Drug Formulation & Bioavailability WEST

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1 2nd Drug Formulation & Bioavailability WEST Newest Methods for Predicting Challenges to Solubility and Matching your Drug Compounds to the Ideal Formulation and Delivery Techniques June 2-3, 2014 Hilton San Diego Resort & Spa San Diego, CA Improve Efficiency and Speed in your Formulation Development! ELI LILLY Identifies Vehicles Best for Solubilizing Early-Stage Compounds GILEAD Targets CMC Methods that Improve Formulations on Rapid Timelines NOVARTIS Uses Modeling & Simulation to Reduce Reliance on Animal Studies that Lack Predictive Value Insight from Industry Leaders: AMITAVA MITRA Principal Scientist, Biopharmaceutics MERCK Overcome Preformulation Challenges Specific to Each Technology! PFIZER Identifies the Formulation Techniques Best Matched for Each Compound MERCK Unites Pharmaceutical and Manufacturing Expertise to Add Stability to Hot-Melt Extrusions TAKEDA Improves Oral Exposure through Particle Size Reduction PLUS: In-Depth Intensive Workshop: Predicting and Mitigating the Food Effect on Bioavailability Key Program Sessions Include: Building Technology Maps to Match the Best Method for Each Compound Bioequivalence Considerations for Fixed-Dose Combination Products Enhancing API Permeability and Solubility Adding Stability to Hot-Melt Extrusions Industrial Perspectives on Dissolution Method Development Microfluidic Platforms for Early Formulation Development Chemical Space and Molecular Weight as Challenges to Downstream Development SPONSORS: Mike Brandl Senior Research Scientist, Analytical Development GILEAD DAVID Bender Research Scientist ELI LILLY Ron Chen Senior Scientist, Analytical Chemistry & DMPK TAKEDA LIPING ZHOU Senior Scientist, CMC & Engineering IPSEN

2 WELCOME TO BIO WEST! Drug industry successes in the post-blockbuster era will depend on the accuracy and versatility of formulation and pre-formulation experts. There has never been greater need to rapidly diversify your product portfolio and find new therapeutic approaches; in addition, the massive rise of generics and biosimilars has led to a more urgent need to improve existing drugs in order to expand their lifecycles and maximize revenue. ExL Pharma invites you to its 2nd annual Drug Formulation & Bioavailability West conference. This year s exclusive case studies were chosen according to past audience demand. Their focus on the most urgent challenges in formulation and delivery techniques will help you dramatically improve solubility, maximize product lifecycles, and gain the best returns for your company s investments. Attendees will learn from in-depth examinations of: 99Clearly demonstrating bioequivalence of fixed-dose combination products 99Technical breakthroughs to add stability to hot-melt extrusions 99Identifying vehicles best for solubilizing early-stage compounds 99Maximizing form control and solubility 99Strategies to improve compound success and lower absorption challenges from the earliest stages 99Boosting ROI by using modeling and simulation to reduce reliance on animal studies that lack predictive value 99Brainstorming the best industrial strategies for dissolution method development And don t miss our in-depth workshop devoted to Predicting and Mitigating Food Effects on drug absorption and efficacy! The learning and networking that you achieve here will help your company overcome its most urgent solubility enhancement challenges, and thus save millions of dollars thanks to a more successful and compliant drug development pipeline. We look forward to welcoming you to San Diego this summer! Sincerely, Matt Greenbaum Matt Greenbaum Senior Conference Producer ExL Pharma Who Should Attend: 99Formulation / Pre-Formulation 99Pharmaceutical Development 99Preclinical Development 99Medicinal / Analytical Chemistry 99Characterization 99Analytical Development 99Drug Delivery 99Drug Discovery 99DMPK 99Material Science 99Life-Cycle Management 99Product Development 99Toxicology 99Pharmaceutics 99Physicochemistry 99Chemical Engineering 99Solid State 99Process R&D 99In-Licensing 99Partnering, Licensing & Alliance 99Intellectual Property This Program Will Also Be Of Interest To: 99Solubility Companies 99Formulation Characterization Specialists and Software Designers 99Drug Delivery Companies 99API Manufacturers CO-LOCATED EVENT: Your registration at this conference will also allow you to network with the industry leaders at the Promotional Review Committee Compliance & Best Practices West conference! HOTEL INFOrmaTION Hilton San Diego Resort & Spa 1775 E Mission Bay Dr. San Diego, CA Phone: Patent Expiry Legal Counsel SPONSORSHIP & EXHIBITING OPPORTUNITIES Do you want to spread the word about your organization s solutions and services to potential clients who will be attending this event? Take advantage of the opportunity to exhibit, underwrite an educational session, host a networking event, or distribute promotional items to attendees. ExL Pharma will work closely with you to customize a package that will suit all of your needs. If you require overnight accommodations, please contact the Hilton San Diego Resort & Spa at to book your room. ExL has reserved a block of rooms at a discounted rate for conference participants. Please mention ExL s June Meeting to take advantage of this discount. You must book your room by May 12th to be eligible for the discounted rate. Please book your room early, as the rooms available at this rate are limited.

