Chemo Drugs

Question 1

Alkylating Agents Classes

Answer 1

Nitrogen mustards
Nitrosureas
Platinum Drugs
Miscellanous

Question 2

Nitrogen Mustards

Answer 2

Melphalan, Cyclophosphamide, Ifosfamide, Chlorambucil and Estramustine

Men Can Inject Cocaine Everday

Question 3

Nitrosureas

Answer 3

Carmustine, Lomustine, Nimustine and Streptozocin (Streptozotocin

“Ustines” and streptozocin

Question 4

Platinum Drugs

Answer 4

Carboplatin, Cisplatin, and Oxaliplatin

“Platins”

Question 5

Miscellanous Alkylating Drugs

Answer 5

Busulfan, Procarbazine

Question 6

Nitrogen Mustards MOA

Answer 6

• Link two Guanine molecules together causing DNA damage

(Azridium intm. –> Chloro)

N-7 Alkylation

Question 7

Nitrosurea Alkylating Agents MOA

Answer 7

• Have a chloroethyl group that attaches to oxygen on Guanine
• 06 alkylation

Question 8

Streptozcin MOA

Answer 8

• Has a methyl group
• Get an O6 methylation to Guanine

Question 9

Platinum Alkylating Agents MOA

Answer 9

• Alkylate and cross link (inter or intra) two Guanine molecules
• DNA damage –> N7 alkylation

Question 10

Bulsulfan MOA

Answer 10

Remove mesylate (CH3SO3-) to form R–CH2+

Cause intra- and inter-crosslink of DNA molecules

N7 alkylation

Question 11

Procarbazine MOA

Answer 11

Form methyldiazonium ion (CH3-N+≡N) and methyl cation (CH3+)

Nonspecific alkylating agent which methylates guanine at O6

Question 12

Antimetabolite Examples And…..

Answer 12

5-Fluorouracil (5-FU), capecitabine, gemcitabine, cytarabine and azacitidine

“ines”

Question 13

Antimetabolite MOA

Answer 13

Incoporate into the double strand of the DNA molecule  Cause breaks  Destroy the DNA molecules

Miscoding due to incorporation into DNA/RNA (incorporation into DNA molecule)

Question 14

Antimitotics Examples

Answer 14

Taxanes

Paclitaxel
Docetaxel

“axes”

Question 15

Antimitotic MOA

Answer 15

Bind to free tubulin (mitotic spindle) –> Stable bonding
Produce stable microtubules
Inhibit microtubule disassembly (spindles stick)

Question 16

Vinca Alkyloids Examples

Answer 16

Vinblastine, vincristine, vindesine and vinorelbine

“Vin”

Question 17

MOA Vinca Alkyloids

Answer 17

Prevent microtube polymerization

• Do not allow microtubule to form spindle

Inhibit formation of mitotic spindle

Question 18

Antitumour Antibiotics Examples

Answer 18

• Antracyclines
• DNA intercelating agents

Daunorubicin, doxorubicin, epirubicin, idarubicin and mitoxantrone

“ubicins”

Question 19

Anthracyclines MOA

Answer 19

Intercalate with DNA perpendicular to its longitudinal axis
Cause single and double stranded DNA cleavage

Question 20

PARP Inhibitors MOA

What does PARP Stand for?

Answer 20

Involved in DNA repair (inhibit DNA repair)

PARP: Poly (ADP-ribose) polymerase

Question 21

PARP Inhibitor Examples

Answer 21

Olaparib, rucaparib, niraparib, iniparib and talazoparib

“paribs” suffix

Question 22

PARP Inhibitors MOA

Answer 22

Block DNA repair in cancer cells and cause cancer cell death

Question 23

Targeted Tx Agents

Answer 23

• Tyrosine Kinase Inhibitors

Monoclonal Antibodies

Apoptosis Inducing Agents

Angiogenesis Inhibitors

Question 24

Tyrosine Kinase Inhibitor Examples

Answer 24

Imatinib, Gefitinib, Ibrutinib

“inibs”

Question 25

Monoclonal ANtibodies Examples

Answer 25

Prastuzumab, Pertuzumab, T-DM1, Bevacizumab, Rituximab "umabs"

Question 26

Apoptosis Inducing Examples

Answer 26

Bortezomib, Oblimersen (nucleotide drug), THINK O's

Question 27

Angiogenesis Inhibitors

Answer 27

Bevacizumab, Sunitinib

Question 28

Tyrosine Kinase Inhibitor MOA

Answer 28

Tyrosine kinase (TK) domain is present in growth factor receptors, such as epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR), and signaling protein kinases such as Ras and Raf - Inhibit angiogensis

Question 29

Immatinib MOA

Answer 29

Tyrosine-Kinase Inhibitor Inhibit BCR-ABL tyrosine kinase Inhibit proliferation and induce apoptosis in BCR-ABL positive cells

Question 30

Gefitnib MOA

Answer 30

Inhibitor of epidermal growth factor receptor (EGFR) Signaling via EGF-EGFR promotes DNA synthesis, proliferation, migration and survival

Question 31

Monoclonal Antibodies MOA

Answer 31

Bind to subdomain IV of Her2 protein

Question 32

Pertuzumab MOA

Answer 32

Monoclonal antibody binds to subdomain II of Her2 protein Block homodimerization of Her2 and heterodimerization of Her2-Her3 - Inhibit Her2-signaling pathway and decrease cell growth THINK ER

Question 33

Bortezomib MOA

Answer 33

Proteasome inhibitor and apoptosis-inducing agent Bind to 26S proteasome, prevent proteosome-mediated degradation of pro-apoptotic factors and induce apoptosis

Question 34

Bevacizumab MOA

Answer 34

- Starve Cancer cells - Anti-angiogenesis monoclonal antibody blocking vascular endothelial growth factor (VEGF) - VEGF and its receptors (VEGFR) can induce and promote angiogenesis (take out either one)

Question 35

Sunlitib MOA

Answer 35

Multiple-targeted tyrosine kinase inhibitor Inhibit VEGFR, platelet-derived growth factor receptor (PDGFR), colony stimulating factor receptor (CSFR) and tyrosine-protein kinase KIT (CD117) Angiogenesis inhibitor Sun --> Star --> Millions

Question 36

PD-1 Mechanism

Answer 36

programmed cell death protein 1 (CD279) Surface protein on T-cells Prevent T-cells from killing other cells upon binding PD-L1 Check immune responses

Question 37

PD- L1 Mechanism

Answer 37

programmed cell death ligand 1 (CD274 or B7-H1) Transmembrane protein Prevent T-cells from killing PD-L1-containging cells

Question 38

PD-1 and PD-L1 Cancer Mechanism. Prevent cancer?

Answer 38

PD-L1 binds to PD-1 and inhibits T-cell killing of tumour cell Blocking PD-L1 allows T cell killing of tumour cell

Question 39

Pd-1 Inhibitors

Answer 39

Pembrolizumab Nivolumab Cemiplimab

Question 40

PD-L1 Inhibitors

Answer 40

Atezolizumab Avelumab Durvalumab

Question 41

Tamoxifen MOA and What is it?

Answer 41

- Block ER and inhibit breast cancer cell growth May slightly increase the chance of getting uterine cancer (ER in breast to block function, if goes to uterus activates ER) - Hormonal Tx Think TAMMY

Question 42

How do hormones promote cancer?

Answer 42

Hormones can bind estrogen receptor (ER) and progesterone receptor (PR) to promote cancer cell growth