Anti-cancer drugs

Question 1

6 classes of anticancer drugs

Answer 1

1. alkylating drugs
2. platinating drugs
3. anti-metabolites
4. cytotoxic antibodies
5. mitotic inhibitors
6. topoisomerase inhibitors

Question 2

alkylating drug examples (2)

Answer 2

cyclophosphamide
chlorambucil

Question 3

alkylating drug MOA

Answer 3

• reactive alkyl group forms covalent bonds with DNA, crosslinking it (rigid)
• causes DNA breaks
• disrupts DNA replication and transcription

Question 4

platinating drug examples (2)

Answer 4

(-platin)
cisplatin (!!contradindicated with creatinine clearance <60ml/min)
carboplatin

Question 5

platinating drug MOA

Answer 5

• acts as alkylating drugs
• forms covalent bonds with DNA, crosslinking it and causes DNA breaks
• disrupts DNA replication & transcription

Question 6

anti-metabolites examples (2)

Answer 6

methotrexate (MTX)
5-fluoruoracil (5-FU)

Question 7

anti-metabolites MOA + clinical indications

Answer 7

methotrexate (MTX): inhibits dihydrofolate reductase needed to recycle folate⇒ prevents thymidine monophosphate synthesis
- clinical indication: variety of tumours eg breast cancer/lymphoma

5-fluorouracil (5-FU): inhibits thymidylate synthase, gets misincorporated into DNA & RNA
- clinical indication: colorectal cancer

Question 8

cytotoxic antibodies examples (3)

Answer 8

“-RUBICIN”
anthracyclines e.g. doxorubicin, daunorubicin, epirubicin

Question 9

cytotoxic antibodies MOA (4)

Answer 9

• inhibits RNA/DNA synthesis by intercalating base pairs, prevents DNA replication
• create Fe mediated free O2 radicals that cause DNA damage
• inhibits topoisomerase 2
• alters membrane fluidity & ion transport

Question 10

mitotic inhibitors examples (3)

Answer 10

(-TAXEL)
paclitaxel
docetaxel

vinblastine

Question 11

mitotic inhibitors MOA

Answer 11

• bind to beta subunit of tubulin, disrupting formation of microtubules
• vinblastine bind to polymerizing end to prevent elongation of microtubule
• paclitaxel stabilize microtubules to prevent shortening

Question 12

topoisomerase inhibitors examples (3)

Answer 12

type 1: -TECAN
topotecan
irinotecan

type 2: etoposide

Question 13

topoisomerase MOA

Answer 13

inhibits type 1/2 topoisomerase, intereferes with transcription & replication of DNA

Question 14

phase specific drugs (3)

Answer 14

1. anti-metabolites
2. cytotoxic antibiotics
3. mitotic inhibitors

Question 15

phase non-specific drugs (3)

Answer 15

1. alkylating drugs
2. platinating drugs
3. topoisomerase inhibitors