Anti-cancer Flashcards
6-MP activation
HGPRT
6-MP breakdown
XO
6-MP toxicity
myelosuppression, hepatotoxicity (hepatitis and cholestasis)
Increase 6-MP toxicity via:
alloputinol or febuxostat (block XO)
6-MP MOA
Purine analog
Cladiribine MOA
purine analog
Rx of Hairy cell
Cladribine
Cladribine toxicity
myelo, nephrotoxicity, neurotoxicity
Cytarabine MOA
pyrimidine analog
Cytarabine AE
panCYTopenia (leuko, thrombo, megaloblastic anemia)
5-FU MOA
pyrimidine analog; inhibits thymidilate synthase
Purine analogs
6-MP, azathioprine, cladribine
pyrimidine analogs
cytarabine, 5-FU
Leucovorin: when it works and doesn’t work
works for MTX; does NOT work for 5-FU (actually potentiates it)
MTX MOA
folic acid analog; competitively inhibits DHF reductase
MTX Rx
cancers: leukemiaa (ALL), lymphomas, chorioCA, sarcomas.
Non-neoplastic: ectopic pregnancy (medical abortion), RA, psoriasis, IBD, vasculitis.
MTX AE
myelo (rx = leucovorin), hepatoxoicity, mucocytis, pulmonary fibrosis
hydroxyurea MOA
inhibits ribonucleotide reductase
S-phase drugs
6-MP, 6-TG, azathioprine, cladribine, cytarabine, 5-FU, MTX, hydroxyurea
Anti-tumour ABx
Bleomycin, dactinomycin, doxorubicin, danaurubucin
Bleomycin MOA
Free-radical -> DNA strand breaks
Bleomycin AE
Pulmonary fibrosis, skin hyper pigmentation, mucocytis, *MINIMAL myelosuppresion
Doxo/daunorubicin MOA
Intercalates into DNA -> breaks + free radicals
doxo/daunorubicin AE
dilated cardiomyopathy, alopecia
doxo/daunorubicin AE Rx
Dexrazoxane
Dactinomycin MOA
intercalates
Dactinomycin use
Child tumours (wilms, ewing, rhabdomyosarcoma)
akylating agents act on what stage of cell cycle?
G1
Name all alkylating agents
Busulfan, cycloforfamide, isofosfamide, nitrosureas (___mustanes + streptozocin)
Busulfan MOA
cross-links
busulfan AE
pulmonary fibrosis , hyperpigmentation
busulfan use
CML and ablating pt bone marrow before transplant
cyclophosphamide/isoforphamide MOA
cross-links @ G-N7
cyclophosphamide/isophosphamide AE + Rx
hemorrhagic cystitis; prevent/rx with mesna
nitrosureas (___mustines + streptozocin MOA/use
Bioactivated, cross BBB, crosslink DNA. BBB .: rx brain tumours (i.e. GBM)
nitrosureas (___mustines + streptozocin AE
CNS effects (confusion, dizzy, ataxia)
paclitaxel MOA
hyperstabilize polymerized MTs .: prevent anaphase
paclitaxel AE
myelo, alopecia, hypersensitivity
vincristine/vinblastin MOA
inhibit b-tubulin polymerization
vincristine AE
neurotoxicity (areflexia, peripheral neuritis, paralytic ileus)
vinblatine AE
myelosuppression
cisplatin/carboplatin MOA
crosslink DNA
Cisplatin/carboplatin AE and Rx
Ototoxicity and nephrotoxicity (prevent with amifortine (free radical scavenger) and chloride saline diuresis
etoposide/teniposide MOA
inhibit topo II –> DNA degradation
irinotecan/topotecan
inhibit topo I (prevent unwinding and replication)
Bevacizumab MOA and AE
MOA = VEGF; AE = bleed, clot, impaired wound healing
Erlotinib
MOA = EGFR
Imatinib MOA
tyrosine kinase of Bcr-Abl and c-kit
imatinib AE
fluid retention
Rituximab MOA
CD20 (so all non-hodgkin lymphomas)
Rituximab AE
PML
Tamoxifen MOA
Antagonist: breast
Agonist: endometrium, bone
Tamoxifen use:
breast cancer prophylaxis AND treatment
Raloxifen MOA
Antagonist: breast and endometrium
Agonist: bone
Raloxifen use:
breast cancer prophylaxis ONLY, OP prevention
Traztuzumab MOA/use
HER-2-nu (c-erb-B2) antibody.
Her-2-nu breast cancer and gastric cancer
HER-2-nu mechanism
tyrosine kinase receptor
Traztuzumab AE
Cardiotoxicity
Vemurafenib MOA
small molecule inhibitor of BRAF
Vemurafenib use
Malignant melanoma