SPEC REF 4.13  |  UNIT 4A

Developing New Drugs

From William Withering's digitalis soup to modern three-phase clinical trials — how medicines are discovered, tested and approved.

Learning Objectives — Tick as you master each one

Understand the development of drug testing from historic to contemporary protocols

Describe William Withering's discovery of digitalis and its significance

Explain the purpose and use of placebos in drug trials

Describe the three phases of clinical trials and double-blind methodology

Explain why drugs must be effective, safe, stable, easily administered and manufacturable

Discuss the ethical issues surrounding animal testing and clinical trials

Diagnostic Quiz

Test what you already know before we begin. Don't worry about getting these wrong — that's the point. Attempting to retrieve answers, even incorrectly, primes your brain to learn the material more deeply.

1. William Withering discovered that an extract from which plant could treat dropsy (oedema)?

A Willow bark
B Foxglove
C Poppy
D Cinchona tree
Correct! Foxgloves contain digitalis, which Withering identified as the active ingredient. Today the drug is called digoxin.
Not quite. Willow bark gives us aspirin, poppies give morphine, and cinchona gives quinine. Foxglove was the source of digitalis for treating heart failure.

2. What is a placebo?

A A drug given at a higher dose than normal
B The best currently available treatment
C An inactive substance that looks like the drug being tested
D A drug tested only on animals
Correct! A placebo has no active ingredient but looks identical to the real drug. It controls for the psychological effect of believing you're receiving treatment.
A placebo is an inactive substance designed to look like the real drug. It's used as a control to eliminate the psychological effect of simply receiving "treatment."

3. In a double-blind trial, who knows which patients receive the real drug?

A The patient only
B The doctor only
C Both the patient and the doctor
D Neither the patient nor the doctor
Correct! "Double-blind" means neither the patient nor the doctor/scientist knows who gets the drug and who gets the placebo. This removes unconscious bias from both sides.
In a double-blind trial, neither the patient nor the doctor knows who receives the drug or the placebo. This prevents bias from either party influencing the results.

4. Approximately how long does it take and how much does it cost to develop a new drug?

A ~10 years & ~US$2.6 billion
B ~5 years & ~US$500 million
C ~2 years & ~US$100 million
D ~20 years & ~US$10 billion
Correct! It takes about 10 years and around US$2.6 billion to bring a new medicine to market.
It typically takes about 10 years and approximately US$2.6 billion to develop a new drug and get it approved.

5. Which phase of clinical trials involves the largest number of patients?

A Phase 1
B Phase 3
C Phase 2
D Pre-clinical
Correct! Phase 3 trials use thousands of patients (5,000+) and are the final step before regulatory approval.
Phase 3 involves the largest numbers — over 5,000 volunteer patients. Phase 1 uses a small number of healthy volunteers, and Phase 2 uses 100–500 patients with the target disease.

Your score is tracked at the bottom of the page. Don't worry about mistakes — they help you learn.

William Withering & Digitalis Soup

Throughout history, almost every culture has used plants to treat diseases. In the 21st century, modern pharmaceutical companies still recognise the value of plant-based medicines — but the way drugs are developed and tested has changed dramatically.

🧠 Feynman Analogy — Think of it like this

Imagine you're a detective in the 1700s. You hear that a local "wise woman" has a secret soup recipe that cures a mysterious illness. You don't know which ingredient in the soup is doing the work — it has 20 different herbs! So you spend 10 years testing each ingredient one by one on different patients to figure out which one is the magic bullet. That's exactly what William Withering did.

The Story

William Withering (1741–99) was a British doctor and keen botanist. In 1775, a patient with severe heart failure came to him. Withering had no effective treatment, so his patient visited a local "wise woman" who used herbal remedies. After drinking her soup, the patient recovered.

Withering was fascinated. He bought the recipe — it contained about 20 different herbs. He guessed that foxglove contained the active ingredient. This plant contains a chemical called digitalis, which had been known as a poison for centuries but was also linked to reports of curing oedema (dropsy) — swelling caused by fluid retention when the heart and kidneys fail.

