Cancer Drugs

Question 1

1. Why is single agent chemotherapy rarely used?
2. Why is combination chemotherapy chemotherapy preferred?
3. What is adjuvant chemotherapy?
4. What is neoadjuvant chemotherapy?

Answer 1

1. genetically resistant cells are selected out, thus rarely curative
2. different MOAs and side effect profiles reduces the likelihood of resistance and toxicity
3. given after initial treatment (radiotherapy/surgery) to reduce the risk of recurrence
4. used to shrink tumours prior to surgical/radiological treatments

Question 2

1. What is the MOA of alkylating agents?

2. Name 3 examples of alkylating agents

Answer 2

1. bind to alkyl groups on DNA, causing interstrand crosslinking, which interferes with transcription and DNA replication leading to apoptosis.
2. cyclophosphamide
   cisplatin
   lomustine

Question 3

1. What is the MOA of antimetabolites?

2. Name 4 examples of antimetabolites

Answer 3

1. interfere with cell metabolism, including DNA and protein synthesis
2. methotrexate
   5-FU
   mercaptopurine
   Capecitabine

Question 4

1. What is the MOA of anti-tumour antibiotics?

2. Name 2 examples of anti-tumour antibiotics

Answer 4

1. interrupt DNA and RNA synthesis
2. doxorubicin
   bleomycin

Question 5

1. what is the MOA of topoisomerase inhibitors?

2. Name an example of topoisomerase inhibitor

Answer 5

1. interrupt regulation of DNA unwinding

2. etoposide

Question 6

1. What is the MOA of vinca alkaloids and taxanes?

2. name 2 examples of vinca alkaloids/taxanes?

Answer 6

1. PLANT DERIVATIVES. Affect microtubule formation thus disrupt formation of mitotic spindle
2. Docataxel
   Vinblastine
   Vincristine

Question 7

1. What is the MOA of anti-oestrogens?

2. Name 3 examples of anti-oestrogens

Answer 7

1. used in oestrogen positive breast/ovarian cancers.
2. letrozole, anastrozole (aromatase inhibitors)
   Tamoxifen (oestrogen receptor antagonists)

Question 8

1. What is the MOA of platinum compounds?
2. Name 3 examples of platinum compounds
3. Which malignancies are platinum compounds used to treat?

Answer 8

1. causes interstrand crosslinking, which interferes with transcription and DNA replication leading to apoptosis.
2. cisplatin
   carboplatin
3. solid tumours

Question 9

Name 5 general side effects of chemotherapy

Answer 9

1. GI irritation - diarrhoea, nausea and vomiting, sore mouth
2. Myelosuppression leading to anaemia, neutropenia and thrombocytopenia
3. hair loss
4. infertility
5. tumpir lysis syndrome (hyperuricaemia, hyperkalaemia, hypophosphataemia or hypocalcaemia, with consequent renal damage and cardiac arrythmia)

Question 10

Name 3 specific side effects of alkylating agents

Answer 10

1. impaired future fertility
2. bone marrow suppression and neutropenia
3. development of other malignancies - AML and bladder cancer

Question 11

1. Name 5 side effects specific to platinum compounds?
2. Which side effects are associated with cisplatin?
3. Which side effects are associated with carboplatin?

Answer 11

1. severe nausea and vomiting
   nephrotoxicity
   ototoxicity
   peripheral neuropathy
   myelosuppression

2. nausea and vomiting; nephrotoxicity
3. less nephro- neuro and oto-toxicity than cisplatin but is more myelotoxic

Question 12

1. What is the MOA of Bortezomib?

2. What malignancy is it generally used to treat?

Answer 12

1. proteasome inhibitors (prevent breakdown of pro-apoptotic factors)
2. myeloma

Question 13

What side effects are associated with anastrozole? (10)

Answer 13

• hot flushes
• vaginal dryness
• vaginal bleeding
• hair thinning
• anorexia
• nausea and vomiting
• diarrhoea
• headache
• arthralgia
• stevens-johnson’s syndrome

Question 14

What is a risk of chemotherapy administered intravenously?

Answer 14

extravasation - leads to localised tissue ulceration and necrosis

Question 15

Name 2 important drug interractions for tamoxifen

Answer 15

1. SSRIs

2. Warfarin