DRUG FORMULATION & BIOAVAILABILITY

January 26-28, 2015 | Hilton Boston Logan Airport | Boston, MA

ALL-NEW CASE STUDIES:

FOUR IN-DEPTH PROGRAM TRACKS FOCUSING ON THE NEWEST BIOAVAILABILITY ENHANCEMENT TECHNIQUES:

• Modeling & Simulation for Enabled Formulations

• Managing Formulation Evolution Throughout Drug Life Cycles

• Team Leadership Styles for Advanced Formulation Development

• Rethinking Early-Stage Formulation Methods

Michael Ausborn Site Head, Pharma Research & Early Development F. HOFFMAN – LA ROCHE

• Agnostic modalities in future drug development

• Action plans to proceed without real human data

• Solid-state chemistry as the next focal point for drug design

• Latest challenges in simulating supersaturation

• Adjust to the shorter developmental timelines of fixed-dose

combinations

• Optimal screening approaches for cocrystals

• Identify and address pH-dependent absorption

• Risk protocols for photoreactivity and phototoxicity

• Transition your teams from small to large molecule work

• Device-based oral biologic delivery

4th

Robert Saklatvala Director, Basic Pharmaceutical Sciences MERCK

Keith Horspool VP, Pharmaceutical Development BOEHRINGER-INGELHEIM

Evan Thackaberry Therapeutic Area Leader, Safety Assessment GENENTECH

Sponsors/

Distinguished Speaker Faculty Includes:

Breakthrough Techniques in Optimizing the Screening, Delivery, Solubility, and Stability of Drugs and Biologics to Enhance Product Life Cycles

TWO EXTENSIVE INTERACTIVE WORKSHOPS SETTING

BEST PRACTICE FOR YOUR GREATEST CHALLENGES:

• The Industry’s Technical and Regulatory Path Forward forPediatric Formulations

• Selecting Methodologies, Priorities, and Risks in Salt andPolymorph Screening

Riccardo Panicucci Global Head, Chemical & Pharma Profiling NOVARTIS

Liping Zhou Senior Scientist, CMC & Engineering IPSEN

“An excellent event with very focused views of new technologies.”

— Senior CMC Team Leader, ALCON

HOTEL INFORMATIONHilton Boston Logan Airport One Hotel DriveBoston, MA 02128

To make reservations, please call 1-800-445-8667 and request the negotiated rate for ExL’s 4th Drug Formulation & Bioavailability Conference. You may also make reservations using the following weblink: http://www.hilton.com/en/hi/groups/personalized/B/BOSLHHH-EXL-20150125/index.jhtml. The group rates are available until January 5, 2015.

DEAR COLLEAGUE,The biopharma industry, facing unprecedented regulatory and patent-life pressure, is

leaning harder than ever on its formulation teams in order to accelerate time-to-market,

expand product life cycles, and maximize revenue. Longstanding challenges to drug

solubility are still causing development slowdowns, with 90% of APIs and 40% of drugs

at market believed to be poorly-soluble. Only by employing the most innovative new

formulation and delivery technologies, and accurately matching each type of molecule

to its optimal design and delivery method, can you make significant progress against this

challenge.

And amidst these ever-present problems, you are now facing new regulatory hurdles,

particularly regarding FDA’s position on the development of pediatric formulations for all

new drug candidates.

That is why you cannot afford to miss ExL Pharma’s 4th Drug Formulation &

Bioavailability conference. Built specifically around feedback from YOU – our audience

– the 2015 conference features an all-new program that targets your greatest and most

immediate formulation, solubility, permeability, and bioavailability challenges.

Across 3 full days, and featuring more than 6 hours of unparalleled networking, 4 unique

program tracks, 2 in-depth interactive workshops, and over 200 of the industry’s most

distinguished drug formulation, preformulation, and delivery experts, your attendance

will prepare you to:

9 Develop action plans when real human data is lacking

9 Explore the potential for solid-state chemistry as the next breakthrough in drug

design

9 Select the optimal technologies for advancing drug candidates and maintaining a

robust pipeline

9 Transition your formulators from small-molecule work to peptides and biologics

9 Improve your modeling & simulation tactics for enabled formulations

9 Successfully redesign previously-unworkable drugs on a molecular level

9 Set priorities and risks in salt and polymorph screening

9 Adapt to new scientific and regulatory challenges in the development of pediatric

formulations

I look forward to welcoming you to Boston alongside the leaders of the biopharma

industry so we can set next practice together!