Over the next 10 years, Withering tested a variety of foxglove preparations on 163 patients at Birmingham General Hospital. He discovered that:

  • Many patients improved, though some almost died of digitalis poisoning
  • Side effects included nausea, vomiting and worse
  • Getting the dose right was critical — too much was lethal
  • Dried and powdered leaves worked best (boiling reduced effectiveness)
  • The patient's heartbeat became stronger and more regular, kidneys recovered, excess fluid was expelled

The drug based on foxglove chemicals is now called digoxin, and it's still prescribed by doctors today — about 230 years after Withering's work.

Visible Thinking Routine

See — Think — Wonder

Consider Withering's approach to drug discovery. Think carefully about what you notice, what it makes you think, and what questions it raises.

Thinking prompts to consider:
• Withering had no control group, no placebo, no blinding — how reliable were his results?
• Some patients nearly died — would this be acceptable today?
• He tested on real, sick patients from the start — today we start with lab tests and animals first. Why?
• Despite the limitations, his work led to a medicine still used 230+ years later. What does this tell us about the relationship between scientific rigour and useful outcomes?
Progress Check 1

Fill in the blanks using the word bank:

foxglove digitalis 163 oedema digoxin 10

William Withering discovered that the plant contained a chemical called that could treat the condition known as . He tested his treatments on patients over years. The modern drug based on this work is called .

Explain the following in your own words:

a) Why was Withering's method considered both groundbreaking and risky?

b) Why did boiling the foxglove leaves reduce the drug's effectiveness?

a) Groundbreaking: He was systematic — testing on many patients over 10 years, refining the dose, recording side effects. This was early evidence-based medicine. Risky: He had no control group, some patients nearly died from poisoning, and there were no ethical review boards.

b) Heat can denature or break down organic molecules. Boiling likely degraded the active digitalis compounds, reducing their concentration and therefore their therapeutic effect. Drying and powdering preserved the chemical structure better.

Compare & Evaluate:

William Withering tested his foxglove preparations directly on sick patients at Birmingham General Hospital. Today, drugs must pass through pre-clinical testing, animal testing, and three phases of clinical trials before they can be prescribed.

Evaluate the strengths and limitations of Withering's approach compared to modern drug testing protocols. Consider: reliability of results, patient safety, and the pace of discovery. [6 marks]

Mark scheme guidance (6 marks):
Strengths of Withering's approach: tested on real patients with the condition, refined dosage through observation over 10 years, led to a medicine still in use today, pragmatic approach in an era with no alternatives.

Limitations: no control group or placebo, no blinding (both patient and doctor knew treatment was given), risk of poisoning/death, no statistical analysis, small/biased sample from one hospital, no ethical oversight.

Modern advantages: controlled variables, statistical significance, patient safety protections, ethical review boards, phased approach reduces risk, placebos and double-blinding remove bias.

Evaluation point: Modern protocols are more reliable and safer but are extremely slow (~10 years) and expensive (~$2.6 billion). Withering's faster approach was essential in his era but would be unacceptable today due to the uncontrolled risks to patients.

What Makes a Good Drug?

Every medicine that comes onto the market today is the result of years of research and development (R&D). It takes about 10 years and around US$2.6 billion to develop a new drug. A new medicine must meet all five of the following criteria:

The Five Drug Criteria

1. Effective — It must cure, prevent, or relieve the symptoms of the disease it is designed for.

2. Safe — It must be non-toxic and without unacceptable side effects.

3. Stable — It must be stored for a reasonable period and used under normal conditions without breaking down.

4. Easily taken in and removed — It must reach its target in the body and be excreted (removed) once it has done its job.

