Podcast
Questions and Answers
What is the purpose of the hit discovery process?
What is the purpose of the hit discovery process?
- To evaluate the safety of a drug candidate
- To synthesize known drugs
- To screen for compounds with the desired activity (correct)
- To develop new therapeutic strategies
Which method is NOT mentioned as part of the hit discovery process?
Which method is NOT mentioned as part of the hit discovery process?
- High-throughput screening
- Computer-aided structure-based drug design
- Natural extracts screening
- Patient-derived testing (correct)
What is a lead compound?
What is a lead compound?
- A chemical compound that has been abandoned
- Any compound that has undergone structural modifications
- A compound that shows minimal therapeutic potential
- A chemical compound that shows promise for treating a disease (correct)
What is the primary focus of lead optimization?
What is the primary focus of lead optimization?
What does SAR stand for in the context of drug development?
What does SAR stand for in the context of drug development?
Which of the following modifications is NOT a systematic approach mentioned?
Which of the following modifications is NOT a systematic approach mentioned?
In the hit discovery process, which screening method allows for the evaluation of many compounds?
In the hit discovery process, which screening method allows for the evaluation of many compounds?
What characterizes a hit compound in drug discovery?
What characterizes a hit compound in drug discovery?
What is one reason why aspirin might lose its potency when stored improperly?
What is one reason why aspirin might lose its potency when stored improperly?
Which of the following composes the basic structure of organic chemistry?
Which of the following composes the basic structure of organic chemistry?
In the context of drug design, what do the terms 'hit' and 'lead' refer to?
In the context of drug design, what do the terms 'hit' and 'lead' refer to?
What is an important aspect of understanding reaction kinetics in chemistry?
What is an important aspect of understanding reaction kinetics in chemistry?
What is the role of enzymes in drug interactions?
What is the role of enzymes in drug interactions?
Which of the following is a key factor influencing drug solubility?
Which of the following is a key factor influencing drug solubility?
Why is thermodynamics important in the study of chemistry?
Why is thermodynamics important in the study of chemistry?
What is the primary goal of in vitro assays conducted during preclinical research?
What is the primary goal of in vitro assays conducted during preclinical research?
What is a practical implication of knowledge in spectroscopy in chemistry?
What is a practical implication of knowledge in spectroscopy in chemistry?
Which of the following accurately describes the purpose of Phase I clinical trials?
Which of the following accurately describes the purpose of Phase I clinical trials?
Which component is NOT part of the in vivo ADME process during drug development?
Which component is NOT part of the in vivo ADME process during drug development?
What is the expected probability of a drug entering Phase II clinical trials?
What is the expected probability of a drug entering Phase II clinical trials?
Which route of administration is NOT mentioned as a method to prevent drug interaction with healthy tissues?
Which route of administration is NOT mentioned as a method to prevent drug interaction with healthy tissues?
What is the primary focus of Phase III clinical trials?
What is the primary focus of Phase III clinical trials?
During preclinical research, lead compounds are tested on which of the following?
During preclinical research, lead compounds are tested on which of the following?
How long does clinical development typically take, from the selection of potential drug candidates to market?
How long does clinical development typically take, from the selection of potential drug candidates to market?
What is the probability of drugs being approved during clinical trials?
What is the probability of drugs being approved during clinical trials?
Which factor is NOT a common reason for failure in clinical trials?
Which factor is NOT a common reason for failure in clinical trials?
Which regulatory agency is responsible for drug approval in the USA?
Which regulatory agency is responsible for drug approval in the USA?
What percentage decline in clinical trial starts was observed in 2023 compared to 2022?
What percentage decline in clinical trial starts was observed in 2023 compared to 2022?
How many novel active substances (NAS) were launched globally in 2023?
How many novel active substances (NAS) were launched globally in 2023?
What was a contributing factor to the decline in clinical trial starts in 2023?
What was a contributing factor to the decline in clinical trial starts in 2023?
Which statement is accurate regarding the approval process for new drugs?
Which statement is accurate regarding the approval process for new drugs?
What aspect of drug development is NOT typically assessed during clinical trials?
What aspect of drug development is NOT typically assessed during clinical trials?
What percentage of new product launches in the past five years were in oncology, neurology, and immunology?
What percentage of new product launches in the past five years were in oncology, neurology, and immunology?
What does the composite success rate in drug R&D indicate for 2023?
What does the composite success rate in drug R&D indicate for 2023?
Which of the following is NOT a category included in infectious diseases treatments mentioned?
Which of the following is NOT a category included in infectious diseases treatments mentioned?
What is the main purpose of post-marketing monitoring?