3 Monday, June 2, 2014 / Intensive Workshop 8:00 Registration & Continental Breakfast 8:45 Introduction from Workshop Chairperson 9:00 Workshop Begins 10:30 Networking & Refreshment Break 11:00 Workshop Resumes 12:00 Lunch for Workshop Attendees WORKSHOP THEME: Predicting and Mitigating the Food Effect on Bioavailability There is a pronounced unmet need in the industry to reliably predict food effects before entering clinical trials, yet negative food effects in particular can be both highly difficult to avoid and antagonistic towards patients jeopardizing clinical adherence, clinical data quality, and overall market uptake. This workshop will emphasize: Predetermining when your rate-limiting steps will be solubility or permeability Overcoming food effects through mechanisms that set preferential absorption either very early or very late in the GI tract Humanizing animal models to improve predictive value Predicting transporter competition and impact on drug absorption Confront food effects through supersaturation and particle size options Tycho Heimbach, Senior Investigator II, Associate Director, NOVARTIS Chong-Hui Gu, Director, Head of CMC, AGIOS PHARMACEUTICALS Steven Sutton, Associate Professor, UNIVERSITY OF NEW ENGLAND SCHOOL OF PHARMACY Monday, June 2, 2014 / Main Conference Day One 1:00 Introduction from Conference Chairperson Optimizing New Formulation and Preformulation Techniques 1:15 Technological Breakthroughs to Add Stability to hot-melt Extrusions Supercoated fluids can make hot-melt extrusion techniques significantly easier to use, as can new plasticization techniques that fundamentally change the extrusion method itself. Many drug candidates for this formulation risk degradation through simple human error: as drug sponsors with an eye on reducing the use of raw materials attempt to reduce the flow rate, the resulting increased residence time within the extruder itself causes them to overheat and lose quality. Some drugs are particularly sensitive to this and must be monitored with special care during extrusion. Graciela Terife, Senior Scientist, Drug Solubilization, MERCK 1:45 Key Considerations of Formulation and Process parameters during Drug Product Development using hot-melt Extrusions (HME) Principles of HME process Application of HME process in the pharma industry Case studies: Formulation design of HME product during early development Challenges of HME process and their mitigation strategies Identification of critical process parameters of HME during scale-up Commercialization of a Fixed Dosage Combination Product using HME process - A Unique Perspective Indrajit Ghosh, Senior Project Manager, Pharmaceutical Development, CELGENE 2:15 CASE STUDY: Preformulation Options for improved Bioavailability The current high-throughput screening paradigm has yielded more and more drug candidates that are poorly soluble in water. These poorly soluble compounds in most cases will have poor oral exposure, posing significant challenges for drug safety evaluation and formulation development. Some common preformulation approaches to improve oral exposure include salt screening, amorphous API, particle size reduction, and solubility enhancing formulation vehicles. This session analyzes case studies that succeeded using these approaches Ron Chen, Senior Scientist, Analytical Chemistry & DMPK, TAKEDA 2:45 Spray Dried Dispersions: A Versatile and Scalable approach to Bioavailability Enhancement An understanding of the specific properties of a molecule enables deliberate selection of a technology for enhancing bioavailability. These properties define the problem statement and therefore inform the selection of the optimal technology platform. A majority of new drug candidates fall into the BCS Class II category and exhibit low aqueous solubility. For these compounds, spray dried amorphous dispersions represent a versatile and scalable technology with a proven track record for increasing bioavailability. Enhance aqueous solubility across a wide range of compound properties Employ large selection of applicable excipients for formulation optimization Scale support from pre-feasibility (10s of mg API) through Phase III clinical trials and commercial manufacture Nathan Bennette, Technical Group Leader, BenD Research 3:15 Build Technology Maps to Identify the Methods Best Suited for Each Compound s Challenges Formulation experts are presented with an often baffling spectrum of technical options, from micronization and lipid formation to cocrystals and amorphous solid dispersions; often, specific vendors or research partners will recommend the techniques that they can most easily provide to you, even if it isn t the optimal method for a particular