Chemotherapy: Anticancer

Question 1

Melphalan

Which cancers?

Answer 1

Nitrogen mustard alkylating agent
Phenylalanine derivative of mechlorethamine
Chronic myeloid leukaemia & occasionally melanoma

Question 2

Cyclophosphamide

Which cancers?

Answer 2

Nitrogen mustard alkylating agent
Prodrug, converted to active forms in liver.
Lymphomas, some forms of leukaemia, some solid tumours

Question 3

Lomustine

Which cancers?

Answer 3

Nitrosurea
Cross-links DNA to other DNA strands/ protein, prevents replication of dsDNA.
Lymphoma (particularly cutaneous lymphoma), melanoma, kidney & lung tumours.
Penetrates BBB- can be used to treat cancers in the brain

Question 4

Mitomycin C

Answer 4

Aziridine-containing antibiotic

Alkylates and cross-links DNA, preventing strand separation during DNA replication & transcription

Question 5

Cisplatin

Answer 5

Platinum based

Sarcomas, some carcinomas (small cell lung, ovarian), lymphomas, germ cell tumours

Question 6

Doxorubicin

Answer 6

Anthracycline antibiotic
Intercalates in DNA
Structurally closely related to Daunomycin
Often administered by local injection

Question 7

Daunomycin

Answer 7

Planar polycyclic anthracycline antibiotic

Intercalates in dsDNA, caused local unwinding

Question 8

Mitoxantrone

Which cancers?

Answer 8

Anthracycline agent

Metastatic breast cancer, acute myeloid leukaemia, non-Hodgkin’s lymphoma.

Question 9

Methotrexate

Replaced?

Answer 9

Antimetabolite and antifolate drug
Inhibits metabolism of folic acid
Replaced more toxic & powerful antifolate aminopterin

Question 10

Leucovorin

Used with?

Answer 10

Adjuvant

Used with methotrexate, and also in synergistic combination with 5-Fluorouracil

Question 11

5-Fluorouracil

Used with?
Which cancers?

Answer 11

Antimetabolite
Pyrimidine analogue
Typically administered with Leucovorin
Colorectal and pancreatic cancer (established form of chemotherapy for decades)

Question 12

Etoposide

Which cancers?

Answer 12

Topoisomerse II inhibitor

Lung, testicular, lymphoma, non-lymphocytic leukaemia

Question 13

Topotecan

Which cancers?

Answer 13

Topoisomerase I inhibitor

Ovarian & lung cancer

Question 14

Vinblastine

Which cancers?

Answer 14

Vinca alkaloid
Anti-mitotic drug
Hodgkin’s lymphoma, non-small cell lung cancer, breast & testicular cancer

Question 15

Taxol

Which cancers?

Answer 15

Part of the taxane category
Mitotic inhibitor
Lung, ovarian, breast, head & neck cancer, and advanced forms of Karopsi’s sarcoma

Question 16

Tamoxifen

Which cancers?

Answer 16

Oestrogen receptor antagonist
Breast cancer (v widely used)
Orally active

Question 17

Toremifene

Answer 17

Tamoxifen analogue without estrogen agonist properties

Question 18

Goseraline

Answer 18

Decapeptide analogue of gonadotrophin-releasing hormone

Disrupts endogenous hormonal feedback systems -> down regulation of testosterone & estrogen production

Question 19

Flutamide

Which cancers?

Answer 19

Oral anti-androgen drug
Prostate cancer
Competes with testosterone & its powerful metabolite DHT for binding to androgen R in prostate gland-> thus prevents their stimulation of growth of prostate cancer cells.

Question 20

Prednisone

Which cancers?

Answer 20

Synthetic corticosteroid prodrug, converted -> prednisolone in the liver.
Inhibits growth of lymphocytes in leukaemias

Question 21

Rituximab

Answer 21

anti-CD20 monoclonal antibody

Question 22

Trastuzumab

Answer 22

anti-HER2 monoclonal antibody

Question 23

Bevacizumab

Answer 23

anti-VEGF monoclonal antibody

Question 24

Cetuximab

Answer 24

anti-EGFR monoclonal antibody

Question 25

Erlotinib

Answer 25

small molecule ligand

Inhibits EGFR tyrosine kinase

Question 26

Imatinib (marketed as Gleevec/Glivec)

Which cancers?

Answer 26

2-phenylaminopyrimidine derivative
Specifically inhibits a number of tyrosine kinase enzymes
Chronic myeloid leukaemia and gastrointestinal stromal tumours