Human microtracer studies in drug development: How, when and why

Purpose of the symposium

We welcome interested pharma companies that want to know more about, or that are considering the use of microtracers in drug development programmes.

Both the clinic of ICON as well as the AMS laboratory of TNO have conducted a large number of microtracer studies during the last 10 years. The increased interest in microtracer studies triggered ICON and TNO to organise this one-day symposium to share experiences, to discuss hurdles and challenges.

Programme and speakers

(Please note: registration for this event is closed)

The symposium starts at 9 a.m. and ends at 5 p.m. with drinks and bites.

The programme consist of two main sessions:

1. In the morning session we will be focused on 14C-materials and GMP requirements.
2. In the afternoon session several pharmaceutical companies will share their microtracer study designs and experiences. Among confirmed speakers are leading human ADME scientists of GSK, Roche, Boehringer Ingelheim, BMS, PTC Therapeutics, and Pfizer.

See full programme

Speakers

• Esther van Duijn, PhD – TNO (view LinkedIn profile)
• Arjen Akkerman, MSc, PharmD - ICON (view LinkedIn profile)
• Ralf Kiesling, BSc, PharmD – Boehringer Ingelheim Pharma GmbH & Co.KG (view LinkedIn profile)
• Prof. Harry Hendrikse, PhD - Amsterdam UMC (view LinkedIn profile)
• Dr. Wouter Vaes, PhD - TNO (view LinkedIn profile)
• Graeme Young, PhD - GSK (view LinkedIn profile)
• Bianca van Groen, PhD - Roche Pharma (view LinkedIn profile)
• Xiaomin Wang, PhD - BMS (view LinkedIn profile)
• Stefan Blech, PhD - Boehringer-Ingelheim Pharma GmbH Co. KG (view LinkedIn profile)
• Ron Kong, PhD – PTC Therapeutics, Inc (view LinkedIn profile)
• Doug Spracklin, PhD - Pfizer (view LinkedIn profile)

Advantages of using microtracer studies

Microtracer studies have found broad application in early clinical drug development over the past ten years. Especially human ADME and Absolute Bioavailability (ABA) single-arm microtracer studies have found traction among both large and smaller sized pharmaceutical companies.

The discriminating factor of microtracer studies is mainly the use of very small amounts of the radioactive tracer material, while the cold dose remains at a therapeutic level.

The advantages can be summarized as:

• Elimination of animal (QWBA) dosimetry studies
• The use of fit-for-purpose 14C-material GMP approaches.
• The early availability of human metabolite profiles with the consequent elimination of radioactive animal and late stage human ADME studies.
• No necessity to generate intravenous toxicology data for the ABA study because the intravenous microtracer dose is only a small fraction compared to the concomitant therapeutic level oral dose.

Microdosing Network meeting

On April 22nd, a meeting of the International Phase-0 Microdosing Network will be held at the same location, Fletcher Hotel Leiden. The meeting will cover Phase 0 approaches in the broadest sense and is led by Tal Burt. Registration for this Phase 0 meeting is through the Tal Burt Network directly.

Location

The symposium will be held in the Fletcher Hotel Leiden, in the Netherlands.

Fletcher Wellness-Hotel Leiden
Bargelaan 180
2333 CW Leiden

More information and travel options can be found on the Fletcher Wellness-Hotel Leiden website.

Full programme Microtracer Symposium

Morning session: GMP / Non-GMP

• 09.25 - 09.30: “Opening and welcome” Esther van Duijn, PhD – TNO
• 09.30 - 09.50: "Manufacturing of Microtracer IMP’s under GMP" Arjen Akkerman, MSc, PharmD - ICON
• 10.00 - 10.20: “Providing 14C API for hADME – from the point of view of the Isotope Chemistry” Ralf Kiesling, BSc, PharmD – Boehringer Ingelheim Pharma GmbH & Co.KG
• 10.30 - 11.00: Break
• 11.00 - 11.20: "Microtracer studies: what is needed?" Prof. Harry Hendrikse, PhD - Amsterdam UMC (location VUmc)
• 11.30 - 11.50: "Can Threshold of Toxicological Concern (TTC) principles be helpful to assess the quality of 14C-drug substance in microtracer studies" Dr. Wouter Vaes, PhD - TNO
• 12.15 - 13.00: Lunch

Afternoon session Clinical Microtracer Studies

• 13.00 - 13.20: "The human ADME paradigm shift(s)* and a summary of GSK experiences [* on behalf of the EFPIA DMPK Network working group]" Graeme Young, PhD - GSK
• 13.30 - 13.50: “Pediatric [14C]microtracer studies - innovative approach to study metabolite profiles and mass balance in this vulnerable population” Bianca van Groen, PhD - Roche Pharma
• 14.00 - 14.20: “Bioanalytical perspectives for supporting microtracer clinical studies” Xiaomin Wang, PhD - BMS
• 14.30 - 15.00: Break
• 15.00 - 15.20: “Microtracer Studies @ Boehringer-Ingelheim; current approaches and future perspectives” Dr. Stefan Blech, PhD; - Boehringer-Ingelheim Pharma GmbH Co. KG
• 15.30 - 15.50: “Combination of microtracer and regular radioactivity doses – an approach to investigating emvododstat ADME in human” Ron Kong, PhD – PTC Therapeutics, Inc
• 16.00 - 16.20: “The AMS-enabled Human Absorption, Distribution, Metabolism & Excretion (hADME) Study: A Technological and Strategic Paradigm Shift” Doug Spracklin, PhD - Pfizer

16.30 - 17.00: Discussion time

17.00 -18.30: Wrap up, drinks & bites