Breast Cancer Drug Mechanisms Flashcards
Raloxifene
SERM
Binds to ERs, where it has agonist/antagonist actions depending on the tissue
Estrogenic on bone
Anti-estrogenic on breast
Tamoxifen
SERM
Binds to ERs, where it has agonist/antagonist actions depending on the tissue
Estrogenic on bone, uterus
Anti-estrogenic on breast
Ademaciclib (Verzenio)
CDK 4/6 inhibitor -> prevents phosphorylation/inactivation of Rb protein -> prevents DNA transcription by E2F needed for DNA replication
Methotrexate
Antimetabolite
Inhibits dihydrofolate reductase -> dec. active folate -> dec. thymidine -> dec. DNA synthesis
Paclitaxel Albumin-stabilized Nanoparticle Formulation (Abraxane)
Microtubule inhibitor
Albumin carries paclitaxel into tumor interstitium via albumin-activated gp60 pathway
Ado-Trastuzumab (Kadcyla, TDM1)
Trastuzumab binds to HER2 receptor -> flags cells for immune destruction, decreases intercellular HER2-directed growth pathways
Emtansine is a microtubule inhibitor
Everolimus (Afinitor)
mTOR inhibitor -> dec. cell proliferation
Hypoxia-inducible factor inhibitor -> dec. VEGF
Anastrozole (Arimidex)
Aromatase inhibitor
Capecitabine (Xeloda)
Antimetabolite
Prodrug converted to 5-FU -> thymidylate synthetase inhibitor -> dec. thymidine -> dec. DNA synthesis
Cyclophosphamide (Cytoxan)
Alkylating agent
Creates crosslinks between DNA -> dec. DNA synthesis
Docetaxel (Taxotere)
Microtubule inhibitor
Hyperstabilizes microtubules -> prevents microtubule disassembly -> dec. cell division
Doxorubicin (Adriamycin)
DNA intercalater -> prevents DNA/RNA polymerase from attaching to base pairs
Topoisomerase II inihbitor
Epirubicin (Ellence)
DNA intercalater -> prevents DNA/RNA polymerase from attaching to base pairs
Topoisomerase II inihbitor
Eribulin (Halaven)
Microtubule inhibitor
Exemestane (Aromasin)
Steroidal aromastase inhibitor