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