Drug Discovery Module 2

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Questions and Answers

What is the main task when working with therapeutic antibodies in drug discovery?

Designing complex synthetic molecules

Choosing the appropriate molecular target in advance (correct)

Identifying potential side effects of the antibodies

Sourcing compounds from remote locations

Which of the following drugs is derived from natural products?

Aspirin

Ciclosporin (correct)

Paracetamol

Ibuprofen

What is one of the main causes of project failure in drug discovery?

Inability to predict therapeutic efficacy (correct)

Limited access to technological resources

Insufficient funding for research

Complications in patenting the drug

Why is exploiting a library of natural compounds considered an attractive strategy in drug discovery?

It has led to important therapeutic breakthroughs Signup and view all the answers

Which of the following best describes the initial stage of drug discovery?

Theoretical compounds are filtered in silico Signup and view all the answers

What is one potential challenge when utilizing natural products in drug discovery?

Access to source material in remote locations Signup and view all the answers

Which drug is known for its use in treating malaria and derived from a natural product?

Artemisinin Signup and view all the answers

What does increasing the emphasis on defined molecular targets in drug discovery projects aim to achieve?

Reduce unforeseen therapeutic outcomes Signup and view all the answers

What is one major reason for incorporating pharmacokinetic and toxicological studies earlier in the drug discovery process?

To reduce the likelihood of compounds failing during clinical development. Signup and view all the answers

What trend in drug discovery has significantly increased the number of available compounds for testing?

The expansion from small to massive compound collections and virtual libraries. Signup and view all the answers

What is a significant method used to accelerate the lead optimization process in drug discovery?

High-throughput screening and in silico assessments. Signup and view all the answers

Which aspect of a drug's properties was traditionally investigated after its discovery?

Pharmacokinetic properties. Signup and view all the answers

What is a key factor in project planning for drug discovery when moving from research to development?

The project's objectives and expected timelines must be agreed upon. Signup and view all the answers

Which approach is increasingly being utilized to generate leads in drug discovery?

In silico predictions and assessment. Signup and view all the answers

What is a common goal during the lead optimization phase of drug discovery?

To improve drug metabolism and pharmacokinetic characteristics. Signup and view all the answers

What is the first step in the drug discovery process?

Defining the disease area and therapeutic need Signup and view all the answers

Why is it important to focus on cloned human targets as starting points in drug discovery?

They allow for more accurate modeling of human responses in research. Signup and view all the answers

What was a common methodology used for measuring the functional activity of drug targets before 1980?

Indirect measurement in isolated tissue preparations Signup and view all the answers

What is essential for the identification of a lead structure in drug development?

Validation of a molecular drug target Signup and view all the answers

Which type of products are classified under biopharmaceutical agents?

Endogenous mediators, monoclonal antibodies, and vaccines Signup and view all the answers

What aspect of the drug discovery process changed with the introduction of molecular drug targets?

Emphasis on defined molecular protein drug targets Signup and view all the answers

What is a primary challenge when dealing with endogenous molecules in drug development?

Producing sufficient quantities for market needs Signup and view all the answers

What does the drug discovery process typically begin with in terms of focus?

Choosing a disease area and defining therapeutic needs Signup and view all the answers

What is the significance of molecular drug targets in modern drug discovery?

They allow for the direct screening of compounds. Signup and view all the answers

Study Notes

Module 2: Drug Discovery

Drug discovery is a three-phase process: discovery, development, and commercialization
Drug discovery: from therapeutic concept to molecule
Drug development: from molecule to registered product
Commercialization: from product to therapeutic application to sales

Drug Discovery Process

The three phases are not independent; they must be closely coordinated throughout the project
Scientific strength and originality, along with the plan's development and marketing considerations, are critical criteria for evaluation
Historically, drug discovery was compartmentalized: scientists produced molecules; development teams ensured safety and transformed them into registrable drugs; and marketing focused on sales
Today, biomedical science has advanced, leading to a more technology-driven, expensive, and competitive drug discovery and development process. Partnerships with other companies and academic groups are also common
The process now aims to create a new synthetic drug and often has outcomes that differ from the original project goal
A significant emphasis on identified, well-defined molecular targets, often proteins, is crucial to success. This approach is newer than the less molecularly specific 'premolecular' strategy and should decrease instances of therapeutic surprises

Drug Discovery Phase

A typical new drug project starts with a choice of disease area and definition of the therapeutic need, as well as the identification of the molecular 'drug target'.
Next, creating the lead structure by design, testing, and fine-tuning is crucial for pharmaceutical development
The focus on specific molecular targets has only recently become the norm; in the past, the general mechanisms that drive the disease were the primary focus

Drug Discovery Process (continued)

The limited availability of specific protein targets in sufficient amounts hampered earlier drug research. Instead, researchers had to investigate functional activity through indirect means or animal models
Modern techniques like high-throughput screening (HTS) have allowed scientists to bypass these earlier limitations, significantly speeding the process by identifying 'hits' – compounds with significant activity against the target. The results can be highly significant (hundreds or thousands of compounds)
Hits are then 'validated' to see if they show a consistent structure-activity relationship in various tests and belong to a 'hit series'. This hit series becomes the basis for further chemical exploration
Once a lead series is narrowed in lead identification, researchers explore the compounds' properties, focusing on pharmacokinetic and toxicological aspects to reduce to a handful of lead series. This is done through parallel synthesis of derivatives, followed by testing for properties.
Finally, a few highly validated 'drug candidates' are selected for further development that can be subjected to preclinical trials

Trends in Drug Discovery

Drug discovery is becoming more focused on cloned molecular targets using high-throughput screens.
The time from the start of a project to identifying the compound has drastically decreased (3 years or less)
Computational or 'in silico' predictions about the molecule can generate new leads rapidly and efficiently
Researchers are now focusing on human targets to streamline the process and identify compounds through both in silico calculation and high-throughput screening of large natural product compound libraries
Pharmacokinetic and toxicological characteristics are now routinely considered in early drug development stages

Project Planning

Defining clear project objectives, expected timelines, and resource needs that are agreed upon within the team and approved by management are critical to success
The project begins when a specific target and screening methods have already been chosen to identify relevant drug candidates for moving to the preclinical stages
Decision-making during the drug discovery process also must include factors such as compound cost and availability, the significance of a desired result (vital versus preferable property), and the known probability of a compound failing; these must all be considered alongside the research itself

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Description

Explore the phases of drug discovery including discovery, development, and commercialization. This module delves into how these phases are interrelated and the impact of modern biomedical science on the drug development process. Understand the current landscape of drug discovery and the importance of collaboration in this field.