Cancer Drugs - Exam 3 Flashcards
Cyclophosphamide
(Cytoxan, Neosar)
Alkylating Agents
Nitrogen mustards
Most widely used
alkylating agent!
Mech: Binding to guanine molecules to
prevent separation
of DNA strands
pro drug
Use: not vesicant, admin IV or PO
SE: ACUTE
HEMORRHAGIC
CYSTITIS!!!
Admin w/ Mesna
(Mesnex) and adequate hydration!
-Bone marrow
suppression!
Dose limiting
Notes:
Carmustine
(BiCNU, Gliadel)
Nitrosureas
(Alkylating agent)
Mech: Bifunctional alkylating compound
Highly lipophilic
(good crossing BBB)
Use:
SE: Bone marrow
suppression!
Dose limiting
Notes:
Cisplatin
(Platinol-AQ)
Platinum compounds
(-platin)
Mech: Forms cross-links
btwn DNA strands
Use: 1st line therapy for
ovarian cancer and
non-small cell lung
cancer
SE: -Kidney damage
(reduced w/
hydration,
diuretic)
-Severe nausea,
Vomiting
-Peripheral
neuropathy
Notes:
Methotrexate
(Rheumatrex, Trexall)
Folic Acid Analogs
Antimetabolites
Mech: Inhibits an enzyme
in folic acid activation , cannot synth folic acid!
S Phase specific!
Use: High dose admin to
be effective against
cancer cells!
Leucovorin given to
help protect normal
cells
SE: -Bone marrow
suppression
-Kidney damage
-Fetal
malformation
Cytarabine
(cytosine arabinoside
or Ara-C)
Pyrimidine analogs
(cytosine, uracil, Thymine)
Mech: Incorporated into DNA, suppresses further DNA synth
S phase specific!
Use:
SE: Bone marrow suppression!
Pulmonary edema
Liver damage
Kidney damage
Mercaptopurine
(Purinethol)
Prodrug , activated in cells
Purine analogs
(Adenine, Guanine)
Mech: Incorporated into DNA, suppresses further DNA synth
S phase specific
Use:
SE: Bone marrow suppression
Mild hepatotoxicity
Etoposide
(Toposar)
Topoisomerase inhibitors
Mech: Permits cleaving of the DNA but does not permit
repair! Cell death occurs due to accumulation of DNA with multiple breaks
Use: Protein binding HIGH (will increase serum level of warfarin, SSRI, etc. )
SE: Bone marrow suppression
Doxorubicin
(adriamycin) – conventional
Doxorubicin
(Doxil, Caelyx) – liposomal
Rubicin = red in color! RED DEVIL
Anti-tumor antibiotics Anthrocyclines
Mech: Intercalation with DNA, slips btwn base pairs and
distorts structure of DNA
Use: Liposomal assoc w/ infusion reactions but more likely to
just target cancer cells
SE: Infusion reaction with liposomal form!
Dactinomycin
(Actinomycin D)
Non-anthracyclines
Mech: Intercalates w/ DNA & distorts structure, inhibits RNA & protein synthesis
SE: Bone marrow suppression
Vincristine
Vinca alkaloids
Mitotic Inhibitors
(Vin-)
Mech: Block mitosis during metaphase
Disrupts assembly of microtubules by binding to tubulin
Cell stops in metaphase = apoptosis
Use: ** BONE MARROW SPARRING!!**
SE: Peripheral neuropathy!
Dose-limiting tox!
Disrupts neuro-tubules in neurons!
Vinblastine
(Veblan)
Mech: Block mitosis during metaphase
Disrupts assembly of microtubules by binding to tubulin
Cell stops in metaphase = apoptosis
SE: neurotoxicity less common, less severe than vincristine
Bone marrow suppression dose limiting
Paclitaxel
(Abraxane, Taxol)
Taxanes
Mech: Promotes formation of microtubule bundles
Inhibits cell division
Promotes apoptosis
SE: Severe hypersensitivity reaction with Taxol!
