SubjectsSubjects(version: 847)
Course, academic year 2018/2019
  
Trends in Drug Research and Development - N111045
Title in English: Výzkum a vývoj léčiv
Guaranteed by: Department of Organic Technology (111)
Actual: from 2013 to 2018
Semester: summer
Points: summer s.:3
E-Credits: summer s.:3
Examination process: summer s.:
Hours per week, examination: summer s.:2/0 C+Ex [hours/week]
Capacity: 178 / unknown (unknown)
Min. number of students: unlimited
Language: Czech
Teaching methods: full-time
Level:  
For type:  
Note: course can be enrolled in outside the study plan
enabled for web enrollment
Guarantor: Zbytovská Jarmila doc.Mgr. Dr.rer.nat.
This subject contains the following additional online materials
Annotation -
Last update: TAJ111 (30.08.2013)
The subject presents the particular periods of the drug discovery process from searching for active structures to clinical testing. It describes the basic stages of a drug's life inside the organism (the LADME model) and relationships between its structure and activity (QSAR). The drug's physical-chemical properties and their parameterisation are also discussed.
Aim of the course -
Last update: TAJ111 (30.08.2013)

Students will be able to:

  • understand issues of the structure-activity relationships of drugs
  • apply the basic QSAR principles
  • characterise drug's life inside the organism using enlarged knowledge in pharmacokinetics
  • understand issues of drug discovery

Literature -
Last update: TAJ111 (30.08.2013)

R: Kuchař M.: Výzkum a vývoj léčiv. Vydavatelství VŠCHT Praha, 2008. ISBN 978-80-7080-677-7

A: Tsaioun K., Kates S.: ADMET for Medicinal Chemists: A Practical Guide. Wiley 2011. ISBN 978-0470484074

A: Hartl J., Palát K.: Farmaceutická chemie I. Karolinum 2011. ISBN 978-80-246-2033-6

A: Smith D. van den Waterbeemd H., Walker D.: Pharmacokinetics and metabolism in drug design. Wiley 2006. ISBN 3-527-31368

Learning resources -
Last update: TAJ111 (30.08.2013)

Learning materials distributed by lecturer

Syllabus
Last update: TAJ111 (30.08.2013)

1. Relationships between structure and biological activity of drugs, historical view, basic principles.

2. The particular periods of the drug discovery process, preclinical and clinical testing.

3. Current trends in drug discovery, biotechnology, management of drug research and development.

4. Development of generic drugs, relationships between original and generic companies.

5. The LADME model, pharmacokinetics.

6. Intramolecular interactions, drugs´ physical-chemical properties and their parametrization.

7. Electron parameters, Hammett polar constants, molar refraction.

8. Lipophilic parameters, fragment constants, substituent parameters, chromatographic values and lipophilicity.

9. Molecular topology, connectivity and flexibility indices.

10. Interpretation of regression relationships, dependent and independent variables, collienarity of parameters, selection of structure changes.

11. Practical impacts of QSAR.

12. Relationships between chirality and biological activity.

13. Current QSAR approaches, the CoMFA method, similarity models, lead structures identification, molecular modelling.

14. Economic issues of drug research and development, minimization of risk factors.

Registration requirements
Last update: TAJ111 (30.08.2013)

Pharmacology I, Introduction into Chemistry of Pharmaceuticals

Teaching methods
Activity Credits Hours
Účast na přednáškách 1 28
Příprava na přednášky, semináře, laboratoře, exkurzi nebo praxi 1 28
Příprava na zkoušku a její absolvování 1 28
3 / 3 84 / 84
Coursework assessment
Form Significance
Regular attendance 20
Examination test 80

 
VŠCHT Praha