Anti-Cancer Flashcards
Melphalan
Covalent oh cross links DNA
Nitrogen Mustard
Accumulates in tissues - increasing sensitivity for melanoma cells as is an L-Phenylalanine (melanin precursor)
Carmustine
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
Lomustine
ANitrosourease
Alkylate carbomoylates and cross-links DNA
Lipophillic therefore can be used for brain tumours
Cause reduction in circulating rbc’s and platelets
Cisplatin
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
Daunomycin
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
Actinomycin D
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
Mitoxantrone
Non-covalently intercalated DNA
Does not create free radicals
Breast cancer, acute myloid leukaemia
Also Topoisomerase type 2 inhibitor
Methotrexate
Anti-metabolite
Inhibits dihydrofolate reductase used in folic acid synthesis
Competes with folic acid for transport into cell
Prevents purine and thymidylate synthesis
Leucovorin
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
5-Fluorouracil
Analogue of D-UMP
Inhibits thymidylate synthase and hence pyrimidine synthesis
Colorectal cancer
Topotecan
Topoisomerase type 1 inhibitors
Topoisomerase type 1 forms single strand breaks to allow the local unwinding of sections of DNA for replication and transcription
Campothecins
Topoisomerase type 1 inhibitors
Topoisomerase type 1 forms single strand breaks to allow the local unwinding of sections of DNA for replication and transcription
Etoposides
Topoisomerase type 2 inhibitor
Topoisomerase type 2 causes double strand breaks in DNA for local unwinding
Vinblastine
Vinca-Alkaloid
Bind to free tublin dimers leading to disassembly of microtubules
Vincristine
Vinca-Alkaloid
Bind to free tublin dimers leading to disassembly of microtubules
Taxol
Binds to microtubule structures and prevents their disassembly
Tamoxifen
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
Anastrozole
Aromatase antagonist - oestrogen synthesis
Flutamide
Competitive testosterone antagonist
Goseraline
Strong GnRH agonist, initially causes testosterone release through LH but sustained activation leads to completely inhibition
Prednisone
Pro-drug converted into prednisolone in the liver
Glucocorticoid
Lymphocytolytic
Used against lymphoblastic leukaemia
Trastuzumab
Monoclonal antibody
Binds to extra cellular surface of HER2 and prevents growth factor binding
(HER2 overexpressed in 20-30% breast cancers)
Cetuximab
Monoclonal antibody
Targets extra cellular domain of epidermal growth factor receptor 1 and prevents ligand binding
Colorectal and head and neck cancers
Bevacizumab
Monoclonal antibody against VEGF
Prevents angiogenesis
Lung, breast and metastatic colorectal cancer