Sincerely,

Matt GreenbaumMatt GreenbaumSenior Conference Producer ExL Pharma

WHO SHOULD ATTEND: Pharmaceutical and biotech executives responsible for:

9 Pharmaceutical development

9 Preclinical development

9 Formulation

9 Preformulation

9Medicinal / Analytical / Solid-State Chemistry

9 Physicochemistry

9 Pharmaceutics

9 Pharmacokinetics / DMPK

9Drug Delivery

9Drug Discovery

9Material Science

9 Life-Cycle / Portfolio Management

9 Toxicology

9Chemical Engineering

9 Process R&D

THIS PROGRAM WOULD ALSO BE OF INTEREST TO:

9 Solubility / Formulation Characterization service providers

9Drug Delivery specialists

9API manufacturers / providers

9CROs

9CMOs

SPONSORSHIP & EXHIBITING OPPORTUNITIESDo 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.

WELCOME TO BIO EAST!

“Very good examples provided. Great explanations to questions raised!”

– Associate Director, Pharmaceutical Sciences, TAKEDA

PRE-CONFERENCE WORKSHOP DAY – MONDAY, JANUARY 26TH, 2015

8:30 Registration and Continental Breakfast for Morning Workshop Participants

9:00 MORNING WORKSHOP:

The Industry’s Technical and Regulatory Path Forward for Pediatric Formulations g Overview of FDA preferences for the developmental timeline of pediatric versions of all new drugs and the need for greater regulatory clarity g Brainstorm the development of more discriminating methods than the hundred-person profile g Isolate the formulations, ingredients, excipients, and sugars linked to pediatric products that represent the greatest analytical challenge g Understand acceptable levels of degradation of pediatric products g Extrapolation from adult products to pediatrics – when does it work and when doesn’t it? g Determine the best data submission packages for your PIP and pediatric strategy to different regulatory agencies g Reorient your development cycle around these additional formulation needs

Manuel Sanchez-Felix, Senior Fellow, Formulation, NOVARTIS

Elizabeth Galella, Research Scientist, BRISTOL-MYERS SQUIBB

Madhavi Srikoti, Research Scientist, BRISTOL-MYERS SQUIBB

12:00 Luncheon for AM Workshop Participants; Registration for Afternoon Workshop

1:00 AFTERNOON WORKSHOP:

Selecting Methodologies, Priorities, and Risks in Salt and Polymorph Screening g Target the screening techniques that give you the highest confidence in form stability and solubility g Employ different crystallization methods to give the clearest understanding of the compound’s purity profile g Understand the full scope of relationships between crystallization and screening methods – pros and cons of each g Maximize form stability during scale-up through exploring different solvents, ratios, and procedures g Ensure you maintain the same API ratio in cocrystals during production scale-up – compare and contrast different methods g Instill new habits of mind for cocrystal screening based on understanding our system, the importance of proper crystallization,

and avoiding impractical techniques i.e. Grinding, melting g Set best practice on screening and bioavailability testing based on your company’s acceptability criteria g Measure amorphous content and particle size during and after scale-up of salts to test characterization and solubility g Differentiate between essential elements of molecular and formulation screening g Determine the ideal material for further stability and solubility steps based on the amount of crystal in your sample g Focus patenting strategy on platform technology in cases where you are partnering with other companies on co-developed molecules g Predetermine cases where the formulation is so instrumental to function that you must patent both molecule and formulation

Marianne Langston, Senior Scientist, Chemical Development, TAKEDA

Brian Chekal, Senior Principal Scientist, Crystallization Process Development, PFIZER

4:00 End of Workshop Day

“Informative and thought-provoking. Great panel discussions!”

– President, AMYLYX PHARMACEUTICALS

“A very well-organized event!”

