Breast Cancer Drug Mechanisms

Question 1

Raloxifene

Answer 1

SERM

Binds to ERs, where it has agonist/antagonist actions depending on the tissue

Estrogenic on bone
Anti-estrogenic on breast

Question 2

Tamoxifen

Answer 2

SERM

Binds to ERs, where it has agonist/antagonist actions depending on the tissue

Estrogenic on bone, uterus
Anti-estrogenic on breast

Question 3

Ademaciclib (Verzenio)

Answer 3

CDK 4/6 inhibitor -> prevents phosphorylation/inactivation of Rb protein -> prevents DNA transcription by E2F needed for DNA replication

Question 4

Methotrexate

Answer 4

Antimetabolite

Inhibits dihydrofolate reductase -> dec. active folate -> dec. thymidine -> dec. DNA synthesis

Question 5

Paclitaxel Albumin-stabilized Nanoparticle Formulation (Abraxane)

Answer 5

Microtubule inhibitor

Albumin carries paclitaxel into tumor interstitium via albumin-activated gp60 pathway

Question 6

Ado-Trastuzumab (Kadcyla, TDM1)

Answer 6

Trastuzumab binds to HER2 receptor -> flags cells for immune destruction, decreases intercellular HER2-directed growth pathways

Emtansine is a microtubule inhibitor

Question 7

Everolimus (Afinitor)

Answer 7

mTOR inhibitor -> dec. cell proliferation

Hypoxia-inducible factor inhibitor -> dec. VEGF

Question 8

Anastrozole (Arimidex)

Answer 8

Aromatase inhibitor

Question 9

Capecitabine (Xeloda)

Answer 9

Antimetabolite

Prodrug converted to 5-FU -> thymidylate synthetase inhibitor -> dec. thymidine -> dec. DNA synthesis

Question 10

Cyclophosphamide (Cytoxan)

Answer 10

Alkylating agent

Creates crosslinks between DNA -> dec. DNA synthesis

Question 11

Docetaxel (Taxotere)

Answer 11

Microtubule inhibitor

Hyperstabilizes microtubules -> prevents microtubule disassembly -> dec. cell division

Question 12

Doxorubicin (Adriamycin)

Answer 12

DNA intercalater -> prevents DNA/RNA polymerase from attaching to base pairs

Topoisomerase II inihbitor

Question 13

Epirubicin (Ellence)

Answer 13

DNA intercalater -> prevents DNA/RNA polymerase from attaching to base pairs

Topoisomerase II inihbitor

Question 14

Eribulin (Halaven)

Answer 14

Microtubule inhibitor

Question 15

Exemestane (Aromasin)

Answer 15

Steroidal aromastase inhibitor

Question 16

Letrozole (Femara)

Answer 16

Non-steroidal aromatase inhibitor

Question 17

Gemcitabine (Gemzar)

Answer 17

Thymidylate synthetase inhibitor -> dec. thymidine -> dec. DNA synthesis

Question 18

Goserelin (Zoladex)

Answer 18

Synthetic analogue of LHRH -> Inhibition of pituitary gonadotropin secretion -> dec. LH -> ovarian suppression of E

Question 19

Trastuzumab (Herceptin)

Answer 19

Binds to Her2 -> flags cells for immune destruction, decreases intercellular HER2-directed growth pathways

Question 20

Palbociclib (Ibrance)

Answer 20

CDK 4/6 inhibitor -> prevents phosphorylation/inactivation of Rb protein -> prevents DNA transcription by E2F needed for DNA replication

Question 21

Ixabepilone (Ixempra)

Answer 21

Microtuble inhibitor

Question 22

Ribociclib (Kisqali)

Answer 22

CDK 4/6 inhibitor -> prevents phosphorylation/inactivation of Rb protein -> prevents DNA transcription by E2F needed for DNA replication

Question 23

Lapatinib (Tykerb)

Answer 23

4-anilinoquinazoline kinase inhibitor of EGFR and EGFR type 2 -> inhibits ErbB-driven growth

Question 24

Neratinib (Nerlynx)

Answer 24

Irreversibly binds to EGFR, Her2, and Her4 -> prevents autophosphorylation of tyrosine on receptors -> dec. oncogenic signaling

Question 25

Paclitaxel (Taxol)

Answer 25

Microtubule inhibitor

Question 26

Pertuzumab (Perjeta)

Answer 26

Binds to Her2 receptors -> inhibit interaction with other Her family members

Question 27

Vinblastine

Answer 27

Microtubule inhibitor

Question 28

Carboplatin

Answer 28

Alkylating agent Creates crosslinks between DNA -> dec. DNA synthesis

Question 29

Cisplatin

Answer 29

Alkylating agent Creates crosslinks between DNA -> dec. DNA synthesis

Question 30

Liposomal doxorubicin (Doxil)

Answer 30

DNA intercalater -> prevents DNA/RNA polymerase from attaching to base pairs Topoisomerase II inihbitor

Question 31

Vinorelbine

Answer 31

Microtubule inhibitor