A Novel Drug Development Approach

ACCELERATE MORE MOLECULES TO CLINIC WITH Novel Drug Development Approach A customized and multidisciplinary platform can identify the most suitable drug delivery technology during early-stage drug development, reduce potential risks and contribute to overall time and cost savings. DAYS OF LOW-HANGING FRUIT IN THE DRUG DISCOVERY ERA ARE OVER Comparison of Marketed vs. Pipeline Drugs Shows Trend Towards Low Solubility •90% of pipeline drugs have low solubility 36% of marketed drugs have low solubility The Innovator's Pipeline, Ralph Lipp, American Pharmaceutical Review, http://ow.ly/VRTvn Poor solubility leads to poor bioavailability and further challenges in drug development. CHALLENGES DURING EARLY-STAGE DRUG DEVELOPMENT ARE INCREASING Challenges at the Molecule Level Meeting the Development Criteria A Limited availability of the active pharmaceutical ingredient (few grams) Quality CMC (early and late) Adequate PK profile Efficacy Only semi-quantitative information available at early stages Lower inter- and intrapatient variability of PK behavior is desirable (AUC, CMAX, avoidance of food effect, etc.) Speed Fast to proof of concept Seamless transition to full development and market Risk High attrition Low bioavailability Late technology changes Cost Development cost Aggregate development cost Cost of goods Balancing the Short and Long-Term Needs at Every Stage formulation & PK profile developability & pre-formulation - suitable first-in-man formulations manufacturability - solubility data - permeability data - expected efficacious dose (human) - solid state information (salts, polymorphs) scalability -expected bioavailability - expected CMAX, CMIN - suitable formulation shelf-life drugability Phase I Pre-clinical NEED FOR A NEW DRUG DEVELOPMENT MODEL The linear R&D model leads to 1 out of 10 drug candidates reaching patients. A parallel and customized approach will give each molecule the best chance to succeed. Optiform Solution Suite - A Novel Approach to Enhance Bioavailability 1 Select Faster 2 Kill Earlier 3 Improve Outcome Risk-based scenario Select the right advanced delivery approach faster by applying high throughput screening tools factoring in physical, chemical, processing and biopharmaceutical risks Better prepared to face the next bioavailability hurdle beyond exposure: limit variability, reduce CMAX/CMIN ratio Staged and parallel screenings are key to success Progressive and data-driven de-risking process Process Roadmap of Optiform Solution Suite Bioavailability Enhancement in 12 Weeks 1 Assess Enhance 3 Deliver High throughput molecule characterization DISSOLUTION ISSUES ENHANCED BIOAVAILABILITY - Particle size reduction - Salt form Expert technical report Physicochemical properties Candidate formulation materials SOLUBILITY ISSUES Bioavailability/developability classification - Lipid formulation -Solid dispersion or solution For more information on optimizing API performance in the early drug discovery stage, visit: www.catalent.com/optiformebook Catalent. www.catalent.com Catalent. © 2016 Catalent, Inc. All rights reserved.