Anticancer Drugs Flashcards
What is the mechanism of action of alkylation agents?
Are alkylating agents cell cycle phase specific?
They cause formation of covalent bonds between DNA, so cause DNA damage due to intrastrand cross linking.
No.
Name 2 bifunctional alkylating agents.
Name 2 monofunctional alkylating agents.
Cyclophosphamide, Chlorambucil, Mephalan.
Dacarbazine, Busulfan, Hydroxycarbazine, Procarbazine.
What is the mechanism of action of anthracyclines?
Are anthracyclines cell cycle phase specific?
Give 2 examples of anthracyclines.
They inhibit DNA/RNA synthesis. They complex with DNA through intercalation with base pairs and inhibit topoisomerase II activity by stabilising the Topoisomerase II complex.
They are not cell cycle specific.
Epirubicin/ Doxorubicin.
What class of drug is paclitaxel?
What is the mechanism of action for paclitaxel?
What conditions is Paclitaxel 1st line treatment for?
Plant derivative acting as a microtubulebstabilisation agent.
Hyperstabilisation of the microtubule, preventing is from undergoing disassembly and preventing spindle formation.
Advanced ovarian carcinoma and breast cancer.
What class of drug is Tamoxifen?
What is the mechanism of action of Tamoxifen?
Selective oestrogen receptor modulator.
Binds to oestrogen and causes a conformational change which alters the expression of oestrogen dependant genes.
What are pyramiding analogues also known as?
Name a pyramiding analogue.
What is the mechanism of action of pyramiding analogues?
Are pyrimidine analogues cycle specific?
Anti-metabolites.
5- fluorouracil.
Inhibit Thymidine synthesis.
S phase specific.
What class of drug is Etoposide?
What is the mechanism of action of etoposide?
Is Etoposide cell cycle phase specific?
DNA topoisomerase II inhibitor.
Inhibit topoisomerase II and so inhibits DNA are-ligation.
Effects mainly S and G2 phases.
What class of drug is vinblastine?
What is the mechanism of action of vinblastine?
Is vinblastine cell cycle phase specific?
Vinca alkaloid - Tubulidentata polymerase inhibitor.
Causes crystallisation of microtubules at the mitotic spindle, leading to mitotic arrest and cell death.
Yes - inhibits mitosis at metaphase.
What class of drug is Imatinib?
What is the mechanism of action of imatinib?
Is imatinib cell cycle phase specific?
Name another drug in the same class as Imatinib.
What condition is Imatinib used to treat?
Tyrosine kinase inhibitor.
Targets BCR-ABL tyrosine kinase, and inhibition of this causes inhibition of cell proliferation and induces apoptosis.
No.
Ruxolitinib.
CML.
Name a vitamin A analogue.
What is the mechanism of action of vitamin A analogues?
What are vitamin A analogues used to treat?
Tretinoin.
Bind to alpha, beta and gamma retinoic acid receptors, to decrease proliferation of APL cells.
Acute promyelocytic leukaemia.
What does Rituximab inhibit?
What is the mechanism of action of rituximab?
What is rituximab used for?
What does Trastuzamab bind to and what does this do?
CD20 antigen.
Binds to CD20 antigens on normal and malignant B lymphocytes.
Used for non-Hodgkin lymphoma, chronic lymphocytic leukaemia.
Anti-EGF, EGF-2 monoclonal antibody.
What is the general mechanism of action of monoclonal antibodies?
What is Ruxolitinib used alongside for rheumatoid arthritis?
Binding of the antibody to the target activates hits immune responses and cancer cells are killed, or attach to and inactivate growth factors or receptors. So overall, they inhibit the survival pathway.
Used alongside methotrexate.