– Scientist, DMPK, LEXICON PHARMACEUTICALS

WORKSHOP DAY CHAIRPERSON: Keith Horspool, VP, Pharmaceutical Development, BOEHRINGER-INGELHEIM

7:45 Registration Opens & Continental Breakfast

8:45 Chairperson’s Day One Welcome and Opening Remarks

9:00 KEYNOTE: Future Trends in Drug Formulation: Agnostic Modality

g Consider a broader focus beyond pill formulations g Expand delivery tools in early discovery to design molecules for various

administration routes g Brainstorm minimally-invasive delivery of poorly permeable drugs g Design delivery systems to support better patient adherence

Robert Saklatvala, Director, Basic Pharmaceutical Sciences, MERCK

9:45 KEYNOTE: An Action Plan for the Lack of Real Human Data

g Gain insight into formulation methods through awareness of failures as much as successes

g Grasp the significance of the knowledge gap between preclinical and clinical AUC and CMAX data

g Reorient knowledge-sharing towards the correlation of specific methodologies with human outcomes

g Examine the threats to formulation timelines and budgets when different suppliers of the same API yield slightly different purity profiles, processing, performance, and bioequivalence result

Dongmei Qiang, Senior Principal Scientist; Manager, External Collaborations, BOEHRINGER-INGELHEIM

10:30 KEYNOTE: Selecting Technologies that Overcome Solubility Challenges and Advance Drug Delivery and Pipeline Robustness

Michael Ausborn, Site Head, Pharma Research & Early Development, Basel, F. HOFFMAN-LA ROCHE

11:15 Networking & Refreshment Break

11:45 PANEL: “Think Outside the Tablet”: Examine and Explain the Slowdown in New Formulation Approaches

g Understand the limiting scientific explanations behind why no novel widespread formulation approaches have been adopted since solid dispersion technology

g Identify what the industry is missing through an excessive focus on oral administration

g Examine the prospects for achievable new drug targeting and device techniques for parenteral delivery that would not require new formulations

Riccardo Panicucci, Global Head, Chemical & Pharmaceutical Profiling, NOVARTIS

Robert Saklatvala, Director, Basic Pharmaceutical Sciences, MERCK

Speaker TBD, ABBVIE

12:45 Luncheon

MAIN CONFERENCE, DAY ONE – TUESDAY, JANUARY 27TH, 2015

TRACK A Modeling & Simulation for Enabled Formulations

TRACK B Managing Formulation Evolution Throughout Drug Life Cycles

1:45 Nanoformulations to Enhance Bioavailability of APIs

Suresh Bandari, Principal, ST. PETER’S INSTITUTE FOR PHARMACEUTICAL SCIENCES

Utilization of Formulation Design Space to Accelerate Early Clinical Development of Drug Products

g How the inclusion of formulation design space within clinical programs gives real-time flexibility in dose and composition of drug products

g Benefits and applications across the development life cycle including first-in-human studies and optimization of drug product formulations

g Case studies: overcoming solubility challenges for BCS II compounds, optimizing MR formulations, performing early assessments of IVIVCs and developing non-oral dosage forms

Peter Scholes, CSO, QUOTIENT CLINICAL

2:30 Nanonization of API to Enhance Solubility g Exploring opportunities, challenges, and applications of poorly-soluble drugs and

NCEs g Using top-down methods for particle size reduction to enhance solubility g Examining the process parameters and fundamental limits of using bead mills for

particle reduction g Selecting the correct machine design and materials for specific applications g Overview of the clinical benefits and commercialized drugs utilizing nanotechnology

David Watkins, Application Manager, Pharmaceuticals, NETZSCH

Formulation Bridging and Relative Bioavailability Risk Assessment Throughout Development

g Regulatory requirements and expectations for bioavailability assessment at multiple development stages

g ”Biowaivers” for changes to drug product g Risk-based approach to relative bioavailability decisions g Examples of risk assessment outcomes

David Sperry, Research Advisor, Small Molecule Design & Development, ELI LILLY

MAIN CONFERENCE, DAY ONE – TUESDAY, JANUARY 27TH, 2015

3:15 Latest Challenges in Simulating Supersaturation g Overview of the enhancements made to enable supersaturated formulations g Select the best methods for predicting how long supersaturated conditions will be

sustained g Estimate how much supersaturation impacts overall formulation performance g Design in-vitro models best capable of predicting and assessing supersaturations

