Drugs Flashcards
Asatrazole, Letrozole, Vorozole?
Aromatase inhibitors
Who are aromatase inhibitors given to?
Postmenopausal women, ER positive, early stage breast cancer (following radiotherapy)
What is gemcitabine and when is it used?
Antimetabolite used in conjunction with cisplatin to overcome cisplatin resistant ovarian cancer. (Prevents DNA crosslink repair in cancer cells).
What is methotrexate?
An antifolate - binds to DHFR enzyme to inhibit the production of FH4 from FH2. No thymidine/ purine synthesis leads to cell death.
What is Pemetrexate?
CH2FH4 mimetic. Binds to TS enzyme to prevent the formation of FH2. No thymidine synthesis is toxic to cells.
What cancer has pemetrexate had a large success in treating?
Mesothelioma
What is Imatinib?
Small molecule that inhibits the tyrosine kinase domain of the BCR-ABL fusion protein (CML)
What is Rucaparib?
A PARP inhibitor. Single strand breaks persist because PARP function is inhibited. Subsequently, at replication the SSB becomes a DSB; In homologous recombination deficient cells (tumour cells) Mitotic catastrophe takes place as the DSB cannot be repaired.
What type of drugs are BCNU, CCNU and methyl-CCNU?
Chloroethylnitrosureas - alkylating agents which when metabolised form a chloroethyl adduct. If this adducts at O6 and not repaired, it leads to an interstrand crosslink and becomes cytotoxic to a cell.
What are chloambucil, melphalan and mechloroethamine
Nitrogen mustards - alkylating agents (on N7-guanine)
How do platinum drugs induce their cytotoxic effect in cancer cells?
Form a co-ordination complex that is able to produce mono and bifunctional adducts.
What is Doxorubicin>
An intercalating agent that binds DNA in the minor groove.
Which drug is melphalan used to treat?
Multiple myeloma
What is combrestatin?
A vascular disrupting agent - It binds tubulin at established tumour vessels. It blocks endothelial cell proliferation which leads to tumour necrosis (apart form the tumour rim as the vasculature surrounding the tumour is more normal)
What is Vendetanib?
A small molecule that inhibits the tyrosine kinase domain of VEGF2. It also inhibits EGFR and VEGF3