Overview

Several factors led to the recent emphasis on the field of transporters and their impact on drug absorption and disposition. Pharmaceutical industry continues to have keen interest in optimizing the physicochemical space of NCEs and minimizing their Cytochrome P-450 (CYP)-mediated metabolic liability. This led to the increasing selection of compounds that are both hydrophilic and polar in nature. Such chemical space inherits low passive permeability and metabolic clearance characteristics, and more importantly have potential contribution of transporters to their disposition in man. This paradigm shift presents the research community with a more difficult chemical space for addressing drug absorption and predicting pharmacokinetics and tissue distribution. Appropriate understanding of transporters and in vitro and in silico tools that characterize their contribution to drug absorption, disposition and toxicity is key for the success of the pharmaceutical industry. Additionally, the US FDA, EMA and other regulatory agencies provided new guidance on approaches to assess the liabilities of transporter-mediated drug-drug interaction (DDI), efficacy and organ toxicity for new chemical entities (NCEs) with special emphasis on certain transporters with considerable knowledge in the clinic.

Who should attend this course?

The interest in the field of transporters and their impact on drug absorption and disposition has been re-invigorated due to recent FDA and EMA guidance on approaches to assess transporter mediated DDI liabilities for NME. Therefore, this course is designed to serve a variety of scientific communities.

• Senior level managers and industrial, biopharmaceutics and contract research organization (CRO) scientists desiring to understand the overall role of transporters in drug absorption and disposition, subsequently to design compounds with transporter interaction for the optimization of PK/safety profiles.

• Regulatory scientists who needs to understand recent FDA and EMA regulations on drug transporters DDI.

• Scientists who develop and conduct in vitro transporter studies and/or in vivo pharmacokinetic studies.

• Registrants should possess a basic knowledge of drug discovery and development.

*This program is not accredited for Pharmacy CE/CPE

What are the benefits?

By the end of workshop, students will understand the role of transporters in drug disposition, physicochemical properties needed for NMEs to avoid or be substrates for various transporters. Also how to interpret data generated in in vitro/in vivo settings. It will also provide a better understanding of the recent FDA and EMA regulations and how to put them in context from drug development setting. This course will also provide an overview on approaches to characterize the potential for transporters mediated drug-drug interaction using both static and dynamic mechanistic/ whole-body PBPK modeling.

How are the workshops run?

The course is composed of lectures – delivered by leading experts in the field of transporters and provides in-depth overview of various topics presented. It is also mixed with a small group exercises with an expert tutor, where students will be presented with industry relevant examples to integrate acquired knowledge.

Program Faculty

Content

Day 1

Introduction

• Transporter basics – families and function
• Physiochemical Properties – refresher
• Extended clearance classification system [ECCS] and its utility in predicting drug clearance

Intestinal Transporters

• Introduction to oral bioavailability
• Impact of efflux transporters on oral bioavailability and Fa
• Impact of influx transporters on oral bioavailability and Fa and case examples

Hepato-biliary Transporters

• Introduction
• Physicochemical properties that affect drug biliary elimination
• The impacts of Organic Anion Transporting Polypeptide 1B1, 1B3, 2B1, and NTCP on drug disposition
• The impacts of Organic Cation Transporter 1 (OCT1) on drug disposition: Metformin as a case study

Renal Transporters

• Introduction
• Physicochemical factors that affect renal drug elimination
• Impacts of Organic Cation Transporter 2 (OCT2) on renal elimination
• Impacts of Organic Anion Transporter 1 and 3 (OAT1 and OAT3) on renal elimination
• The emerging role of Multidrug and toxin extrusion protein 1 (MATE1) and OAT2 in renal elimination

BBB Transporters

• Introduction
• Impact of efflux transporters on drug brain penetration
• Impact of influx transporters on drug brain penetration
• Preclinical models to assess brain penetration

Impact of metabolic disease on transporter expression and disposition

• Metabolic stress as a regulator of transporter expression
• Impact of metabolic disease on transporter expression in extra-hepatic tissues
• Regulation of transporter expression during pregnancy
• Case Studies: Examples of NAFLD/NASH impact on drug pharmacokinetics and disposition

Day 2

In vitro Approaches to Assess Transporter Impact on Drug Disposition

• Assays using immortalized human cells
• Assays using Recombinant System and Membrane Vesicles for kinetics parameters
• “Bottom up” and “top-down” approaches to assess transporter liabilities

