Introduction to Drug Discovery and Development
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Which enantiomer is known to have calming and sleep-inducing properties in pregnant women?

  • Both R- and S-enantiomers
  • S-enantiomer only
  • Neither R- nor S-enantiomers
  • R-enantiomer only (correct)
  • What is a known effect of the S-enantiomer in the context of pregnancy?

  • Accelerates embryo development
  • Induces sleep in the mother
  • Promotes weight gain
  • Causes teratogenic effects (correct)
  • What could potentially happen if the blood supply to the embryo's limbs is strangulated?

  • Normal development of limbs
  • Improved motor skills in the embryo
  • Enhanced limb growth
  • Severe complications and deformities (correct)
  • In the treatment of morning sickness, which enantiomer should be avoided due to its teratogenic effects?

    <p>S-enantiomer should be avoided</p> Signup and view all the answers

    What aspect of medication for pregnant women is particularly important concerning the R- and S-enantiomers?

    <p>The specific enantiomer's properties</p> Signup and view all the answers

    Which step in the drug discovery process involves determining if a target is critical for treatment through biological assays?

    <p>Target Validation</p> Signup and view all the answers

    What is described as a structure which shows a useful pharmacological activity and can serve as the starting point for drug design?

    <p>Lead Compound</p> Signup and view all the answers

    Which technique is NOT explicitly mentioned as part of lead identification in drug discovery?

    <p>Discovering biological targets</p> Signup and view all the answers

    What does SAR studies primarily focus on in drug development?

    <p>Analyzing the relationship between chemical structure and biological activity</p> Signup and view all the answers

    Which process would most likely involve computational methods in drug design?

    <p>3-D Structure Based Drug Design</p> Signup and view all the answers

    What is the main purpose of pharmacogenomics in the context of drug discovery?

    <p>To understand genetic variations in drug response</p> Signup and view all the answers

    In which stage are new compounds designed and synthesized within the drug discovery process?

    <p>Combinatorial Chemistry</p> Signup and view all the answers

    What is the estimated cost of bringing a new drug to market according to the 2014 Tufts study?

    <p>$2.6 billion</p> Signup and view all the answers

    Which of the following estimates represents the cost of drug development from preclinical to marketing as reported by Bain & Co. in 2003?

    <p>$1.7 billion</p> Signup and view all the answers

    What is the average time taken to develop a new drug?

    <p>12</p> Signup and view all the answers

    In what year did Tufts University report a drug development cost estimate of $230 million?

    <p>1987</p> Signup and view all the answers

    Which estimate includes post-approval research and development costs?

    <p>$897 million</p> Signup and view all the answers

    Which study from Tufts University provides the highest cost estimate for drug development?

    <p>2014</p> Signup and view all the answers

    What was the cost estimate for drug development in 2001 from Tufts University?

    <p>$802 million</p> Signup and view all the answers

    Which of the following is NOT a cited cost estimate for drug development?

    <p>$800 million</p> Signup and view all the answers

    What is the risk associated with drug development as indicated in the content?

    <p>It is a high risk business.</p> Signup and view all the answers

    How many compounds out of every 10,000 synthesized will typically reach clinical testing?

    <p>5</p> Signup and view all the answers

    What percentage of drugs is derived from natural sources?

    <p>50%</p> Signup and view all the answers

    Which source contributes the most to the natural supply of drugs?

    <p>Plants</p> Signup and view all the answers

    What fraction of synthesized compounds will ultimately reach the marketplace?

    <p>1 out of 10,000</p> Signup and view all the answers

    Which of the following is not a natural source of drugs?

    <p>Chemical Synthesis</p> Signup and view all the answers

    What percentage of drugs comes from microorganisms?

    <p>12%</p> Signup and view all the answers

    In the context of drug discovery, what is the correct sequence from synthesis to market?

    <p>Synthesis → Animal Testing → Clinical Testing → Market</p> Signup and view all the answers

    How many compounds typically reach animal testing out of every 5,000 to 10,000 synthesized?

    <p>250</p> Signup and view all the answers

    What is thalidomide known for in the context of drug discovery?

    <p>Having a mixture of optical isomers</p> Signup and view all the answers

    Which of the following sources contributes the least percentage to the total derived from natural sources?

    <p>Animals</p> Signup and view all the answers

    What type of mixture was thalidomide originally used as?

    <p>A racemate</p> Signup and view all the answers

    Which enantiomer of thalidomide is associated with sedative and sleep-enhancing properties?

    <p>S-enantiomer</p> Signup and view all the answers

    What is the effect associated with the R-enantiomer of thalidomide?

    <p>Leads to limb malformations</p> Signup and view all the answers

    Thalidomide's impact on fetal development primarily results from which mechanism?

    <p>Inhibition of blood supply</p> Signup and view all the answers

    Which statement correctly describes the chiral nature of thalidomide?

    <p>It consists of equal proportions of two enantiomers.</p> Signup and view all the answers

    What potential effect does the S-enantiomer of thalidomide avoid in pregnant women?

    <p>Congenital limb defects</p> Signup and view all the answers

    Why was thalidomide initially prescribed to pregnant women?

    <p>To relieve morning sickness</p> Signup and view all the answers

    Which consequence is primarily linked to the use of the R-enantiomer of thalidomide during pregnancy?

    <p>Limb malformations</p> Signup and view all the answers

    What property does the S-enantiomer of thalidomide have that the R-enantiomer does not?

    <p>Sedative effects</p> Signup and view all the answers

    The classification of thalidomide as a drug with a chiral center indicates what about its structure?

    <p>It can exist in multiple forms with distinct properties.</p> Signup and view all the answers

    Study Notes

    Introduction to Drug Discovery and Development

    • Drug discovery and development is a high-risk, complex process
    • It takes an estimated 12 years
    • Several factors affect the process from synthesis to marketing

    Drug Discovery and Development Process

    • Target Identification: Finding the specific biological target (protein) that the drug should interact with
    • Target Validation: Checking if the identified target is crucial in the disease
    • Target + Ligand: Combining the target and potential drug substance (ligand) – involves protein-ligand interaction techniques
    • Lead Identification: Finding a molecule (lead compound) that has a useful effect
    • Lead Optimization: Modifying a lead compound to improve its properties
    • Drug Candidate: Refining compounds from lead optimization to a stage suitable for preclinical studies
    • Preclinical Studies: Animal pharmacology, pharmacokinetics, safety studies
    • Clinical Trials: Phase I (healthy volunteers), Phase II (patients), Phase III (large groups of patients)
    • New Drug Application: Submitting necessary documentation for approval
    • Post Marketing Surveillance: Continued monitoring after drug launch

    Drug Development Costs

    • Drug development costs vary but can be substantial - ranging from hundreds of millions to billions of dollars.
    • Example figures given: 230million,230 million, 230million,2.6 billion

    Sources of Drugs

    • Natural Sources (50%): Plants, animals, minerals, microorganisms
    • Chemical Synthesis (50%)

    Thalidomide

    • Racemate of R- and S-thalidomide isomers: one form is calming and sleep-inducing while the other causes birth defects.
    • Initial use: Morning sickness treatment in pregnant women
    • Side effects: Teratogenic effects (leading to birth defects)
    • Potential cancer treatment: Anti-angiogenic effects inhibit tumor growth.
    • Also used to treat HIV and leprosy

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    Description

    This quiz explores the intricate process of drug discovery and development, which typically spans over 12 years. It covers essential stages such as target identification, lead optimization, and clinical trials. Test your understanding of the steps involved in bringing a drug from conception to market.

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