product class. How can you best survey all the available options and choose the ones that best fit your specific drug candidate? Determine key types of experiments to rank risk assessments of each technology type Broadly survey the industry to understand the capabilities of each technology and whether it is compatible with your drug, your team, and your resources Design earliest-stage experiments to rule out inappropriate process candidates Ravi Shanker, Senior Research Fellow, Pharmaceutical Sciences, PFIZER 3:45 Networking Refreshment Break 4:15 CASE STUDY: Microfluidics a New Platform for early Stage Formulation Development Early formulation development is a significant challenge for the pharmaceutical industry, primarily because of the lack of drug materials available at this stage. The recent advances in microfluidics, which combines the use of tiny volumes of materials with precisely controlled experimental conditions, open new perspectives in the screening and development of clinical trials materials. This session highlights the utility of microfluidic platforms in aiding formulation optimization at the early stage of drug development. Sabiruddin Mirza, Research Associate, School of Engineering & Applied Sciences, HARVARD UNIVERSITY 4:45 CASE STUDY: Nanonization of API to Enhance Solubility Explore opportunities, challenges and applications of poorly soluble drugs and NCEs Using top-down methods for particle size reduction to enhance solubility Examining the process parameters and fundamental limits of using bead mills for particle reduction Selecting the correct machine design and materials for specific applications Overview of the clinical benefits and commercialized drugs utilizing nanotechnology Randall Smith, President, NETZSCH 5:15 Pre-Clinical Formulation Strategies: Keeping Up with the Recent Trends in Drug Discovery and Development In the early discovery phases, the compounds you work with are far from drug-like, and you will encounter them in quantities too low to be helpful for most formulation work. Both turnaround times and the vehicle effect can confound results of initial experiments. Identify vehicles best at solubilizing early-stage compounds Steer clear of excipients that confound pharmacological responses Gauge the severity of impact on clinical parameters caused by use of different excipients in preclinical studies David Bender, Research Scientist, Small Molecule Design & Development, ELI LILLY

4 Monday, June 2, 2014 / Main Conference Day One 5:45 Bioequivalence Considerations for Fixed-Dose Combination Products One of the challenges in registration of fixed-dose combination (FDC) products is in demonstrating that the FDC is bioequivalent to each individual drug (i.e. the mono products). Lack of bioequivalence data would mean additional phase-iii studies with the FDC product to show safety and efficacy, which is a drain on time and staff resources. From a PK perspective, what are the best ways to make sure your drugs behave the same way together as they did when separate? Explore formulation, drug substance and regulatory challenges in assessing bioequivalence Use of preclinical studies (dissolution, animal PK studies and modeling) to guide FDC formulation development Case studies highlighting the challenges in achieving bioequivalence for FDCs and strategies to mitigate such challenges Amitava Mitra, Principal Scientist, Biopharmaceutics, MERCK 6:15 End of Day One Tuesday, June 3, 2014 / Main Conference Day Two 8:00 Continental Breakfast 9:00 Recap of Day One from Chairperson 9:15 Maximize ROI on Research by Using Modeling & Simulation to Reduce Animal Studies that Do Not Add Predictive Value Crossover animal studies of multiple different formulations are not the best investment of time or resources, and likely will not predict human response. Merging the expertise of the modeling & simulation community with the formulation community will allow you to avoid unnecessary animal studies in formulation screening. Cultivate the habits of mind necessary for models and simulations that predict human outcomes while minimizing animal studies Set new performance standards expecting these skills from your team Apply the most useful lessons from post-formulation and DMPK Tycho Heimbach, Senior Investigator II, Associate Director, NOVARTIS Advances in Improving Drug Solubility 10:00 Kinetics and Thermodynamics: Using Clinical Data to Drive Effective Solubilization Technology Selection John McDermott, Director of Drug Product Optimization, QUOTIENT CLINICAL 10:45 Networking & Refreshment Break 11:15 CASE STUDY: Terahertz Spectroscopic Analysis of Crystallinity and Amorphous Content in Drug Substances and Drug Products The