Onc 7

Front 1

Induction therapy

Back 1

- when the tumor is known to be sensitive
- when the feasibility of surgical removal or radiation destruction of the main tumor mass is poor

Front 2

G1 drugs

Back 2

- steriod hormones

Front 3

M drugs

Back 3

- vinca alkyloids
- paclitaxel

Front 4

G2 drugs

Back 4

- bleomycin
- podophyllotoxins

Front 5

S drugs

Back 5

- antimetabolites
- podophyllotoxins

Front 6

CCNS drugs

Back 6

- alkylating agents
- most antibiotics

Front 7

Myelosuppression in chemo

Back 7

- WBC decrease and thrombocytopenia the limiting factors
- G-CSF and GM-CSF being used to accelerate BM

Front 8

antinemetics

Back 8

- agents that affect receptors for NT dopamine (D2) and serotinin (5-HT), which trigger N and V
– 5-HT3 receptor antagonists (Ondansetron)
- dopamine D2-receptor antagonists (prochlorperazine, metoclopramide)

Front 9

most common 2nd malignancy from chemo

Back 9

AML

Front 10

Alkylating agents - mechanism

Back 10

alkylate DNA and cause DNA cross-linking, impairing DNA replication

Front 11

alkylating agents - toxicity

Back 11

- myelosuppression, except cisplatin with renal toxicity
- N and V

Front 12

alkylating agents - resistance

Back 12

- inc repair, dec perm, inc production of glutathione, an inactivator
- if a tumor is resistant to one alkylating agent, it will also be relatively resistant to others

Front 13

Cyclophosphamide

Back 13

- alkylating agent
- nigrogen mustard
- a prodrug, requiring activation by hepatic cytochrome P450 oxidase

Front 14

Nitrosoureas

Back 14

- alkylating agent
- High lipid solubility facilitates CNS entry
- used for brain tumors

Front 15

Cisplatin

Back 15

- alkylating agent
- inorganic metal complex
- low myelosuppression with cisplatin, instead, renal toxicity

Front 16

Antimetabolites - chemistry

Back 16

- synthetic structural analogs of normal cellular components required for DNA synthesis
- CCS - S phase

Front 17

Antimetabolites - toxicity

Back 17

myelosuppression

Front 18

Antimetabolites - resistance

Back 18

altered target, decrease in activating enzyme, decreased intracellular concentration

Front 19

Methotrexate

Back 19

- Antimetabolite
- antagonist of folic acid
- blocks DHFR
- Leucovorin “rescue” (folinic acid admin) can overcome enzyme block and overcome some toxicity
- resistance due to dec drug uptake, mutant DHFR, inc DHFR expression

Front 20

Purine analougs

Back 20

- Antimetabolite
- 6-MP and 6-TG
- require intracellular conversion by HGPRT to 6-TIMP and dTGTP
- resistance usually decreased HGPRT activity

Front 21

5-Fluorouracil

Back 21

- antimetabolite
- pyrimidine analoug
- inhibits thymidylate synthase and leads to thymineless death by blocking DNA synthesis
- activated to 5-FdUMP

Front 22

ara-C

Back 22

- antimetabolite
- pyrimidine analoug
- inhibits DNA polymerase and DNA synthesis
- activated to Ara-CTP

Front 23

Plant Derivatives for chemo

Back 23

- CCS, inhibition of mitotic spindle function
- cause myelosuppression, except vincristine (peripheral neuropathy)

Front 24

Vinca alkaloids

Back 24

- plant alkyloid
- Vinblastine and Vincristine
- CCS (M-phase) bind tubulin
- vincristine causes peripheral neuropathy

Front 25

Podophyllotoxins

Back 25

- plant alkyoid
- Etoposide
- CCS (S/G2), binds and inhibits topoisomerase II religation, resulting in DNA strand breaks

Front 26

Taxanes

Back 26

- plant alkyoid
- Paclitaxel
- bind to tubulin, but promotes polymerization of microtubules

Front 27

Antibiotics for chemo

Back 27

- natural compounds isolated from soil fungus streptomyces
- CCNS

Front 28

Anthracyclines

Back 28

- Antibiotic
- effects topoisomerase II
- causes myelosuppression - also irreversible cumulative cardiac toxicity

Front 29

Bleomycins

Back 29

- Antibiotic
- unlike other antibiotics, CCS (S) , binding to DNA, causing DNA strand breaks by oxygen radical formation
- pulmonary toxicity
- not MDR

Front 30

hormones and chemo

Back 30

- sex hormones stimulate the proliferation of certain tissues
- Lack of severe toxicity to normal tissue

Front 31

Tamoxifen

Back 31

- hormone
- binds estrogen receptor in G1
- confined to palliative treatment of estrogen-dependent, estrogen receptor positive breast cancers

Front 32

Gonadotropin-Releasing Hormone Agonists

Back 32

- hormones
- Leuprolide and Goserelin are analogs of GnRH
- treatment leads to downreg of receptor and loss of stimulation
- redueces testosterone a lot

Front 33

Hydroxyurea

Back 33

- CCS (S-phase) inhibits ribonucleotide reductase

Front 34

L-Asparaginase

Back 34

- converts blood asparagine to aspartic acid for Inhibition of protein synthesis
- can casue allergic reaction

Front 35

Trastuzumab (Herceptin®)

Back 35

- humanized monoclonal Ab that recognizes HER2
- HER2 overexpression is correlated with poor patient prognosis in breast and ovarian cancers
- mild toxicity
- use for breast cancer

Front 36

Gefitinib (Iressa®)

Back 36

- protein tyrosine kinase inhibitor
- Inhibits EGFR/HER1 R TK
- used for lung cancer
- causes rash and diarrhea
- 10% response rate for NSCLC

Front 37

Erlotnib (Tarveca)

Back 37

- Inhibits EGFR/HER1 R TK
- used for Lung And Colon Cancers
- causes rash and diarrhea

Front 38

Cetuximab (Erbitux®)

Back 38

- humanized monoclonal Ab
- Inhibits EGFR/HER1 R TK
- used Colon Cancers
- causes rash and diarrhea
- a 10.8% response - growth delayed by 1.5 months
– if used w/ irinotecan, 22.9% response and growth delayed by 4.1 months

Front 39

Imatinib (Gleevec®)

Back 39

- Inhibition Of The BCR-ABL Tyrosine Kinase on Ph chrom
- used CML and GIST
- Resistance due to mutation of BCR-Abl

Front 40

Bevacizumab (Avastin®)

Back 40

- Inhibition of VEGF Receptor Tyrosine Kinase Activation
- used for Tumor Angiogenesis
-