Hit-to-Lead & Lead Optimization of Small Molecules and Natural Products
Hit-to-Lead & Lead Optimization of Small Molecules and Natural Products
The Federal Institute for Drugs and Medical Devices (BfArM) offers a workshop in digital format on five Wednesdays in November/December 2020 from 15:00-17:00.
The workshop addresses scientists (mainly post-docs and PhD students) of DZIF projects in the early product development phase. The presentations will be given by experts from academia, industry and regulatory authorities.
Please send your registrations, stating your DZIF project number, by 30.09.2020 to:
Schedule
04.11.2020
Lead Structure & Lead Optimization
Martin Empting (HIPS, Saarbrücken)
Fundamental criteria for LO – drug activity, cytotoxicity and solubility:
• Target Product Profile (TPP)
• Example and case studies how to make analogous more effective and safer
• Discussion and Questions
Success Story
Holger Zimmermann,Tamara Pfaff (AiCuris, Wuppertal)
From hit to market authorization: AIC246 – Letermovir (with focus on early pre-clinical development)
11.11.2020
In vivo PK/PD
Pia Empting (Goethe-University Frankfurt)
Veterinary medicine/ laboratory animal science:
• Animal models/ animal testing
• Microbiological/ histological sample evaluation
• Ethics
Katharina Rox (HZI, Braunschweig)
In vivo efficacy & in vitro safety – single and repeat dose to confirm in vivo pharmacologic effects:
• PK/PD Unit at the HZI
• in vitro safety
• Metabolite ID
• in vivo genotoxicity
18.11.2020
Biological Assays, in vitro ADME
Jennifer Herrmann (HIPS, Saarbrücken)
Basics in vitro Biology – microbiological potency of drug:
• Structure Activity Relationship (SAR)
• Target Identification
• Activity testing (in vitro MICs)
• Resistance development/ frequency of resistance
• Mechanism of resistance
• Examples and case study
Ken Page (Cyprotex, UK)
In vitro ADME – suitable availability of drug:
• Basics & Terminology
• Interpretation of data
25.11.2020
Entrepreneurs in AMR
Marc Creus (University Basel; Juvabis AG)
Current needs and prospects for antibiotics R&D
Technology Transfer
Kordula Kruber (Provendis, Mülheim)
From research to marketable products:
• Invention or discovery?
• Patents & other IP
• Options/chances for commercialisation
• Timelines & pitfalls
• Licensing & cooperations
02.12.2020
Regulatory guidance during LO and preclinical stage
BfArM (Bonn)
Excursion through relevant guidelines:
• What information/data are necessary in the different development stages
Federal Institute for Drugs and Medical Devices (BfArM)
Weekly webinar
Germany