crystalline state of an API can have a dramatic effect on its stability and bioavailability. Many APIs are known to exist in a variety of crystalline states. This includes occurring in multiple crystalline polymorphic forms as well as in an amorphous state. Terahertz spectroscopy is highly sensitive to the lattice vibrations of these different solid forms. This session presents case studies where this method was able to rapidly distinguish between these different forms, even in mixtures of more than one species. Mark Sullivan, Senior R&D Scientist, ADVANTEST 12:00 Technology Spotlight: ElectroNanospray: A Highly Robust System for Creating Complex Nanoparticles in a Single Processing Step Robert Hoerr, Co-Founder, CSO, NANOCOPOEIA 12:20 Strategies for Dissolution Method Development: An Industrial Perspective An IVIVC is not always available for the dissolution method for many drug products, and regulatory guidelines allow for methods that are only suitable as a quality control test by establishing batch-to-batch consistency between clinical (e.g. tablets used in Phase III) and commercial products. In these cases, focusing CMC activities on development of a quality control dissolution test ensures patients will receive efficacious product. This strategy is also accommodating of rapid timelines during clinical development, particularly when formulation compositions or strengths are evolving. This presentation focuses on: Reviewing dissolution method development strategies during clinical development (Phases I, II, III) Evaluating approaches for demonstrating suitability of a dissolution method as a quality control test Case studies and approaches for selecting quality criteria Mike Brandl, Senior Research Scientist, Analytical Development, GILEAD Victor Rucker, Senior Research Scientist, Analytical Development, GILEAD 1:00 Luncheon 2:00 Strategies to Improve Compound Success and Reduce Absorption Challenges from the Earliest Stages By better focusing on the discovery & development interface, drug sponsors can significantly boost the chances that compounds will avoid downstream absorption and other delivery challenges. Through early engagement and partnership with Discovery, one can substantially de-risk drug candidates and enhance product value. Leverage molecular descriptors to guide candidate selection of compounds with desired physicochemical properties Evaluate formulation surrogates to forecast risk associated with orthogonal delivery routes Boost return on investment by preemptively avoiding typical problems of poor solubility Michael Lowinger, Principal Scientist, MERCK 2:45 Bioavailability Improvement via Solubility and/or Permeability Enhancement Addressing bioavailability as the interplay of solubility, permeability and metabolism Improving API solubility may not always provide enhanced bioavailability Strategies for permeability enhancement and superiority of balancing solubility/permeability Liping Zhou, Senior Scientist, CMC & Engineering, IPSEN 3:30 CASE STUDY: Parenteral Delivery of Water-Insoluble Drugs Poor water solubility of more than 60-80% of new chemical entities presents a major hurdle in the design of suitable drug delivery systems for the market dosage form. Administration of those compounds by parenteral route without causing injection site reactions and systemic toxicity effects constitutes another barrier. This session summarizes current solubilization and parenteral delivery technologies for water-insoluble drugs - especially key considerations in the design of stable parenteral drug delivery systems, such as drug physico-chemical and biopharmaceutical properties, selection and evaluation of solubilization and delivery technology, and excipients. The session includes case studies on the development of nanoemulsions and nanosuspensions. Jim Jingjun Huang, former Principal Scientist Formulation, ROCHE 4:00 End of Conference Very good examples provided. Great explanations to questions raised! Associate Director, Pharmaceutical Sciences, TAKEDA A very well-organized event! Scientist, DMPK, LEXICON PHARMACEUTICALS