5. Manufacturable — It must be possible to produce it in a very pure form, in large quantities, and quite cheaply.

🧠 Feynman Analogy — The 5-Star Restaurant Test

Think of a new drug like a dish at a 5-star restaurant. It must: taste great (be effective), not make you ill (be safe), survive in the fridge overnight (be stable), be digestible (easily absorbed and removed), and be replicable by any trained chef (manufacturable at scale). If it fails even one of these tests, it doesn't make the menu.

How Scientists Discover Potential New Drugs

In the past, herbal remedies were a common source of new medicines. Today, scientists use more targeted approaches:

One method is to investigate chemicals that bind to our protein receptors or to the active sites of our enzymes. Researchers often use computer models to fit new molecular structures into the active site of enzymes or receptors that are important in disease processes. This can identify useful starting points for further work.

When scientists find a promising compound, they may patent it. A patent gives the inventor the exclusive right to make and sell the invention for the next 20 years. However, much of those 20 years will be consumed by the testing process.

Progress Check 2

Match each drug criterion to its description:

"It must not break down during normal storage"

A Effective
B Stable
C Safe
D Manufacturable
Correct! Stability means the drug can be stored for some time and used under normal conditions.
This describes stability — the drug must not degrade during storage.

"It must reach its target in the body and be removed once it has done its job"

A Safe
B Effective
C Easily taken in and removed
D Stable
Correct! The drug must be able to reach its target and be excreted afterwards.
This describes the requirement for the drug to be easily absorbed and then removed (excreted) from the body.

Explain why a drug that is highly effective but impossible to manufacture cheaply might never reach patients.

Even if a drug works perfectly, pharmaceutical companies need to produce it in large quantities at a reasonable cost to make it accessible to patients and commercially viable. If the manufacturing process requires rare materials or extremely complex synthesis, the drug may be too expensive for healthcare systems to afford, meaning patients who need it cannot access it. A drug that costs millions per dose helps nobody in practice.

Application question:

A researcher discovers a chemical compound that binds strongly to a receptor involved in Alzheimer's disease. In lab tests on cell cultures, it reduces toxic protein build-up by 85%. However, when given orally to mice, less than 2% of the compound reaches the brain.

Using your knowledge of drug criteria, explain which requirement this compound fails and suggest how scientists might try to overcome this problem. [4 marks]

Mark scheme (4 marks):
1. The compound fails the "easily taken in" criterion — it cannot effectively reach its target site (the brain) when administered orally [1 mark].
2. This may be because the compound is broken down in the digestive system / cannot cross the blood-brain barrier [1 mark].
3. Scientists could try: modifying the chemical structure to improve absorption / changing the delivery method (e.g. injection, nasal spray, nanoparticle delivery) [1 mark].
4. They could use computer modelling to redesign the molecule so it can cross the blood-brain barrier while retaining its ability to bind to the target receptor [1 mark].

The Drug Development Pipeline

From initial discovery to a medicine on the pharmacy shelf, there is a long and rigorous process. Thousands of compounds are screened, but very few ever make it to market.

🧠 Feynman Analogy — The X-Factor for Molecules

Imagine 10,000 people audition for a singing competition. In the first round (lab tests), most are eliminated because they can't hold a tune (the compound doesn't work in cell cultures). A handful proceed to bootcamp (animal testing), where many more are cut because they can't handle the pressure of performing live (the drug causes harmful effects in a whole organism). Only about 5 make it to the live shows (human clinical trials), and often just 1 wins the competition (gets approved). That one winner then has to prove they can sustain a career (post-market surveillance).

