Podcast
Questions and Answers
Which enantiomer is known to have calming and sleep-inducing properties in pregnant women?
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?
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?
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?
In the treatment of morning sickness, which enantiomer should be avoided due to its teratogenic effects?
What aspect of medication for pregnant women is particularly important concerning the R- and S-enantiomers?
What aspect of medication for pregnant women is particularly important concerning the R- and S-enantiomers?
Which step in the drug discovery process involves determining if a target is critical for treatment through biological assays?
Which step in the drug discovery process involves determining if a target is critical for treatment through biological assays?
What is described as a structure which shows a useful pharmacological activity and can serve as the starting point for drug design?
What is described as a structure which shows a useful pharmacological activity and can serve as the starting point for drug design?
Which technique is NOT explicitly mentioned as part of lead identification in drug discovery?
Which technique is NOT explicitly mentioned as part of lead identification in drug discovery?
What does SAR studies primarily focus on in drug development?
What does SAR studies primarily focus on in drug development?
Which process would most likely involve computational methods in drug design?
Which process would most likely involve computational methods in drug design?
What is the main purpose of pharmacogenomics in the context of drug discovery?
What is the main purpose of pharmacogenomics in the context of drug discovery?
In which stage are new compounds designed and synthesized within the drug discovery process?
In which stage are new compounds designed and synthesized within the drug discovery process?
What is the estimated cost of bringing a new drug to market according to the 2014 Tufts study?
What is the estimated cost of bringing a new drug to market according to the 2014 Tufts study?
Which of the following estimates represents the cost of drug development from preclinical to marketing as reported by Bain & Co. in 2003?
Which of the following estimates represents the cost of drug development from preclinical to marketing as reported by Bain & Co. in 2003?
What is the average time taken to develop a new drug?
What is the average time taken to develop a new drug?
In what year did Tufts University report a drug development cost estimate of $230 million?
In what year did Tufts University report a drug development cost estimate of $230 million?
Which estimate includes post-approval research and development costs?
Which estimate includes post-approval research and development costs?
Which study from Tufts University provides the highest cost estimate for drug development?
Which study from Tufts University provides the highest cost estimate for drug development?
What was the cost estimate for drug development in 2001 from Tufts University?
What was the cost estimate for drug development in 2001 from Tufts University?
Which of the following is NOT a cited cost estimate for drug development?
Which of the following is NOT a cited cost estimate for drug development?
What is the risk associated with drug development as indicated in the content?
What is the risk associated with drug development as indicated in the content?
How many compounds out of every 10,000 synthesized will typically reach clinical testing?
How many compounds out of every 10,000 synthesized will typically reach clinical testing?
What percentage of drugs is derived from natural sources?
What percentage of drugs is derived from natural sources?
Which source contributes the most to the natural supply of drugs?
Which source contributes the most to the natural supply of drugs?
What fraction of synthesized compounds will ultimately reach the marketplace?
What fraction of synthesized compounds will ultimately reach the marketplace?
Which of the following is not a natural source of drugs?
Which of the following is not a natural source of drugs?
What percentage of drugs comes from microorganisms?
What percentage of drugs comes from microorganisms?
In the context of drug discovery, what is the correct sequence from synthesis to market?
In the context of drug discovery, what is the correct sequence from synthesis to market?
How many compounds typically reach animal testing out of every 5,000 to 10,000 synthesized?
How many compounds typically reach animal testing out of every 5,000 to 10,000 synthesized?
What is thalidomide known for in the context of drug discovery?
What is thalidomide known for in the context of drug discovery?
Which of the following sources contributes the least percentage to the total derived from natural sources?
Which of the following sources contributes the least percentage to the total derived from natural sources?
What type of mixture was thalidomide originally used as?
What type of mixture was thalidomide originally used as?
Which enantiomer of thalidomide is associated with sedative and sleep-enhancing properties?
Which enantiomer of thalidomide is associated with sedative and sleep-enhancing properties?
What is the effect associated with the R-enantiomer of thalidomide?
What is the effect associated with the R-enantiomer of thalidomide?
Thalidomide's impact on fetal development primarily results from which mechanism?
Thalidomide's impact on fetal development primarily results from which mechanism?
Which statement correctly describes the chiral nature of thalidomide?
Which statement correctly describes the chiral nature of thalidomide?
What potential effect does the S-enantiomer of thalidomide avoid in pregnant women?
What potential effect does the S-enantiomer of thalidomide avoid in pregnant women?
Why was thalidomide initially prescribed to pregnant women?
Why was thalidomide initially prescribed to pregnant women?
Which consequence is primarily linked to the use of the R-enantiomer of thalidomide during pregnancy?
Which consequence is primarily linked to the use of the R-enantiomer of thalidomide during pregnancy?
What property does the S-enantiomer of thalidomide have that the R-enantiomer does not?
What property does the S-enantiomer of thalidomide have that the R-enantiomer does not?
The classification of thalidomide as a drug with a chiral center indicates what about its structure?
The classification of thalidomide as a drug with a chiral center indicates what about its structure?
Flashcards
Target Identification
Target Identification
The process of finding a biological target (e.g., protein) that is involved in a disease.
Cost of Drug Development
Cost of Drug Development
The estimated cost of bringing a new drug from preclinical development to the market.
Estimated cost (1987)
Estimated cost (1987)
230 million dollars
Target Validation
Target Validation
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Lead Compound Identification
Lead Compound Identification
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Estimated cost (2001)
Estimated cost (2001)
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Structure-based drug design
Structure-based drug design
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Estimated cost (2003)
Estimated cost (2003)
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Combinatorial chemistry
Combinatorial chemistry
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Estimated cost (2003, Bain & Co.)
Estimated cost (2003, Bain & Co.)
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Estimated cost (2014)
Estimated cost (2014)
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Lead Identification
Lead Identification
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Lead Optimization
Lead Optimization
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Average development time
Average development time
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Drug Development Risk
Drug Development Risk
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Drug Development Success Rate
Drug Development Success Rate
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Drug Sources
Drug Sources
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Natural Drug Sources
Natural Drug Sources
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Chemical Synthesis Sources
Chemical Synthesis Sources
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Thalidomide Example
Thalidomide Example
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Thalidomide's chiral centre
Thalidomide's chiral centre
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Racemate of Thalidomide
Racemate of Thalidomide
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R-enantiomer of Thalidomide
R-enantiomer of Thalidomide
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S-enantiomer of Thalidomide
S-enantiomer of Thalidomide
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Thalidomide and pregnancy
Thalidomide and pregnancy
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Morning sickness remedy
Morning sickness remedy
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Enantiomer difference
Enantiomer difference
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Limb development harm
Limb development harm
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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.
