Anti-cancer drugs

Question 1

Cyclophosphamide

Answer 1

• bifunctional alkylating agent
  1. alkylates DNA bases —> DNA fragmentation
  2. cross-link formation, prevents DNA uncoiling for synthesis/transcription –> DNA damage

Question 2

Dacarbazine

Answer 2

monofunctional alkylation of DNA and protein

indication: Hodgkins lymphoma

Question 3

Methotrexate

Answer 3

folate antagonist

• inhibiting several enzymes needed for nucleotide synthesis → inhibits cell division → stops cancer cell growth

Question 4

Hydroxycarbamide (prev Hydroxyurea)

Answer 4

inactivates ribonucleotide reductase, selectively inhibits DNA synthesis

indication: essential thrombocythaemia

Question 5

Cytosine arabinoside

Answer 5

• DNA polymerase inhibitor

- gets incorporated into DNA introduces double strand breaks

Question 6

5-fluorouracil MoA

Answer 6

inhibits thymidylate synthase by covalently binding to it + forming a ternary complex

=> which inhibits formation of thymidylate from uracil

• ⇒ inhibiting DNA and RNA synthesis → cell death

Question 7

Etoposide

Answer 7

topoismerase inhibitor

forms a complex w DNA topoisomerase II+inhibits it → thus inhibiting DNA re-ligation

=> DNA double strand breaks

Question 8

Vinblastine

Answer 8

tubulin polymerase inhibitor

Question 9

Rituximab

Answer 9

monoclonal AB directed against B-cell CD20 antigen found on normal + malignant B-cells

used in treatment for:

• Non-hodkin’s lymphoma
• Chronic lymphocytic leukaemia
• Rheumatoid arthritis

Question 10

Doxorubicin

Answer 10

anthracyclic antibiotic
DNA/RNA synthesis inhibitor

• intercalates btwn base pairs
• inhibits topoisomerase II activity