The Development Timeline

1. Early Phase Research
4–6 years
Scientists identify 5,000–10,000 potential compounds through screening chemicals that bind to protein receptors or enzyme active sites. Computer models help fit new structures into target molecules. Most compounds are eliminated at this stage.
2. Pre-clinical Testing
~1 year
The new compound is tested on cell cultures, tissue cultures, and whole organs in the lab. These tests check whether it does what scientists predicted. Many chemicals fail here because they don't work in living tissue or have harmful effects. Compounds that pass move into development.
3. Animal Testing
Part of pre-clinical phase
Before testing on humans, the drug must be tested on animals — the law requires it. A good delivery system must be found (tablets, injections, nasal spray). Tests show how the drug works in a whole organism: is it taken into cells? Is it chemically changed? Is it safely excreted? Tests must be carried out on at least two species — a rodent and a non-rodent. Mice and rats are the most commonly used.
4. Clinical Trials (Phases 1–3)
6–7 years
Human testing in three phases (detailed in next section). Approximately 250 compounds enter trials, but only about 5 make it through all three phases successfully.
5. Regulatory Review
0.5–2 years
A regulatory authority reviews all the data — beneficial effects vs. harmful effects — before deciding whether to grant a licence. The drug cannot be sold without this licence.
6. Post-market Surveillance
Continuous
Even after approval, the medicine is monitored for safety and effectiveness for as long as it is prescribed. Any adverse reactions are reported and recorded. The benefits must always outweigh the risks.
Visible Thinking Routine

Connect — Extend — Challenge

Progress Check 3 — Sequence the Drug Development Pipeline

Drag the stages into the correct order from first to last:

Animal testing Post-market surveillance Early phase research Clinical trials Regulatory review Pre-clinical testing

Drop stages here in order (1st → 6th):

Clinical Trials

If animal testing is successful, a regulatory authority will take decisions about whether the drug can be trialled on people. The testing varies from country to country, but internationally it must follow strict criteria.

Phase 1 — Safety Testing

The new drug (or in some cases, a placebo) is given to a small number of healthy volunteers. The goal is to check that the drug works as expected in the human body and doesn't cause any unexpected side effects.

At the same time, scientists continue looking at the effects of longer-term use of the drug in animal trials.

🧠 Feynman Simplification

Phase 1 asks a simple question: "Is this safe for humans at all?" It's like dipping your toe in the pool before jumping in. Small group, healthy people, cautious doses.

Phase 2 — Does it Work?

If Phase 1 is successful, the drug moves to Phase 2 trials. This is when the new drug is used with patients who actually have the target disease. Between 100 and 500 patient volunteers are recruited.

Patients are given either the new drug or a similar number receive the best current treatment (or sometimes a placebo). This is the first chance for scientists and doctors to see how the new medicine affects the disease in a real patient.

Volunteers are closely monitored to find out more about the ideal dose, the effectiveness of the drug, and any side effects. Success at this stage means the compound has a good chance of becoming a useful medicine.

Understanding Placebos

A placebo is a substance that looks like the drug being tested but has no active ingredient. It serves as a control in the experiment.

Why use a placebo? Patients often appear to respond to a treatment simply because they believe it will help them — not because of any chemical effect. This is called the placebo effect. Using a placebo eliminates this possibility, so scientists can be sure any improvement is caused by the actual drug.

🧠 Feynman Analogy

Imagine two students both think they've drunk an energy drink before an exam. One actually drank an energy drink; the other drank coloured water (the placebo). If both students perform equally well, the energy drink doesn't actually work — the improvement was just in their heads. The placebo is what lets you tell the difference.

Phase 3 — Large-Scale Confirmation

Phase 3 trials confirm the effectiveness and safety of the new drug. The numbers of patients involved are large — typically over 5,000 volunteer patients — so the trials have a better chance of showing up any unexpected adverse side effects.

Patients are randomly allocated to receive either the new medicine or the control/placebo. Data on effectiveness, side effects and other information are collected and assessed to see if there are any statistically significant differences between the new medicine and the placebo or currently available drug.

It is difficult to achieve a complete set of results because many patients stop taking the medicine for various reasons — some don't take it regularly.

In some trials, the drug is so successful that the trial is halted early — it becomes unethical to deny the new treatment to patients receiving the old treatment or placebo.

Double-Blind Trials

Phase 2 and 3 trials are normally carried out as double-blind trials. This means neither the doctor/scientist nor the patient knows whether the patient is receiving the new medicine, a control medicine, or a placebo.

Why double-blind?

