Drugs Flashcards
carboplatin MOA & AE
intrastrand DNA link
myelosuppression, infection susceptibility
cyclophosphamide MOA & AE
inter- and intrastrand links
myelosuppression, hemorrhagic cystitis (give MENSA prophylatically)
doxorubicin MOA & AE
intercalate, topo II inh, radicals
BM suppression, cardiotoxicity
dactinomycin MOA & AE
intercalator, dna dependent rna syn inh
myelosuppression, hepatic dysfunction, infection susceptibility
etoposide MOA & AE
topo II inhibitor
hematologic toxicity, BP instability
ifosfamide MOA & AE
inter- and intrastrand links
BM suppression, hemorrhagic cystitis (give MENSA prophylatically)
vincristine MOA & AE
blocks MT polymerization
neurotoxicity, “stocking glove”
vHL mutation and RCC
VHL gene functions to mediate ub of HIF to send it to protease to be degraded (controlling mechanism)
w/ VHL mutation, no ub of HIF occurs so it can go on to activate EPO in hypoxic situations (such as new cell growth of tumors)
EPO–>VEGF activation
VEGF and RCC
target VEGF to stop angiogenesis needed for tumor growth
sequence of RCC therapy
- bevacizumab: Ab to VEGF
- -“nib”: TK inhibitor
- everolimus, temsirolimus: block mTOR
*TKI first then mTOR!
Rapamycins
Temsirolimus - weekly IV
Everolimus - daily oral
CYP substrates
bind to FKBP12 and inhibit mTORC1
(caveat: there is mTORC2 that actually promotes new cell growth but there is no drug to block that as of date)
TKIS
axitnib
sunitinib
sorafenib
pazopanib
significant CYP!
VEGFR TK Inhibitors
SE: CV: HTN, thromboembolism, hemorrhagic events, blood dyscrasias
VEGF inh
bevacizumab - IV
thrombo, HTN, CHF, blood dyscrasias
BBW: hemorrhage, gi perfs, wound healing complications!
Immunotherapy IL-2
IL-2 (Aldesleukin) - activates JAK-STAT pathway to turn activate NK cells to kill cancer cells
MOA: IV 3 x week, max 14 dose
“controlled septic shock”
AE: hypotension, tachy, hematologic toxicity, renal toxcity
WATCH FOR SEPSIS
Immunotherapy IFN-alpha
IFN-alpha 2 b - activates JAK-STAT to upreg genes for antiviral, antiproliferative, antitumor activities
AE: BBW - neuropsy, autoimmune, infectious dx
common - flu-like, leukopenia, neutropenia
