1. Pipeline for the Development of Novel Drugs

2. Ústí nad Labem
Ostrava
Prague
Pardubice
Brno

3. HEALTH ENVIRONMENT BioMed Research UH FVZ UHK Faf LFHK
University Hospital HK
BioMed
Research UH
FVZ
UHK
Faf
LFHK
Faculty of Military Health Sciences
Faculty of Medicine
Pharmaceutical Faculty
Faculty of Science and Faculty of Informatics and Management UHK

4. 2011
2016
7 researchers / 3.2 FTE
64 researchers / 17 FTE
2 institutes
(UHHK, FMHS)
4 institutes
(UHHK, FMHS, UHK, IMH) -
19 national projects
2 mil CZK
22 mil CZK
8 articles
62 IF articles
6 patents

5. OUR GROUP University Hospital Hradec Kralove
Biomedical Research Center
University of Defense
Faculty of Military Health Science
Department of Toxicology and Military Pharmacy
University of Hradec Kralove
Faculty of Science – Department of Chemistry; Department of Biology
Faculty of Informatics and Management - Center for Basic and Applied Science
National Institute of Mental Health
Laboratory of Chemistry
- Over 60 people in total

6. AIMS
Basic research (own drug development, medical devices, proteomics as diagnostic)
Applied research (service for the clinics and private sector e.g. proteomics, pharmacokinetics od drugs etc.)
Education and self-development (pre and postgraduated students, internships, seminars)

7. INTERNATIONAL COOPERATION
Canada
USA
Brazil
Croatia
Sweden
France
Germany
Serbia
Hungary
Korea
Singapore
India
UAE UK
Italy
Slovakia
Over 40 IF papers per year
(2013 – 42 IF; 2014 – 46 IF; 2015 – 46 IF; 2016 – 48 IF)

8. Pipeline

9. In vitro biologial assessment In vivo assesment, toxicity
FIELDS OF EXPERTISE
Představení proteomické skupiny Centra Biomedicínského Výzkumu
2) Proteomics
3) Medical devices
1) Drug Development:
Chemical synthesis
In vitro biologial assessment
In vivo assesment, toxicity
Pharmacokinetics
Pharmacodynamics

10. DRUG DEVELOPMENT PROCESS
In silico methods, organic synthesis
Design and Synthesis
In-vitro evaluation
1st selection
Toxicity
Pharmacokinetics
2nd selection
In-vivo
Candidate
„Drug candidate “- recommendation for preclinical trials, commercialization, ip protection
Pipeline: reactivators, radioprotectives, vaccine adjuvans,
decontamination & desinfection, Alzheimer’s drugs, antitumor drugs

11. VIRTUAL SCREENING, MOLECULAR MODELING
Enzyme known structure (enzym, receptor)- RTG;
docking of drug candidates into the enzyme cavity

12. Multi-Target Directed Ligands
CHEMICAL SYNTHESIS
Multi-Target Directed Ligands
Alzheimer‘s disease
ABAD

13. PHYSICO-CHEMICAL PROPERTIES
Assessment:
Solubility
log P/log D
pKa
Metabolites: in vitro prediction
BBB prediction: PAMPA assay
phospholipid layer (fast)
CaCo-2 cell line (more precise)
PAMPA assay

14. IN VITRO SCREENING Efficacy on selected target: Fast Simple Economy
Availability:
Physico-chemical properties
BBB penetration
Metabolization
Safety:
Cytotoxicity evaluation

15. TOXICITY Acute toxicity (MTD, LD50) Sub-acute toxicity (28 days)
Chronic toxicity (90 days)
i.m., i.v., i.p., p.o., s.c. administration
Mice, rats, pig, guinea pig, dog

16. PHARMACOKINETICS Assesment of promising candidates
Plasma or tissue levels
T1/2, bioavalability, clearence
Organe distribution
Blood-brain barrier penetration

17. PHARMACODYNAMICS IN VIVO
ACETYLCHOLINESTERASE REACTIVATORS (In house)
RADIOPROTECTIVES
(In house)
ANTICANCER DRUGS
(Medical faculty UK)
ALZHEIMER‘S DISEASE
(AS Prague)
DECONTAMINATION AND DESINFECTION
ADJUVANS
(In house, Slovak republic)
MEDICAL DEVICES

18. Patents Derivativesof benzothiazolylurea, preparation and their use
- Patent (PV )
14-merkaptotetradecyl)-trimethylammonium-bromide, as surfactant for gold nanorods
- Patent (PV )
Quaternary ammonium salt, desinfection mixtures and their use
- Patent (PV )
Desinfectionmixtures with quaternary ammonium salts
- Patent (PUV )