INPHARMADevelopment of an innovativeanti-inflammatory drugwith a novel mechanism of action– inhibitor of inducible NO-synthase
Problem. Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used in medicine.Every year over 300 million people use them. All NSAIDs have one target –cyclooxygenase (COX), an enzyme responsible for prostaglandin synthesis. Due to thisNSAIDs have adverse ulcerogenic effect on gastointestinal mucosa, possibly causingdangerous bleedings. NSAIDs use causes 103 000 hospitalizations and 16500 deaths ayear in USA alone.Solution. Development of an anti-inflammatory drug with a new mechanism of action, notrelated to inhibition of COX, will solve this problem. The solution is based on a newmolecule, created under leadership of professor V. Granik. The new molecule is aderivative of aminoguanidine – the best selective inhibitor of inducible NO-synthase,bonded with a structural component – a “carrier”, which ensures high bioavailability of thedrug in oral use, high potency and better safety profile.Technology is based on selective inhibition of inducible NO-synthase (iNOS). Thisisoform of the enzyme catalyzes excessive production of nitric oxide, which is a mainmechanism of pathological inflammation. Experiments (on peritonitis models) have proventhe new compound’s potent anti-inflammatory activity. The compound’s safety is proven –its LD50 > 5000 mg/kg (mice, per os) which is much better than LD50 values of the knownNSAIDs (diclofenac, indomethacin, etc.).Problem & Solution
World market. In 2010 world sales of NSAIDS (Anti-Reumatics, Non-Steroidal, according toIMS Health data) amounted to $10.15 billion. Sales leader - Celebrex (Pfizer) – $2.49 billion.Competitors:1) Classic NSAIDs (non-selective COX inhibitors) –have gastrointestinal adverse effects.2) Selective COX-2 inhibitors: coxibs (Celebrex, etc.), nimesulide - cause complications ofcardiovascular system, increased liver and kidney toxicity.Advantages:The new drug does not inhibit COX activity, so it does not cause adverse ulcerogenic effectsthat lead to hospitalizations and deaths of many patients using NSAIDs.Potential customers – “Big Pharma” companies, interested in market launch of a novelNSAID – iNOS inhibitor exhibiting high effectiveness, selectivity, high bioavailability in oral useand good toxicity and adverse effects profile.Business model provides for licensing the development after finishing Phase I and II clinicaltrials in Russia (2016-2017) with transferring rights to a strategic investor(s) (Russianpharmaceutical company, “Big Pharma” company) for certain markets. Planned volume ofdeals (license agreements), including up-front and milestone payments – at least $100 million.Market & Business model
TeamLeader:Khazanov Veniamin, professor, PhD, an expert in drug development andcommercialization. Since 1991 he has been doing high technology business,has 20 years of experience in organizing and managing projects of drugdevelopment for medical purposes. Creator and head of “iPhar” group ofcompanies - one of the leading Russian centers of drug development.Science team, key persons:Belska Nataly, PhD - pharmacologist, immunologist. Work experience: ScientificInstitute of Pharmacology of Siberian Branch of Russian Academy of MedicalSciences – head of Department of Experimental Biological Models, ZAO“INPHARMA” – director of preclinical trials. Responsibility: organization andcontrol of preclinical trials of the drug.Joseph Schwarz, PhD - world-class expert in the fields of pharmaceuticaltechnology, drug formulation and manufacturing technology (Canada).Formerly one of the heads of formulation department of TEVA (Israel). Advisoron pharmaceutical development of the substance and dosage forms of the anti-inflammatory drug.
Project needsR&D platformINPHARMA has the necessary resources (laboratories, equipment and staff) fordeveloping laboratory synthesis technology of the substance for the newdrug, production of test samples for preclinical trials, studying itspharmacological activity.IPHAR company is the main partner (R&D platform) for preclinical trials anddosage form development of the new drug as well as for IP protection issuesand project commercialization. IPHAR has the necessary materialresources, qualified staff and established network of partnerships with highereducation institutes, scientific institutes and clinical centers of Russia, foreignorganizations and specialists from UK, Sweden, Italy, Canada, USA, Israeland other countries.Financial needsCo-investments (about 20 million rub.) and grant funding (20 million rub.) - forperforming preclinical trials of the new drug.