Anticancer Drugs Flashcards
What are the hallmarks of cancer? (6)
Self sufficiency in growth signals
Insensitivity if anti-growth signals
Evading apoptosis
Sustained angiogenesis
Tissue invasion and metastasis
Limitless replicative potential
Cancer therapy requires a multidisciniplary approach. True or false?
True
What are 2 chemotheraphy approaches?
- Attack cells at S phase to inhibit DNA replication
- Attack cells at M phase to inhibit cell division
Cancer chemotherapy is based on principle that cancer cells are actively replicating DNA and actively dividing. True or false?
True
What class of cancer chemotheraphy?
- Structural analog of DNA nucleotide
- Structural analog of molecule needed for production of DNA nucleotides
- Bind DNA and cause DNA damage
S phase blockers
What are the S-phase blockers? (4)
Mercaptopurine
Methotrexate (MTX)
Doxorubicin
Cisplatin
What drug:
S-phase blocker
Used for the treatment of leukemia
Mercaptopurine
What drug:
S-phase blocker
Analog of folic acid
Treatment for ALL breast, lung
Methotrexate
What drug:
S-phase blocker
Damages DNA
Main chemo in breast cancer
Doxorubicin
What 2 drugs cause DNA damage?
Doxyrubicin
Cisplatin
What drug:
S-phase blocker
Damages DNA
Used for ovarian/testicular cancer
Cisplatin
What class of cancer chemotherapy is this:
- Block microtubule polymerization
- Promote and stabilize microtubule polymerization
- Spindle cannot form so chromosomes cannot segregate and mitosis does not occur
M-phase blockers
What M- phase blocker:
• Spindle cannot form so chromosomes cannot segregate and mitosis does not occur
Vinca alkaloids
Examples- vinblastine for breast, NSCLC
What M- phase blocker:
• Spindle is “locked” so chromosomes cannot segregate, mitosis does not occur
Taxanes
Example: paclitaxel
What drug:
- selective estrogen receptor (ER) modulator (SERM) used to treat ER+ breast cancer
- binds ER and blocks estrogen binding
- preventive role for post-menopausal ER+ breast cancer
Tamoxifen
What type of drug:
- This type of medication blocks estrogen formation by binding to aromatase and preventing enzyme activity.
- 2nd line therapy.
aromatase inhibitor
Anastrozole (Arimidex)
What hormonal drugs are used in the treatment of early prostate cancer?
anti-androgens
Early prostate cancer can bind to androgen and acting on the receptor. However, in late stages, cancer does not bind to androgen. True or false?
True
What type of anticancer drugs:
Stimulate the immune system to destroy cancer cells or to minimize toxicities of cancer therapies
Biological response modifiers
What are 3 types of biological response modifiers?
Colony-stimulating factors (CSFs)
Interleukin 2 (IL-2)
Interferons
What are hematopoietic growth factors that stimulate bone marrow stem cells to divide and become platelets, white blood cells, or red blood cells?
Colony stimulating factors (CSFs)
What are adjuvants to high-dose chemotherapy to limit anemia and infection risk? (3)
G-CSF and GM-CSF increase white blood cells, limit infection risk
Erythropoietin increases red blood cells, limits anemia and need for transfusions
What biological response modifier:
- Used mainly for renal cell carcinoma, also in malignant melanoma, colorectal carcinoma
- Stimulates t-cell growth
IL-2 (Aldesleukin)
Note: IL = Interleukin
_______ are endogenous cytokines made and secreted by lymphocytes.
Interferons
What endogenous cytokine:
- Targets immune cells and macrophages
- Is used for hematologic malignancies, including hairy cell leukemia
- Used against AIDS related Karposi’s sarcoma
Interferons
What are 2 types of approved targeted therapies against cancer?
antibodies
tyrosine kinase inhibitors (TKIs)
What targeted therapy has -ib on the end of the drug name ?
tyrosine kinase inhibitors (TKIs)
What targeted therapy has -ab on the end of the drug name?
Antibody
What are 3 important targeted TKIs we should be familiar with?
Imatinib (Gleevec)
Erlotinib (Tarceva)
Gefitinib (Iressa)
What are 2 important targeted monoclonal antibodies we should be familar with?
Trastuzumab (Herceptin)
Bevacizumab (Avastin)
Imatinib is a small molecule tyrosine kinase inhibitor of: (3)
BCR-ABL
C-Kit
PDGFR
What drug is used for patients with:
chronic myeloid leukemia (CML)
GI stromal tumors (GIST) have mutated c-kit
imatinib (Gleevec)
Trastuzumab is a monoclonal antibody against what receptor?
HER2
Note to self: Human Epidermal GF receptor
What type of cancers does trastuzumab target? (2)
breast
gastric
What is the adverse side effect of using trastuzumab alone as treatment?
Cardiotoxicity
