Anti-Cancer

Question 1

Melphalan

Answer 1

Covalent oh cross links DNA
Nitrogen Mustard
Accumulates in tissues - increasing sensitivity for melanoma cells as is an L-Phenylalanine (melanin precursor)

Question 2

Carmustine

Answer 2

A Nitrosourease
Alkylate carbomoylates and cross-links DNA
Lipophillic therefore can be used for brain tumours
Cause reduction in circulating rbc’s and platelets
Must be given IV

Question 3

Lomustine

Answer 3

ANitrosourease
Alkylate carbomoylates and cross-links DNA
Lipophillic therefore can be used for brain tumours
Cause reduction in circulating rbc’s and platelets

Question 4

Cisplatin

Answer 4

Covalently binds DNA
Cross-linking agent between Guanine 
Changes shape of major groove 
IV administration 
Platinum containing compound therefore associated renal toxicity and bone marrow suppression

Question 5

Daunomycin

Answer 5

Non-covalently binds DNA
Intercalates between strands disrupting major+minor groves
Induces oxidative damage causing DNA fragmentation
Anthracyclin
Cardiac side effects-lipid peroxidation
Topoisomerase type 2 inhibitor

Question 6

Actinomycin D

Answer 6

Non-covalently binds DNA
Intercalates between strands disrupting major+minor groves
Induces oxidative damage causing DNA fragmentation
Anthracyclin
Cardiac side effects-lipid peroxidation
Topoisomerase type 2 inhibitor

Question 7

Mitoxantrone

Answer 7

Non-covalently intercalated DNA
Does not create free radicals
Breast cancer, acute myloid leukaemia
Also Topoisomerase type 2 inhibitor

Question 8

Methotrexate

Answer 8

Anti-metabolite
Inhibits dihydrofolate reductase used in folic acid synthesis
Competes with folic acid for transport into cell
Prevents purine and thymidylate synthesis

Question 9

Leucovorin

Answer 9

Salvage healthy tissue from folic acid depletion following methotrexate use
N-formyl-tetrahydrofolate therefore used as alternative substrate at low levels
Doesn’t provide high enough demand for rapidly dividing cells

Question 10

5-Fluorouracil

Answer 10

Analogue of D-UMP
Inhibits thymidylate synthase and hence pyrimidine synthesis
Colorectal cancer

Question 11

Topotecan

Answer 11

Topoisomerase type 1 inhibitors

Topoisomerase type 1 forms single strand breaks to allow the local unwinding of sections of DNA for replication and transcription

Question 12

Campothecins

Answer 12

Topoisomerase type 1 inhibitors

Topoisomerase type 1 forms single strand breaks to allow the local unwinding of sections of DNA for replication and transcription

Question 13

Etoposides

Answer 13

Topoisomerase type 2 inhibitor

Topoisomerase type 2 causes double strand breaks in DNA for local unwinding

Question 14

Vinblastine

Answer 14

Vinca-Alkaloid

Bind to free tublin dimers leading to disassembly of microtubules

Question 15

Vincristine

Answer 15

Vinca-Alkaloid

Bind to free tublin dimers leading to disassembly of microtubules

Question 16

Taxol

Answer 16

Binds to microtubule structures and prevents their disassembly

Question 17

Tamoxifen

Answer 17

Competitively binds to oestrogen receptor and antagonises it - inhibits cell proliferation
Successful in 70% breast cancers
Agonist for receptor in uterus however - increases endometrial proliferation TOREMIFENE better

Question 18

Anastrozole

Answer 18

Aromatase antagonist - oestrogen synthesis

Question 19

Flutamide

Answer 19

Competitive testosterone antagonist

Question 20

Goseraline

Answer 20

Strong GnRH agonist, initially causes testosterone release through LH but sustained activation leads to completely inhibition

Question 21

Prednisone

Answer 21

Pro-drug converted into prednisolone in the liver
Glucocorticoid
Lymphocytolytic
Used against lymphoblastic leukaemia

Question 22

Trastuzumab

Answer 22

Monoclonal antibody
Binds to extra cellular surface of HER2 and prevents growth factor binding

(HER2 overexpressed in 20-30% breast cancers)

Question 23

Cetuximab

Answer 23

Monoclonal antibody
Targets extra cellular domain of epidermal growth factor receptor 1 and prevents ligand binding
Colorectal and head and neck cancers

Question 24

Bevacizumab

Answer 24

Monoclonal antibody against VEGF
Prevents angiogenesis
Lung, breast and metastatic colorectal cancer

Question 25

Imatinib

Answer 25

Small molecule inhibitor of BCL-ABL tyrosine kinase

Inhibits tyrosine kinase of c-KIT mutations seen in GI stomach tumours

Question 26

Erlotinib

Answer 26

Small molecule inhibitor of EGFR tyrosine kinase

Lung cancers

Question 27

Mastinib

Answer 27

Small molecule inhibitor
Veterinary use
Against Mast cell tumours and tyrosine kinases

Question 28

Cyclophosphamide

Answer 28

Covalently binds DNA, forms cross links between strands
Nitrogen Mustard
Cross links between Guanine and either another guanine or other nucleophilic groups
Lymphoid tumours, breast, lung and ovary carcinomas
Must first be activated by cytochrome p450
Forms imonium ion in alkaline or neutral Ph, becomes carbonium ion the reacts with guanine