In vivo Approaches to Assess Transporter Impact on Drug Disposition

• Renal and biliary recovery and clearance calculation in preclinical species

Introduction to Static and Dynamic Models to Predict Human Hepatic, Renal, and Intestinal Clearance and DDI

• Transporter-enzyme interplay and the extended clearance concepts
• Prediction of hepatic transporter mediated clearance
• Principles of drug-drug interactions
• Extended net effect model to project hepatic transporter-mediated DDI
• Static models to project intestinal transporter-mediated DDI
• Static models to project renal transporter-mediated DDI

Introduction to FDA Guidance on Transporter Mediated DDI

• P-gp and BCRP transporter DDI regulation
• Renal transporter DDI regulation
• Hepatic transporter DDI regulation
• Considerations of other emerging transporters: MATE, MRP2, OAT2 and BSEP
• Clinical Trials for transporter-mediated DDIs: The Principals

Testimonials

2017 Testimonials

• Good course and speakers kept my attention. Materials were good, breaks at appropriate time. Good networking opportunities. Nice receptions and good food. Overall, very well organized. This course was highly recommended to me and I will highly recommended it to others. Excited to be back to work and retrospectively looking at compounds using ECCS classification.
• Loved the real case examples. Great group interactions. New information that people can use away in their projects. Great speakers! I don’t like it, I love it!
• Hands on workshops were great. Everything was really great, one of the best workshops I ever attended. Just the right size.
• The event app was excellent! Thank you for making the notes available online.
• Overall, the course was very informative on the roles and importance of various transporters. This experience has helped to conceptualize particular concepts regarding transporters. I plan on bringing into my research.
• It far exceeded my expectations and was way more than what was advertised! Extremely satisfied. Really loved being here for the workshop.
• The problem solving sessions were the best part for us to synthesize information in a practical way. Realistic DMPK reps face. Great workshop, I learned a lot.
• I enjoyed the integration of the concepts with real data from the in vitro assays. The ability to interact with colleagues in a multi-day event is great for having meaningful discussions and interactions.
• Really loved the course and networking!
• I really enjoyed the group interactions/exercises.
• This conference felt like some very knowledgeable people having productive brainstorming sessions, whereas most conferences feel more like a pageantry. The most interesting, relevant info often came originally from questions and the answers often dove into personal experience, very valuable!
• Enthusiasm of instructors was infectious. Hands-on sessions helped reinforce the concepts. Plating hepatocytes was a good hands-on exercise.
• Wonderful opportunity for students to gain prospective on transporters. Lectures were very informative. Understand more about where the research is going regarding drug disposition.
• Great energy! Met a lot of wonderful people doing exciting work. Enjoyable meeting :-).
• A great overall experience! Very well organized.
• Nicely delivered, well-structured talks. Covered the important topics in the transporter field.
• Thank you for this event, it was very organized and interesting!
• Loved the Whova app, it was organized and helped to put me in the right place at the right time. The speakers were excellent in facilitating discussions!
• Networking and overview were great! Nice updated building and venue.
• Very engaging, practical and promoted in-class discussion.
• Excellent session!
• Very good experience.
• Great experience meeting everyone. The crowd was approachable and friendly, just like a family!
• Great workshop! Learned a lot and met/networked with multiple people!
• The workshop is a really great, touching essence of the advanced level of transporters.
• Appreciate the mix of the intense science + fun! Excellent learning experience. I will pass the info along!
• Great opportunity to network. Great food, literally gained 10 Ibs, it was so good. The cheat sheet list in work book was great, will be easy to follow up with attendees.
• Great course overall. Met a lot of great people and learned a lot!
• I loved the workshop.
• Good organization and great presentations. Very good overview of the transporter field from basics to advanced concepts. Like it.