Patients often appear to respond to a treatment because they believe it will do them good — this is the placebo effect. But doctors can also unconsciously influence results. If a doctor knows a patient is receiving the new drug, they might interpret symptoms more favourably. Double-blinding removes bias from both sides.

Instead of a placebo, a control medicine (the best-performing available treatment) is sometimes used to avoid denying any patient treatment entirely.

🧠 Feynman Analogy

Think of a blind taste test for Coca-Cola vs. Pepsi, but the person pouring the drinks doesn't know which is which either. This way, neither the taster's preference nor the server's body language can influence the result. That's double-blinding.

Progress Check 4

1. How many patient volunteers are typically involved in Phase 2 trials?

A 5–10 healthy volunteers
B 50–100 healthy volunteers
C 100–500 patients with the disease
D 5,000+ patients with the disease
Correct! Phase 2 involves 100–500 patients who have the target disease.
Phase 2 trials involve 100–500 patients with the target disease (not healthy volunteers — that's Phase 1). 5,000+ is Phase 3.

2. Why might a clinical trial be halted early?

A The company runs out of funding
B The drug is so effective that it's unethical to withhold it
C All patients have recovered
D The trial has been running for over 10 years
Correct! If the evidence shows the new treatment is dramatically better, it becomes unethical to deny it to patients in the control group.
A trial may be halted early when the drug proves so successful that continuing to give some patients a placebo or inferior treatment would be unethical.

Complete the comparison table — fill in each cell:

Feature Phase 1 Phase 2 Phase 3
Participants
Main purpose
Phase 1: Small number of healthy volunteers | Purpose: Check safety, dose, side effects
Phase 2: 100–500 patients with the target disease | Purpose: Test effectiveness, find ideal dose
Phase 3: 5,000+ patients | Purpose: Confirm effectiveness and safety at large scale, detect rare side effects

Evaluate this claim:

"Double-blind trials are the gold standard, so single-blind or unblinded trials should never be used."

Do you agree or disagree? Justify your answer with reference to specific scenarios. [4 marks]

Disagree (with nuance):
While double-blind trials are indeed the gold standard for reducing bias, they are not always practical or ethical:

Surgical trials: It's impossible to blind a surgeon to whether they are performing the real procedure.
Life-threatening conditions: If no treatment exists, using a placebo may be unethical — all patients should receive the experimental drug.
Distinctive side effects: If the drug causes obvious side effects (e.g. a rash), patients and doctors can guess who is in the treatment group, breaking the blind.
Rare diseases: With very few patients available, a randomised controlled trial may not be feasible.

Double-blind trials minimise bias and are preferred whenever possible, but good science adapts to ethical and practical constraints.

Ethics of Drug Testing

Drug development raises important ethical questions at every stage — from animal testing to the use of placebos in human trials.

Animal Testing — The Debate

Some people have strong ethical objections to the use of animals in drug testing. However, the law currently states that animal testing must be carried out before drugs can be tested on people.

Key considerations:

  • Mice and rats are the most widely used animals. Their use is perceived as less emotive than dogs, cats, or monkeys.
  • Rodents provide valid models because their genetic make-up and strains are well known. They are small and easy to keep in humane conditions.
  • Scientists try to replace animals with tissue cultures and computer models wherever possible.
  • The numbers of animals used are kept to a minimum, and tests are designed to cause the minimum of distress.
  • However, information from computer models or tissue cultures alone is not yet sufficient to move directly to human testing.
Visible Thinking Routine

Claim — Support — Question

Consider this statement: "Animal testing is a necessary evil — without it, we cannot guarantee the safety of new medicines for humans."

Arguments FOR animal testing:
• The law requires it before human trials can begin
• Animals (especially mammals) share similar biological systems with humans
• It has contributed to life-saving treatments (insulin, antibiotics, vaccines)
• There is currently no complete alternative that replicates a whole living organism

Arguments AGAINST animal testing:
• Animals suffer pain and distress — this is ethically wrong
• Animal responses don't always predict human responses accurately
• Computer modelling and tissue cultures are improving and may replace animal testing
• The "3Rs" principle (Replace, Reduce, Refine) should be more aggressively pursued

Exam tip: Whatever your personal view, always present a balanced argument with points from both sides. Use specific examples and scientific reasoning.

