W5.4_Discovery and Design of Drugs

Question 1

What is the aim of anti-cancer drugs?

Answer 1

• Killing cells selectively without causing undue toxicity (therapeutic window as wide as possible to better control and reduce toxicity) -> reduce growth of tumour cells

Question 2

What were the key advances in 1990s that made discovery and design of drugs easier?

Answer 2

• High increase in understanding of basic biology/disease mechanism/genetics
• Better in vitro models -> reduced animal use
• Structural data to support understanding
• Better understanding of human pharmacokinetics
• Improved computational prediction
• Broad range of technologies beyond small molecules and vaccines

Question 3

What would happen to the properties of a drug when its logD increases? How is it achieved?

Answer 3

• Potency, permeability, metabolism, albumin binding, toxicity increases, while solubility decreases
• Methods: changing functional groups, position of acidic/basic groups