Anticancer Drug Design

Question 1

What are the 9 classifications of cancer drugs via MoA?

Cytotoxic (5) vs non-cytotoxic (4)

Answer 1

Cytotoxic
1. Alkylating agents
2. Platinum-based drugs
3. Antimetabolites
4. Topoisomerase-interactive drugs
5. Anti-microtubule drugs

Non-cytotoxic
6. Hormonal agents
7. Targeted therapies
8. Vascular targeting therapies
9. Immunotherapies

Question 2

Alkylating drugs MoA

Answer 2

1. Formation of azirinidyl species, which is attacked by nucleophiles
2. Formation of intra- and interstrand crosslinks (2Cl molecules, hence 2 bonds formed)

Question 3

Platinum drugs MoA

Answer 3

1. Forms DNA interstrand and intrastand crosslinks, altering the topology of DNA
2. DNA will unwind and bend towards major groove, will be recognised by mismatch repair and undergo apoptosis

Considered an alkylating agent