Innovatieproject Geneesmiddelen

• What is intravenous medication?

  Medication delivered directly into a vein.
• How long does it take to bring a new drug on the market?

  10-15 years
• How many new drugs are brought on the market each year?

  20-50 new drugs are brought on the market each year
• how many FDA approved drugs are there currently?

  1500+ approved drugs
• How much does a new drug cost?

  around 1,5 miljard dollar
• How many of the drugs are biologicals and how many are small molecules?

  80% is biologicals and 20% is small molecules
• How are drugs classified?

  Drugs are classified by their biological effect, chemical structure and target system
• What happens in progeria disease?

  An genetic abnormality leads to proteins not being broke down well, which causes the cell nucleus to deform. This happens to 1 in 4 million children.
• What happens in ‘sleeping sickness’?

  protozoal parasites called Trypanosoma brucei are transmitted by the tsetse fly. The gambiense tsetse fly leads to chronic disease and progresses during 1-2 years, this is 95% of the cases. Rhodesiene tsetse fly leads to acute disease and kills within weeks. There are 1500 reported cases per year. Mostly in Congo, South Sudan, Uganda and Angola.
• What did Claude Bernard study?

  he studies how signal flowbetween nerve and muscle cells using frog limbs and with the use of plant extract. Acetylcholine is an agonist which causes contraction of the muscle. Curare is an antagonist which binds with the acetylcholine receptor and leads to paralysation.
• Robert J. Lefkowitz and Brian K. Kobilka won a nobel prise for?

  in 2012 they won a nobel prize for the first crystal structure of a GPCR. Adrenaline causes fight-or-flight response, however noradrenaline acts as an endogenous agonist at its GPCR.
• What do beta2 antagonists fight against?

  high blood pressure
• What is oral medication?

  Medication taken by mouth.
• What is inhalation medication?

  Medication that is inhaled into the lungs.
• What is transdermal medication?

  Medication that is absorbed through the skin into the bloodstream.
• What is subcutaan medication?

  Medication administered into the layer of tissue just beneath the skin.
• What is intramusculair medication?

  Medication injected directly into the muscle tissue.
• What influences the form of indulgence?

  type of medicine, form of therapy and the patient’s convenience
• How does drug metabolism by CYP450 work?

  Enzymatic oxidation and reduction reactions. it’s an enzyme family of 57 members. Metabolizes endogenous and exogenous compounds. Allows the body to excrete xenobiotics by making them more polar.
• what does MEC stand for and what is the therapeutic window?

  MEC stands for Minimum Effective Concentration. The therapeutic window refers to the range of drug concentrations in the body that produce the desired therapeutic effect without causing significant toxicity.
• What is meant by ‘on-target’?

  Hitting the intended target.
• What is meant by ‘off-target’?

  Not hitting the intended target.
• What is in vivo testing?

  Testing conducted on living organisms.
• What is in vitro testing?

  Testing conducted outside of a living organism, typically in a laboratory setting.
• What is in silico testing?

  Computer-based simulation or modeling of biological, chemical, or physical processes to predict outcomes or test hypotheses.
• How do you validate a drug target?


  you have to demonstrate that the target is valid. First you need to develop an assay to determine compounds that interact with your target and the check the ADMET properties. The better the validation, the lower the risk in advancing a project.
• What do histamine receptors do?


  Histamine receptors mediate the effects of histamine, a chemical involved in allergic reactions, inflammation, and neurotransmission. There is secretion of gastric acid here, this is treatable with metiamide, but this is toxic to blood cells.
• What does the H4 receptor do?

  The H4 receptor is involved in regulating immune responses and inflammation.
• What are the benefits of small molecule drugs?

  Target specificity, oral administration, ease of synthesis, and ability to penetrate cell membranes.
• What are the benefits of biologicals?

  Improved crop yield and quality, reduced reliance on chemical pesticides, and enhanced soil health and biodiversity. However they are not easy to administer, they do not penetrate the cell membranes and they are expensive to make.
• What is an assay?

  A test or analysis to determine the composition or quality of a substance.
• What are the modern assay systems?

  biochemical pathway assays (binding of molecules or enzyme functions) and cell based assays (Signaling event).
• What are the assay requirements?

  pharmacological relevance, reproducible over time, costs should be reasonable, large signal to noise ratio and DMSO tolerant.
• What is a hit?

  A hit refers to a successful connection or interaction with a target or object.
• What is High-throughput scresning?

  A method for quickly and efficiently testing a large number of samples or compounds in a short amount of time. This happens robotically and uses both assays. This is expensiveand time consuming.
• What are focused libraries in drug discovery?

  Libraries containing compounds with specific structural features or properties that are designed to target a particular biological target or pathway in drug discovery. This is chemically diverse.
• what is virtual screening?

  Process of using computer algorithms to identify potential drug candidates by screening large databases of compounds. Large databases.
• What is hit validation?

  Hit validation is the process of confirming the accuracy or success of a hit in a scientific experiment or analysis.
• What is hit-to-lead?

  The process of identifying a promising compound that can be further developed into a drug.
• What is lead identification?

  A hit that has been validated that is being tested to determine whether it can become a drug.