Chris Towler, Principal Scientist, NOVARTIS

Novel Automated Analysis Methods for Biorelevant Dissolution

g In vitro methods show how APIs and formulations behave in presence of simulated gastric and intestinal pH and biorelevant media (FaSSIF and FeSSIF); the quest for IVIVC

g In vivo predictive dissolution methodology; biphasic dissolution to model GI dissolution and absorption

g Monitoring precipitation from supersaturated solutions and studying the effect of precipitation inhibitors

John Comer, CSO, SIRIUS ANALYTICAL

4:00 Networking & Refreshment Break

4:30 Dosing and Dispersability Studies to Model Supersaturation g Look into excipient options that would allow you to predict or maintain

supersaturation and prevent rapid precipitation g Identify the trends in compound crystalline structure most associated with rapid

nucleus formation, alignment, and precipitation g Properly dose your amorphous solid dispersions for animal studies g Gauge the likelihood of maintaining an amorphous state while in oversaturated

solution

Mengwei Hu, Development Fellow, Basic Pharmaceutical Sciences, MERCK

CASE STUDY: In-Vitro Experiments and Simulation Approaches to Identify and Address pH-Dependent Absorption

g Use in-vitro dissolution and simulation to design acidified formulations of weak bases that minimize the impact of variable gastric pH

g Grasp the role of supersaturation in enhancing absorption of poorly-soluble weak bases

g Utilize buffered formulations and modeling to reduce precipitation of poorly-soluble weak acids

Michael Perlman, Senior Scientist II, Pharmaceutical Profiling, MILLENNIUM PHARMACEUTICALS

5:15 Avoid Underpredicting Exposures through Better Modeling of Enabled Formulations

Manuel Sanchez-Felix, Senior Fellow, Formulation, NOVARTIS

Stepwise Approach to Preformulation and Formulation Development to Maximize Success

Paul Sabo, Senior Technician, PDS Formulation Development, PATHEON

6:00 End of Day One

“Very well-organized with great

content. This event will be a great

reference for the future!”

– Scientist, Pharmaceutics, PHARMATEK LABORATORIES

“Fascinating mix of industry researchers and technologies.”

– Director of Pharmacy Nanotechnology, CONCORDIAUNIVERSITY OF WISCONSIN SCHOOL OF PHARMACY

”Great presentations - clear and knowledgeable.”

– VP, Product Development R&D, CORERX

11:00 KEYNOTE: Oral Delivery for Biologics: Formulations and Other Potential Strategies

g Though IV delivery of standard biologics gives 100% bioavailability, oral formulations can sometimes deliver better results or an improved clearance rate

g Survey the different approaches industry is taking towards oral biologic formulations, through new technical tools and cross-company partnerships

g Identify why some oral formulations fail and carry those lessons forward into the next generation of biologics

g Transcend standard formulation challenges through device-based consumable oral delivery methods

Riccardo Panicucci, Global Head of Chemical & Pharmaceutical Profiling, NOVARTIS

11:45 In Situ Concentration Monitoring as a Measurement Tool within In Vivo Predictive Dissolution Systems

g Recognize the greater need for analyzing realtime free drug concentration g Identify the challenges to in-situ monitoring presented by bio-relevant

simulated fluids and complex foods containing dissolution media g Deploy in-situ measurement tools to reduce mechanical complexity of

pumping-based sampling systems and provide a very high density of realtime concentration data

g Gain insight into drug and formulation behavior via combining the dual-chamber dissolution-permeability setup with the ability to monitor concentration in both compartments

Konstantin Tsinman, Director, Science & Research, PION

12:30 Luncheon

1:30 Aligning Multiple Prediction and Evaluation Methods for Preclinical Formulations

g Choose the best methods for solubility enablement - solubilization or supersaturation?

g Weigh benefits and limits of preclinical in-silico oral absorption modeling g Review early formulation screening techniques g Analyze appropriate formulations to support drug candidate selection and

risk profiling: PD activity, PK clinical projection, and toxicology studies

John Morrison, Senior Research Investigator, Discovery Pharmaceutics, BRISTOL-MYERS SQUIBB