Pre treat w/ H2 blocker, antihistamine, glucocorticoid
-Bone marrow
suppression may
be dose limiting!
Asparaginase
(Elspar)
Mech: Asparaginasae is an enzyme that converts
asparagine into aspartic acid.
Asparagine is an essential amino acid Needed for protein synth!
Use: Limited to Acute Lymphoblastic Leukemia (ALL)
SE: Coagulation deficiencies,
Liver, kidney, pancreas damage
Tamoxifen
(Nolvadex)
Gold standard
for endocrine tx
of breast cancer
Anti-estrogens
Mech: Prodrug that is converted into active form by CYP450
Blocks estrogen receptors , deprive tumor cells of growth promoting influence of estrogen
Activates estrogen receptors in bone, liver, uterus
SE: Increased risk of endometrial cancer and thrombosis!
-Menopause like symptoms
Use of CYP450 inhibitors can negate effect of tamoxifen
Anastrozole
(Arimidex)
Aromatase inhibitors
Mech: Adrenal androgens converted into estrogen by
Aromatase in peripheral tissues
Use: ER pos breast cancer in POSTMENOPAUSAL WOMEN !!
SE: Musculoskeletal pain
Osteoporosis and fractures
Trastuzumab
(Herceptin)
Anti-Human
Epidermal Growth
Factor Receptor 2
(HER2) Antibodies
(-tuzumab)
Mech: Mab that blocks HER2 receptors
- inhibits proliferation
- promotes abx dependent cell death
Use: HER2 pos BC in pre/post menopausal women
SE: Cardio toxicity = arrhythmias & HF
-Flu like
symptoms
(Fatigue, chills,
fever, nausea)
-Potentially fatal
hypersensitivity
reaction
Lapatinib
(Tykerb)
Kinase inhibitor
Mech: inhibits 2 enzymes involved in cell signal transduction = blocks signal that promotes growth of the tumor
Use: HER2 pos BC ONLY!
SE: Diarrhea, nausea, vomiting, Fatigue
Leuprolide
(Eligard, Lupro)
Synthetic analog of GnRH
GnRH agonists
Mech: INITIALLY cause release of hormones that stim INCREASED prod of testosterone, flares symptoms and growth. W/ continued exposure, GnRH receptors become desensitized and less testosterone is produced.
Co admin with androgen receptor blocker Flutamide to reduce the flare!
SE: Erectile dysfunction
Reduced libido
Gynecomastia
Degarelix
(Firmagon)
GnRH antagonist
Mech: Block the GnRH receptors in pituitary
– Reduces production of hormones that stimulate
the testes to produce testosterone
– NO INITIAL FLARE OF PROSTATE CANCER
Use: Used for adv prostate cancer, admin SQ
SE: not enough testosterone = ED, Reduced libido, Gynecomastia
Flutamide
Androgen receptor antagonist
Mech: blocks androgen receptors
Use: only indicated for prostate cancer, often admin w/ GnRH agonist
SE: Not enough testosterone = ED, reduced libido, Gynecomastia
Abiraterone
(Zytiga)
CYP17 inhibitor
Mech: inhib of CYP17, an enzyme necessary for androgen synthesis
Use: in combination with prednisone to treat METASTATIC castration-resistant prostate cancer
SE: Not enough testosterone = ED, reduced libido, Gynecomastia, hypokalemia, edema
Bevacizumab
(Avastin)
Angiogenesis inhibitors
Mech: Monoclonal ab!
Binds to VEGF (compound that stims vessel prolif)
-cannot bind to receptors on vascular endothelium that promote vessel growth
– New vessel growth does not occur
Use: deprive solid tumors of blood supply. CANNOT KILL TUMORS THAT ALREADY EXIST!
SE: GI perforation and/or thromboembolism
**If occurs STOP drug and never use again! **
Hemorrhage in brain, lung, GI, vagina
