Developing EXP-1801 as an imaging agent to quantify pain and analgesia

Summary Abstract There are currently no tools available that can objectively measure painHistoricallypain in humans has been measured using subjective ratings to determine presence and severityIn animal modelspain is measured by semi quantitative assays that rely on the observation of pain behaviorsThough usefulthe inherently subjective nature of these measures has hampered both research and treatment effortsSimply putinaccurate pain measurement leads to inaccurate pain managementOvertreatment and addiction to pain medications are a continuing epidemic in the U SThe estimated economic burden of chronic pain is estimated to exceed $billionOne advantage of an objective pain measuring technology is cost reductionThe average cost to treat a chronic or neuropathic pain patient is $per yearThese costs are exaggerated because many patients have inadequately managed painwhich requires disproportionately more resourcesA significant portion of these costs go to patients who are not experiencing substantial paine gthose who abuse opioidsAnother area where costs could be significantly reduced is in drug developmentThe average pain clinical trial cost is around $millionThe use of a pain imaging technology would allow for objective efficacy databoth pre clinically and in clinical trialsand reduce costs by enabling smaller sample sizes due to more homogeneous populationsi ewith a particularpain signaland more accurate measurement of analgesic effectsWe recently invented a novel positron emission tomographyPETimaging agent that we developing as a tool to address these issues in pain care and therapy developmentAlthough the ability of PET to detect pathological changes forearlydisease detection is widely used in cancer and neurological diseasesit has not yet been used for pain indicationsWe have tested this molecule in healthy rats and non human primates and found a strong signal to background ratio in nerve tissueOur ultimate goals areto change the evaluation ofexperimentalpain therapiesandthe standard of care in pain assessment through molecular imagingThe proposed study is designed to determine the feasibility of our imaging agent to objectively measure pain in rodentsThis will set the stage for a Phase II study that further develops this agent into a tool for quantifying pain analgesia Project Narrative Voltage gated sodium channelsNaVsare centrally involved in pain transmissionincluding aberrant function and expression levels leading to hyperexcitabilityWe recently invented the first positron emission tomographyPETligand for quantifying painThe goal of this Phase I project is to determine the feasibility of this ligand as a technology that objectively and reliably indicates the presence and level of pain in a preclinical study