungency profile. Patient should use Lidocaine as anesthetic before using capsaicin patch, it's very uncomfortable and high cost medicine
• MDFR series compounds showed non pungent and excellent effective topical treatment for neuropathic pain and inflammatory pain
• Broad application of non pungent TRPV1 agonist expected
5. Technical Highlighted Summary
• Less than 2mg/kg dosing, full efficacy showed in formalin test and neuropathic pain model test
• MDFR series compounds did not causing any irritation and edema in mice ear
• MDFR compounds are very much safer than capsaicin