2016 Testimonials

• The agenda of the course was promising, when I first saw it and signed up. I truly hoped to learn some valuable insight in this field to complement my knowledge. My expectation were blown out of the water! The quality of the material, the instructor’s energy level, and knowledge and the extremely professionally planned/logistics (talks, meals, networking)- just amazing! It really felt like this program has been in existence for 10-15 years…..not just 4 years. So impressive. Best of all, on a personal level, to be here has honestly re-invigorated and inspired me during a time when, progressively, I was beginning to feel “stuck”. This brought the itch back THANK YOU!!
• Very well run and organized… Whoova app is a helpful addition to the meeting. The food was great and facilities were effective/accommodating. Most importantly, the speakers were engaging, collaborative and highly informative.
• Wonderful course! Lots of information and background for a new comer like myself. Course instructors took the extra time to make it friendly, informative, and supportive environment for learning. The opportunities to networking were also great thru class infrastructure and shared meals. I have met many individuals where I would not have otherwise.
• I think this course was really valuable and helps bridge the gab between understanding just the action of a transporter vs the impact in PK and prediction. It is helpful for me as a tool to understanding translational science.
• Compared to last year, the three days schedule is much better since the presentation materials were delivered in schedule that allowed more discussion and more importantly giving the audience the time to digest the information provided.
• Love the Handbook and love the content J.
• You Guys Rock!!! Well Done!
• It was nice to renew concepts I had heard almost but did not have a strong background in. I was able to connect the dots on a few things I am working on.
• Very nicely done.
• Excellent course! Good spirit!
• Great Course! You guys clearly put a lot of work into this. Amazing opportunities to learn the content will recommend. Ayman is the man!
• This was a fantastic workshop, very well organized and presented, educational and intellectually stimulating. I loved the networking opportunities and being able to discuss topics with people from academia/industry backgrounds. Thank you for the shuttle service from hotel to campus and the never ending refershments and meals everyday. It has been exhausting 3 days but well worthwhile. I did not like it, I loved it “Ayman, 2016”.
• Great workshop with wonderful people. Would diligently come back again when I have advanced further.
• Course was excellent. Great mix of high quality lectures with good social interaction opportunities.
• Great workshop I learned a great deal about the influence of PBPK on transporters and DDIs, which before I have limited knowledge.
• Great diverse attendance and excellent opportunity to network. Instructors were engaging. Dinners were above and beyond expectations. Looking forward to attending next year. Content is thorough and conversations are enlightening.
• The demo by Optivia was a great in-lab experience. It would be nice to see different technologies/products and possibly run an assay and generate data in the future (sponsor willing).
• Overall, wonderful conference. I feel like I am going back into the industry with much more knowledge and answers to questions regarding transporters. All of the speakers were great, food, entertainments and accommodation helped make this conference more powerful. Your hard work paid off!
• The workshop continues to improve year after year.
• This is a well organized workshop with a good mix of topics. I like that this is very interactive and give enough time for people to network.
• The course exceeded my expectation especially the ECCS classification is very informative.
• Excellent course that provided a strong prospective of transitions as industry sees them. I also liked the FDA lectures as well. It is great to see a high level transporter course. Thanks for keeping the speakers on time.
• Nice course! Good job! Well organized! Nice atmosphere.
• Excellent course. Presenters were great. Everyone (presenters and others attending) are superfamily. I learned a lot about transporters. Topics were well rounded addressed a lot of different topics that are relevant to transporters.
• Hands on demo was good. Would be more interesting to add hepatocyte isolation and B Clear system.
• Everything was amazing! I will strongly recommend the course to other people to attend!
• Great venue and presenters. It is a focused workshop that offers novies insight from academia, government and industry! The scientist can benefit from more recent applications/breakthroughs as well as providing their unique perspectives to transporter science. Thank you!
• A very special conference. I will continue to recommend to prospective students. We plan to provide continued support.
• This was a great workshop. Appreciated that many topics were covered and they were a variety of attendees.
• The organization was excellent and first class. Keep it up!
• As a business development personnel I don’t typically get so granular to the graphs, formulas, etc. What I have found it helpful is the ECCS model. I do foresee this becoming part of guidance and see great value in my ability to speak fluently about it.
• Great way to gain a strong understanding of the role of transporters in drug disposition and development. Excellent way to network. Hand-on learning tool were good.
• Wonderful speakers, expert participants, sufficient time for questions and highly organized.
• Coming in knowing relatively little (other than a few weeks in integrated pharma sciences) I was able to pick up and apply the concepts pretty fast. The structure worked well to aquaint with the basics and then apply them. I was also able to identify areas I am interested in strengthening my education.
• A really very well organized and enjoyable workshop! The speakers did a great job of engaging with all participants and hands on case study exercises reinforced key teaching points in addition to facilitating networking by acting as icebreakers. It was also great to have ping provide an overview of current FDA positions. Whova app was fun.