2:15 Molecular Redesign of Previously Unusable Drugs

g Quantify the amounts of poor drug selectivity and/or excessive toxicity that can be salvaged through new redesign methods

g Screen through early drug candidates that failed due to excessive toxicity and prioritize them for potential redesign

g Clearly demonstrate the link between drug potency and targeting potential g Redesign drug molecular size and receptor preference to avoid once-

unacceptable toxicity levels

Suparna Gupta, Principal Scientist, TRANSTECH PHARMA

3:00 Conference Concludes

8:30 Continental Breakfast

TRACK A Team Leadership Styles for Advanced

Formulation Development

TRACK B Rethinking Early-Stage Formulation Methods

9:00 Overcoming Challenges Formulating High-Drug-Load Fixed-Dose Combinations

g Gauge impact of API attributes on formulation design strategy and product performance

g Incorporate solubility-enhancing technology in fixed-dose combinations g Formulate APIs to provide differentiated release profiles g Use API-sparing tools for identifying and mitigating manufacturing risks

Larry Rosen, Director, Formulation & Basic Pharmaceutical Sciences, MERCK

Solid-State Chemistry: The Next Focal Point for Drug Design g Optimize solid form selection strategy to improve bioavailability and stability g Profile key API physical properties to yield physical forms and particles to

streamline dosage form design and manufacture g Focus on solid-state chemistry and particle properties as the key step in

formulation development for a new generation of drugs

Weili Yu, Senior Principal Scientist, PFIZER

9:45 Transition your Formulators from Small-Molecules to Peptides and Biologics

g Make industry progress towards larger-molecule formulations when companies are not hiring new specialized staff for this purpose

g Clarify how peptide and biologic specifications are set and formulations are implemented with teams more accustomed to working with small molecules

g Build off foundational analytical / bioanalytical skills to enable quicker transitions into peptide and biologics work

Liping Zhou, Senior Scientist, CMC & Engineering, IPSEN

A Strategic Approach to the Regulatory Challenges of Phototoxicity Assessment

g Track the history of photoreactive compounds and their impact on both solubility and patient phototoxicity

g Understand the recent ICH regulatory guidelines and interpret the most likely next steps from FDA and EMEA

g Design protocols and evaluate methods for photoreactivity and phototoxicity risk assessment

Evan Thackaberry, Therapeutic Area Leader, Safety Assessment, GENENTECH

10:30 Networking & Refreshment Break

PLENARY SESSION

MAIN CONFERENCE, DAY TWO – WEDNESDAY, JANUARY 28TH, 2015

SPONSORS:

Media Partners:

Save 15% Per Person when Registering ThreeCan only send three? You can still save 15% off of every registration.

Questions? Comments? Do you have a question or comments that you would like to be addressed at this event? Would you like to get involved as a speaker or discussion leader? Please email Program Director, Matt Greenbaum, at mgreenbaum@exlpharma.com

EARLY-BIRD PRICINGRegister Before Friday, December 12th, 2014:

All-Access Pass: $2,295

Conference and One Workshop: $1,995

Conference Only: $1,695

STANDARD PRICING After December 12th, 2014:

All-Access Pass: $2,495

Conference and One Workshop: $2,195

Conference Only: $1,895

ONSITE PRICING All-Access Pass: $2,595

Conference and One Workshop: $2,495

Conference Only: $1,995

Save 25% Per Person when Registering Four For every three simultaneous registrations from your company, you will receive a four th complimentary registration to the program (must register 4 at one time) this is a savings of 25% per person.

Registration Fees for Attending ExL’s 4th Drug Formulation & Bioavailability conference:

GROUP DISCOUNTS

Terms & ConditionsBy 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 C536 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

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• Four weeks or more: A full refund (minus a $295 processing fee) or a voucher to another ExL event valid for 12 months from the voucher issue date.

• Less than four weeks: A voucher to another ExL event valid for 12 months from the voucher issue dateIf 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 Pharma 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 Pharma’s 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

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January 26-28, 2015 | Hilton Boston Logan Airport | Boston, MA

DRUG FORMULATION & BIOAVAILABILITY

4th

Breakthrough Techniques in Optimizing the Screening, Delivery, Solubility, and Stability of Drugs and Biologics to Enhance Product Life Cycles

Sponsors/

Michael Ausborn F. HOFFMAN – LA ROCHE

Robert Saklatvala MERCK

Keith Horspool BOEHRINGER-INGELHEIM

Evan Thackaberry GENENTECH

Riccardo Panicucci NOVARTIS

Liping Zhou IPSEN