What is the main purpose of post-marketing monitoring?
How many drugs have been recalled from the market according to the information provided?
How many drugs have been recalled from the market according to the information provided?
During which phase are healthy volunteers assessed for safety and pharmacokinetics?
During which phase are healthy volunteers assessed for safety and pharmacokinetics?
Which substance was noted for causing serious hepatotoxicity leading to liver transplant or death?
Which substance was noted for causing serious hepatotoxicity leading to liver transplant or death?
Which step is part of the correct drug development process sequence?
Which step is part of the correct drug development process sequence?
Flashcards
Pharmaceutical Chemistry
Pharmaceutical Chemistry
A field that deals with the design, development, and production of pharmaceuticals.
Medicinal Chemistry
Medicinal Chemistry
A science that focuses on the discovery, development, and optimization of drugs.
Computer-Aided Drug Design
Computer-Aided Drug Design
A method that utilizes computational techniques to identify potential drug candidates.
Active Small Molecules
Active Small Molecules
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Molecular Modelling
Molecular Modelling
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Flipped Classroom
Flipped Classroom
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Summative Assessment
Summative Assessment
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Formative Assessment
Formative Assessment
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Chemistry in Pharmacy
Chemistry in Pharmacy
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Solubility
Solubility
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Lipophilicity
Lipophilicity
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Organic Chemistry
Organic Chemistry
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Enzymes
Enzymes
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Receptors
Receptors
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Reaction Kinetics
Reaction Kinetics
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Thermodynamics
Thermodynamics
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Hit Compound
Hit Compound
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Screening Assays
Screening Assays
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Hit Discovery
Hit Discovery
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Structure-Activity Relationship (SAR)
Structure-Activity Relationship (SAR)
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Lead Compound
Lead Compound
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Lead Optimization
Lead Optimization
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High-Throughput Screening (HTS)
High-Throughput Screening (HTS)
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Virtual Screening
Virtual Screening
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In vitro Testing
In vitro Testing
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Off-Target Effects
Off-Target Effects
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Pharmacokinetics (PK)
Pharmacokinetics (PK)
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In Vivo Animal Models
In Vivo Animal Models
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Dosage Optimization
Dosage Optimization
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Drug Administration Routes
Drug Administration Routes
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Clinical Trial Phases
Clinical Trial Phases
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Phase III Clinical Trial
Phase III Clinical Trial
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Phase I Trial
Phase I Trial
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Phase II Trial
Phase II Trial
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Phase III Trial
Phase III Trial
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Phase IV Trial
Phase IV Trial
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Drug Failure in Clinical Trials
Drug Failure in Clinical Trials
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Drug Review Process
Drug Review Process
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Probability of Drug Approval
Probability of Drug Approval
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Regulatory Agencies (e.g., FDA, EMA, MHRA)
Regulatory Agencies (e.g., FDA, EMA, MHRA)
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What is Clinical Phase I?
What is Clinical Phase I?
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What is a 'Hit Compound'?
What is a 'Hit Compound'?
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What is Post-Marketing Monitoring (Phase IV)?
What is Post-Marketing Monitoring (Phase IV)?
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What has contributed to the rise in the success rate of drug development?
What has contributed to the rise in the success rate of drug development?
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What is a 'Lead Compound'?
What is a 'Lead Compound'?
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What is 'Structure-Activity Relationship (SAR)'?
What is 'Structure-Activity Relationship (SAR)'?
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What is 'Hit Discovery'?
What is 'Hit Discovery'?
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What are the fastest-growing therapeutic areas for new drug launches in recent years?
What are the fastest-growing therapeutic areas for new drug launches in recent years?
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Study Notes
Drugs and Medicines PMP-102
- The lecture covers the long journey from molecule to medicines.
- The lecturer, Dr. Salvatore Ferla, is associated with Swansea University.
About Myself (Salvo)
- Holds a Master's Degree in Medicinal Chemistry (2008).
- Was a co-supervisor of Pharmaceutical Production (QA, GMP) from 2008-2009.
- Registered as a qualified pharmacist since 2008.
- Earned a PhD in Medicinal Chemistry (2009-2013).
- Worked as a Research Associate in Medicinal Chemistry/Drug Design (2013-2018).
- Worked as a Research Fellow in Medicinal Chemistry/Drug Design (2018-2020).
- Served as a Lecturer in Pharmaceutical Chemistry (2020-2023).
- Became a Senior Lecturer in Pharmaceutical Chemistry (2023-present).
About My Work
- Specialises in Pharmaceutical Chemistry, Organic Chemistry, Medicinal Chemistry, Drug Discovery, and Molecular Modelling.