2015 Testimonials

• Nice job! I really like the enthusiasm of the presenters. The information covered a wide range of relevant topics, and particularly some potentially very practical and useful classification system.
• This was great! I learned a lot.
• I would highly recommend this course to fellow colleagues. It was extremely thorough.
• Great presentations and great location.
• I found this workshop to be extremely informative and invaluable learning experience. It was great to be able to meet so many experts in both industry & academia.
• Over all good presentation and interaction with attendees. Coming in with little knowledge, I have learned a lot will need some time to digest all information presented.
• Great short conference. Very nice size and interaction space. Very nice work to all presenter. Thank you.
• Excellent course! The content was a perfect mix of background information, scientific knowledge, case studies, and instructor-participant interactions.
• The course was excellent, the speakers were excellent. The materials were great.
• I learnt a lot from all speakers. Thank you for your time!
• A good course- A lot of material so it was a bit rushed but the support material was good
• Great course and instructors!
• This is an excellent workshop. I have learned a lot. Thanks for the tremendous effort and scientific excellence!
• 3rd Annual Conference survey results:
  • 70% of the registrants strongly agree that The course delivered focused high level understanding/predicting drug disposition.
  • 70% of the registrants strongly agree that the course met my expectations based on the material advertised.
  • 77% of the registrants strongly agree that the course instructors were helpful in information regarding drug transporters and contribution of transporters to addressing my questions and comments.

2014 Testimonials

• “Excellent, love the interactions and forcing me to chew materials as it was presented. Enjoyed challenges and questions making this relevant to my world and work situations. Liked the total picture presented on Day 2 and relating it to DMPK concepts.”
• “Excellent course, very helpful for my work like to attend again.”
• “The course covers interesting topics about drug transporters. It covers basic to high level transporters. I might not digested everything (information) but at least, I had an overall understanding about transporters assay and perspectives.”
• “Very well organized settings. Great discussion and direct interactions, great hospitality. Examples were great because they are real compounds from drug discovery/development.”
• “Great Class”
• “Great Workshop”
• “Excellent course and I feel much more comfortable in the area of transporters and DDI. I especially liked the industry focus and applicability of the concepts discussed.”
• “Interactive workshop”
• “The course is very useful. Lots of information and the instructors were funny and helpful! Nice works!
• I am very glad to take this workshop. All the instructors were amazing and worked hard to explain every concept. I totally recommend this wonderful workshop. Thanks”
• “Enjoyed hands on because it forced class to think about information we were learning real time. Instead of just being lectured at. I liked communication type lectures, this kept people engaged in workshop even with sitting for long period of times.”
• “Very intensive training that covers a broad area in transporter.”
• “Instructors are very nice and friendly. Thank you for the workshop.”
• “A good mix between industry and academia”
• “100% of the attendees in the 2013 workshop agreed that he/she would recommend the course to others who want to learn more about transporters”
• “I enjoyed the class a lot. Instructors were excellent communicators. Slides were very clear, materials were presented in a logical sequence.  All instructors were patients with my question despite being at minimal and moderate level”

Registration

The workshop runs from 8 am to 5 pm Monday and Tuesday. Registration includes program materials, refreshments, lunch on Monday and Tuesday, and dinner after a cocktail reception on Monday night. Registrants are encouraged to purchase the book, Transporters in Drug Discovery and Development, 1st Edition/Detailed Concepts and Best Practice, in addition to their registration as part of this course.

Refunds

Registration fee, subject to a $200 processing charge, will be refunded provided written notification of registration cancellation is received July 15, 2019 prior to the seminar.

Payment

Payment via Visa, Master Card, Discover Card, or American Express can be made upon completion of the online registration process. Electronic checks are also accepted. No payments or registrations will be accepted by phone.

Accommodation

3009 Tower Hill Road,
South Kingstown, Rhode Island, 02874, USA

www.HolidayInn.com/SkingstownRI

A special rate of $119 per night plus tax has been arranged (this rate applies for  August 5-August 6, there is also a special rate of $149.00 plus tax available for August 4). Rooms will only be held at this price until June 30, 2019.

Reservations can be made on the phone by using the Group Code PTC with Holiday Inn Reservations www.IHG.com at 800-Holiday or hotel direct at 401-789-1051 or online by clicking here.
 
This cost is not included in the registration fee and each attendee will be responsible for making his/her own accommodation arrangement.

On-campus housing is available for students and can be reserved by sending an email to pharmce@etal.uri.edu. Singles and doubles are available at a rate of $30/$20 per night respectively.

A free van shuttle service will be provided to and from the nearest accommodation hotel, The Holiday Inn of South Kingstown, and the workshop venue, the University of Rhode Island College of Pharmacy. The shuttle service will pick up attendees at the hotel approximately 30 minutes before the workshop starts each morning. The shuttle also brings attendees back to the hotel at the end of each workshop day. Attendees who wish to utilize this shuttle service must contact pharmce@etal.uri.edu and be in the lobby each morning at approximately 7:30 am.

Sponsorship