Ethical Dilemma: Prescribing Before Full Approval

Sometimes a doctor may want to prescribe a drug before it has completed full human trials — for example, for a terminally ill patient with no other options.

Progress Check 5 — Extended Writing

Suggest two arguments FOR and two arguments AGAINST prescribing a drug before it has completed all stages of testing. [4 marks]

FOR (1 mark each):
• The patient may be terminally ill with no other treatment options — the potential benefit outweighs the unknown risk
• Early-phase results may already show the drug is effective, and waiting years could cost the patient's life

AGAINST (1 mark each):
• The drug may have unknown long-term side effects that haven't been identified in the limited testing
• If the drug harms the patient, it could damage public trust in the pharmaceutical industry and the approval process
• Without Phase 3 data, the ideal dose may be unknown — too much could be toxic, too little could be ineffective

Exam Practice Questions

These are structured like IAL Biology exam questions. Attempt each one before checking the mark scheme. Writing out your answers by hand is the most effective retrieval practice.

2 marks

Question 1

State two properties that a new medicine must have before it can be sold to patients.

3 marks

Question 2

Describe the role of William Withering in the development of the drug digoxin.

4 marks

Question 3

Explain why double-blind trials are used in the testing of new drugs.

6 marks

Question 4

Compare William Withering's methods of discovering digoxin with modern drug testing protocols. In your answer, you should consider the methods used, the reliability of results, and patient safety.

3 marks

Question 5 — Interleaved Retrieval

FROM EARLIER TOPICS: Biological Molecules & Transport

Digoxin must travel through the blood to reach the heart muscle cells. Explain how substances are transported in the blood and describe how digoxin might enter a heart muscle cell.

2 marks

Question 6 — Interleaved Retrieval

FROM EARLIER TOPICS: Enzymes

Scientists use computer models to fit new molecular structures into the active site of enzymes. Explain what is meant by the "active site" of an enzyme and why its shape is important.

Exit Ticket

Rate your confidence on each learning objective, then complete the final retrieval challenge.

Confidence Self-Assessment

1. I can describe Withering's discovery of digitalis

2. I can explain the five criteria for a new drug

3. I can describe the three phases of clinical trials

4. I can explain placebos and double-blind methodology

5. I can discuss ethical issues around animal testing and clinical trials

Visible Thinking Routine

I Used to Think… Now I Think…

Reflect on how your understanding has changed during this lesson.

Final Retrieval Challenge — Brain Dump

Without looking back at any of the lesson content, write everything you can remember about drug development. Try to include key terms, names, numbers, and processes. This is the most powerful form of retrieval practice.

Key facts to check your brain dump against:

Withering: British doctor (1741–99), foxglove, digitalis, 163 patients, 10 years, Birmingham General Hospital, oedema/dropsy, digoxin still used today, dried/powdered leaves best, boiling reduces effectiveness.

Drug criteria: effective, safe, stable, easily taken in and removed, manufacturable at scale.

Development pipeline: ~10 years, ~US$2.6 billion, 5,000–10,000 compounds screened, early research → pre-clinical testing → animal testing → clinical trials → regulatory review → post-market surveillance.

Clinical trials: Phase 1 (small, healthy volunteers, safety), Phase 2 (100–500 patients, effectiveness), Phase 3 (5,000+, confirm at scale). Placebo = inactive substance used as control. Placebo effect = patients improve because they believe they're being treated. Double-blind = neither doctor nor patient knows who gets drug vs. placebo.

Ethics: Animal testing required by law, 3Rs (replace, reduce, refine), mice/rats most common, ethical debate around both animal testing and early access to drugs before full trials.
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