- Develops computer-aided techniques and organic chemistry methods to identify new small molecules that target biological targets. This includes activities against cancer, viruses, or other targets.
How Will We Learn Together?
- The module uses a flipped classroom model.
- Students review pre-class videos on Canvas.
- Students take formative quizzes on Canvas.
- Students participate in live sessions (F2F or Zoom) for discussions, questions, and answers.
- Students actively participate and prepare for final exams.
What Will We Learn?
- Basic Concepts: Acid/base, pH, solubility, lipophilicity, thermodynamics, reaction kinetics, and practical chemistry.
- Advanced Concepts: Carbon compounds, functional groups, spectroscopy techniques (spectrometry), enzymes, receptors, nucleic acids, other targets, basic drug design, drug-like properties, and hit and lead.
- Organic Chemistry: Focus on organic chemistry concepts relevant to drugs and medicinal chemistry.
- Drugs and Drug Targets: Explore the nature of drugs and their interactions with the body's target molecules.
Why Do We Need to Study Chemistry?
- A patient left an aspirin bottle open in a bathroom cabinet.
- Pharmacist A checked the leaflet, which advised keeping the bottle tightly closed and below 25°C, and instructed the patient to discard the medicine.
- Pharmacist B explained the reason aspirin's instability in the bathroom could lessen its effectiveness.
- Patients reacted differently, one distrustful of the advice, and the other accepting it.
- Illustrates the importance of understanding chemical properties like moisture sensitivity and temperature stability for effective drug use.
Learning Outcomes
- Describe the major components of medicines.
- Discuss the steps involved in the development of a medicine.
- Describe the constituents of medicines.
- Understand the key steps in drug discovery and development.
Do I Know the Answer?
- Questions the student should answer relate to HIT COMPOUND definition, PHASE I CLINICAL PHASE definition, and the correct sequence for DRUG DEVELOPMENT PROCESS.
Drug or Medicine?
- A distinction is made between drugs and medicines, with drugs as chemical substances used for diagnosing, treating, or preventing diseases, while medicines can be considered a delivery system for drugs.
- Examples of drugs include 2-acetoxybenzoic acid, Agumentin, Ketoprofen, Ibuprofen 400mg, and Ampicillin.
Medicines Contain...
- Excipients: These are substances in medicines that are not pharmacologically active but are crucial for medication delivery; these are often chemically inert. These include fillers, binders, disintegrants, glidants, colouring agents, antiadherants, lubricants, coatings, preservatives, etc.
How Long Does It Take?
- Drug development to market typically takes 5 to 20 years.
Drug Development Process
- The process is described through stages: in vitro and in vivo testing, human testing, data review, surveillance, basic/early research, discovery/development, phase I to phase III clinical development, pre-clinical, review, and finally post market monitoring to maintain and monitor safety.
Discovery & Development
- In the past: active ingredients often came from traditional medicines, by chance.
- Now, active compounds are targeted: screening hits, medicinal chemistry, etc.
- Steps describe how new drug targets are found, validated, structure activity relationships (SAR) are established etc.
Preclinical Research
- Lead compounds are tested on non-human subjects to assess safety, toxicity, and pharmacokinetics.
- In vitro models evaluate drug activity and off-target effects.
- In vivo tests involve various animal models studying bioavailability, dosage etc.
- Best dosage is calculated for safety and proper administration routes.
- Appropriate formulation is designed to maximize drug delivery without harming healthy tissues.
Clinical Development
- Clinical trials include healthy and patient volunteers to evaluate safety, efficacy, and optimal dosage.
- Phases I to III describe progress involving dosage ranges, safety checks, and efficacy testing.
- Issues during testing (toxicity, lack of efficacy, drug interactions) can cause trials to be stopped.
Review (Licensing approval)
- Regulators such as FDA, EMA, etc., review clinical trial data and approve or reject a new drug based on approval criteria and evidence.
- Failure rates are high.
Post-Marketing Monitoring (Phase IV)
- Post-approval monitoring addresses ongoing safety issues and potential risks.
- Manufacturers are obligated to continuously review the long-term impact on the human body.
- Safety issues discovered cause drug recalls to prevent adverse consequences.
In Summary...
- The steps in discovering a new drug, testing at different phases, and the required monitoring of the drug after approval are explained.
- The difference between a drug and a medicine is described.
- The importance of chemistry in pharmacy/drugs is highlighted.
Now I know the answer...
- Answers the commonly asked questions about hit compounds (a molecule that shows desired activity), phase I clinical trials (involving roughly 100 healthy volunteers to test safety and pharmacokinetics), and the accurate sequence of drug development stages.
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