Cancer Flashcards
Cyclophosphamide
MOA: Arrest DNA replication and can result in DNA damage and chromosome breaks
Group: Alkylating agent
Clinical use: Leukemia, non-Hodgkin’s lymphoma, breast and ovarian cancers, neuroblastoma
Cisplastin
MOA: Arrest DNA replication and can result in DNA damage and chromosome breaks
Group: Alkylating agent
Use: Testicular, bladder, lung ovarian cancers
Methotrexate
Group: Anti metabolites
MOA: inhibit DHFR in 1-carbon folate metabolism pathway
6- Mercaptopurine
Group: Anti-metabolites
1) 6-MP metabolized to 6-TIMP by HGPRT, which inhibits PRPP amidotransferase (rate limiting enzyme of purine synthesis)–> depletes purine nucleotide pools, DNA and RNA synthesis are reduced
2) MP converted by ribonucleotide reductase and incorporated to DNA resulting in DNA damage
5-Fluorouracil
Group: Anti-metabolite
MOA: 5-FU metabolized to FdUMP which inhibits Thymidylate Synthase → causes “thymine-less” cell death
- FdUMP converted to FUTP which is incorporated into and damage RNA and DNA
Cytarabine
Group: Anti-metabolite
MOA: competes with dCTP and inhibits DNA polymerases
- Incorporated into DNA triggering apoptosis and strand breaks
Topotecan
Group: Plant alkaloids
Use: advanced ovarian cancer
MOA: Binds and inhibits activity of Topoisomerase I
- DNA damage
Etoposide
Group: Plant Alkaloids
MOA: Binds to Topo II and traps it in drug-Topo II - DNA complex
- DNA strand breakage
Vincristine
Group: Plant Alkaloids
Use: Wilm’s tumor
MOA: Binds to beta tubulin subunit at + end of polymerizing microtubules and prevents addition of alpha/beta dimers at + end
Paclitaxel
Group: Plant alkoid
MOA: Binds to beta-tubulin subunit of MTs at a site distant from vinca alkaloid binding site
- stabilize MTs preventing dynamic assembly→ apoptosis
Doxorubicin
Group: Anti-tumor
MOA: Inhibits Topo II and intercalates between DNA base pairs causing DNA damage and blocking DNA and RNA synthesis
Bleomycin
Group: Anti tumor antibiotics
MOA: DNA binding and iron binding domain
- Binds to DNA→ oxidation of DNA-bleomycin-Fe complex generates free radicals
- Inhibits DNA synthesis
Prednisone
Group: Endocrine targeted agents
MOA: Suppresses cell division at G1/S in lymphocytes→ decrease proliferation
tamoxifen
Group: Endocrine targeted agents
MOA: ER antagonist in breast
Imatinib
Group: Signalling agent
MOA: Small molecule protein tyrosine kinase inhibitor, Potently inhibits Abl tyrosine kinase
- Inhibits hyperactive Abl kinase in the BCR-Abl fusion created by chromosomal translocation
