Anti cancer Drugs 3 Flashcards
Fulvestrant is an SERD (selective estrogen receptor downregulators). What is its mechanism
Binds to ER and inhibits its dimeriztain and increases its degradation
The only source of estrogen in post menopausal women is from the ocversoin of _________ to _______ by _________
Androstenedione; estrone; aromatase
Aromatase inhibitors are the used for ________
Adjuvant therapy for post menopausal women with hormone receptor positive breast cancer
Nonsteroidal aromatose inhibitors
Anastrozole and letrozole Reversible competitive inhibitor of aromatase
Steroidal aromatase inhibitors
Exemestane Irreversible inhibitor of aromatase
Examples of GnRH agonists and what do they do?
goserelin and leuprolide They cause an initial surge in LH and FSH followed by an inhibition of gonadotropin release
To prevent the intital increase of testosterone when administering GnRH agonsts, give _______
Flutamide
Mechanism of flutamide
It is a non steroidal anitandrogen that is a competitive antagonist at the androgen receptor
Mechanism of imatinib
Inhibitor fo tyrosine kinase of Bcr-Abl
Mechanism of Trastuzumab
Monoclonal antibody against ErB2
Mechanism of asparaginase
It hydrolyzes serum asparagine and thus depriving the tumor cells of the asparagine that is necessary for protein synthesis (Neoplastic tissues require exogenous source of asparagine)
Adverse effects of asparaginase
HS, ↓ in clotting factors (but paradoxically have more thrombotic events), liver abnormalities, pancreatitis (asparaginase can activate enzymes while they are in the pancreas), and seizures and coma due to ammonia toxicity
Hydroxyurea inhibits ______ causing …
Ribonucleotide reductase; depletion of deoxynucleoside triphasophate pools and thus arresting DNA synthesis /
Hydroxyurea kills cells in the ____ phase
S
Interferon α is used to treat:
- hairy cell leukemia - CML - malignant melanoma - kaposi sarcoma
Mechanism of interferon α
- increase the expression of HLA molecules on tumor cells so they can be destroyed - activates NK cells to destroy tumor cells
Mechanism of vinca alkaloids
Binds to β tubulin and hinhits it’s ability polymerize to microtubules and cells arrest in metaphase and die by apoptosis
Adverse effects of vincristine
Peripheral neuropathy with MILD bone marrow depression
Adverse effects of vinblastine
Myelosuppresion is the dose limiting diverse effects and other adverse effects include alopecia and peripheral neuropathy
What is the difference in adverse effects between vincristine and vinblastine?
Vincristine has mild bone marrow suppression while that is the dose limiting adverse effect for vinblastine Vincristine has much worse peripheral neuropathy
Mechanism of taxaxes (paclitaxel and docetaxel)
Bind to β tubules but they allow for the polymerization of microtubules but PREVENTS DEPOLYMERIZATION
What is the difference between the mechanism of vinca alkaloids and taxanes?
Vinca alkaloids do not allow for the polymerization of the microtubules while taxanes do but with taxanes no depolymerization
Adverse effects of paclitaxel
HS, myelosuppresoin, peripheral neuropathy and alopecia
Adverse effects of docetaxel
Peripheral neuropathy is not as bad as in paclitaxel
_________ is required to prevent fluid retention when taking docetaxel
Dexamethasone
__________ is dose limiting in docetaxel
Myelosuppresion
Etoposide inhibits _____________ and blocks the cell at _______
Topoisomerase II (breaks DNA on BOTH strands) S-G2 phase
Campothecins inhibits _____________
Topoisomerase I
Prednisone is used for ___________ and what is its mechanism
Acute leukemia and malignant lymphomas Prednisone is a glucocorticoid and they are lymphocytic and suppress mitosis in lymphocytes
Selective estrogen receptor modulators act as agonists on _______ and as antagonists on ________
Bone, endometrium; breast
Tamoxifen is an _________ on breast cancer and is used for ____________ breast cancer
Antagonist; receptor positive
Raloxifene is a SERM that acts as an ___________ on the bone to inhibit ________
Agonist; resorption
_________ is a SERM that does not have risk for endometrial cancer when using it
Raloxifene
What are some uses for raloxifene?
Prevention of post menopausal osteoporosis and prophylaxis of breast cancer in high risk post menopausal women