5 SPONSORS: Media Partners: Registration Fees for Attending ExL s 2nd Drug Formulation & Bioavailability West conference: STANDARD PRICING Your Investment: Conference + Workshop: $2,295 Conference Only: $1,995 ONSITE PRICING Your Investment: Conference + Workshop: $2,395 Conference Only: $2,095 GROUP DISCOUNTS Save 25% Per Person when Registering Four For every three simultaneous registrations from your company, you will receive a fourth complimentary registration to the program (must register 4 at one time) this is a savings of 25% per person. Save 15% Per Person when Registering Three Can only send three? You can still save 15% off of every registration. Terms & Conditions By registering for an ExL Events, Inc. ( ExL Pharma ) event, you agree to the following set of terms and conditions listed below: Registration Fee: The fee includes the conference all program materials and designated continental breakfasts lunches and refreshments. Payment: Make checks payable to ExL Events, Inc. and write code C488 on your check. You may also use Visa, MasterCard, Discover or American Express. Payments must be received in full prior to the commencement of the conference. Any discount applied cannot be combined with any other offer and must be paid in full at the time of order. Parties must be employed by the same organization and register simultaneously to realize group discount pricing options. Group discounts available to individuals must be registered simultaneously and employed by the same organization. Cancellation and Refund Policy If you need to cancel your registration for an upcoming ExL event, please note the following policies derived from the Start Date of the event: Four weeks or more: A full refund (minus a $295 processing fee) or a voucher to another ExL event valid for 18 months from the voucher issue date. Less than four weeks: A voucher to another ExL event valid for 18 months from the voucher issue date If you cancel at any time after receiving the conference documentation, the voucher issued will be $395 less Substitution Charges: There will be an administrative charge of $300 to substitute, exchange and/or replace attendee badges with a colleague occurring within five business days of the conference. ExL Events reserves the right to cancel any conference it deems necessary and will not be responsible for airfare hotel or any other costs incurred by registrants. ExL Events liability is limited to the conference registration fee in the event of a cancellation and does not include changes in program date content speakers or venue. *The opinions of ExL speakers do not necessarily reflect those of the companies they represent, nor ExL Events, Inc. Please Note: Speakers and agenda are subject to change without notice. In the event of a speaker cancellation, significant effort to find a suitable replacement will be made. The content in ExL slide presentations, including news, data, advertisements and other information, is provided by ExL Events, Inc. s ( ExL s ) designated speakers and is designed for informational purposes for its attendees, and is NOT INTENDED for purposes of copywriting, nor redistribution to other outlets without the express written permission of ExL s designated speaking parties. Neither ExL, nor its content providers and/or speakers and attendees shall be liable for any errors, inaccuracies or delays in content, or for any actions taken in reliance thereon. EXL EVENTS, INC. EXPRESSLY DISCLAIMS ALL WARRANTIES, EXPRESSED OR IMPLIED, AS TO THE ACCURACY OF ANY THE CONTENT PROVIDED, OR AS TO THE FITNESS OF THE INFORMATION FOR ANY PURPOSE. Although ExL makes reasonable efforts to obtain reliable content from third parties, ExL does not guarantee the accuracy of or endorse the views or opinions given by any third party content provider. ExL presentations may point to other Internet sites that may be of interest to you, however ExL does not endorse or take responsibility for the content on such other sites

6 Conference Code: C488 Method of Payment: Check Credit Card Make checks payable to ExL Events, Inc. Card Type: o MasterCard o Visa o AMEX Card Number: Exp. Date: Name on Card: Yes! Register me for the Conference + Workshop Signature: Yes! Register me for the Conference Only Please contact me: I'm interested in marketing opportunities at this event I wish to receive updates on ExL Pharma's upcoming events Name: Title: Company: Dept: Address: City: State: Zip: Phone: Fax: 2nd Drug Formulation & Bioavailability WEST Newest Methods for Predicting Challenges to Solubility and Matching your Drug Compounds to the Ideal Formulation and Delivery Techniques June 2-3, 2014 Hilton San Diego Resort & Spa San Diego, CA Improve Efficiency and Speed in your Formulation Development! ELI LILLY Identifies Vehicles Best for Solubilizing Early-Stage Compounds GILEAD Targets CMC Methods that Improve Formulations on Rapid Timelines NOVARTIS Uses Modeling & Simulation to Reduce Reliance on Animal Studies that Lack Predictive Value Overcome Preformulation Challenges Specific to Each Technology! BRISTOL-MYERS SQUIBB Designs Process Strategies to Prevent Form Conversion in Wet Granulation Formulations MERCK Unites Pharmaceutical and Manufacturing Expertise to Add Stability to Hot-Melt Extrusions TAKEDA Improves Oral Exposure through Particle Size Reduction