Cancer drugs Flashcards
purine analogs - decrease de novo purine synth
activated by HGPRT; S phase specific
use: prevent organ rejection, RA, IBD, SLE, wean pt off steroids in chronic disease, tx steroid refractory chronic disease
azathioprine
6-mercaptopurine
6-thioguanine
purine analog - inhibits DNApol, causes DNA strand breaks; S phase specific
used for Hairy cell leukemia
Cladribine
pyrimidine analog - inhibits DNApol; S phase specific
used for AML, lymphoma
Cytarabine
pyrimidine analog activated to 5F-dUMP which complexes folic acid - inhib thymidylate synthase - lowers dTMP - lowers DNA synth; S phase specific
use: colon CA, pancreatic CA, basal cell carcinoma
5-fluorouracil
folic acid analog that competitively inhib DHF reductase - lowers dTMP - lowers DNA synthesis; S phase specific
use: ALL, lymphomas, choriocarcinoma, sarcomas, ectopic pregnancy, med abortion w/ misoprostol, RA, psoriasis, IBD, vasculitis
Methotrexate
myelosuppression SE is reversible with Leucovorin
induces free radical formation - breaks in DNA strands
use: testicular CA, Hodgkin’s
Bleomycin
intercalates in DNA
use: Wilms tumor, Ewing sarcoma, rhabdomyosarcoma, childhood tumors
Dactinomycin
generates free radicals, intercalate DNA - breaks in DNA - less replication
use: solid tumors, leukemias, lymphomas
Doxorubicin
Daunorubicin
cross links DNA via alkylation
use: CML, ablate bone marrow before transplant
Busulfan
cross link DNA at guanine N7 via alkylation
bioactivated by liver
use: solid tumors, leukemia, lymphomas
Cyclophosphamide
ifosfamide
cross link DNA via alkylation, crosses BBB, bioactivation required
use: brain tumors (glioblastoma multiforme)
Nitrosoureas: carmustine, lomustine, semustine, streptozocin
hyperstabilize polymerized microtubules in M phase - mitotic spindle can’t break down - no anaphase
use: ovarian & breast carcinoma
Paclitaxel
other taxols
vinca alkaloids bind beta tubulin - inhib polymerization into microtubules - prevent mitotic spindle formation (M phase arrest)
use: solid tumors, leukemias, Hodgkin’s, non Hodgkin’s
Vincristine & Vinblastine
Hodgkin’s = Vinblastine
non Hodgkin’s = Vincristine
cross links DNA
use: testicular, bladder, ovary, lung carcinomas
cisplatin
carboplatin
inhibit topoisomerase II - DNA degradation
use: solid tumor esp. testicular & small cell lung CA, leukemia, lymphoma
Etoposide
teniposide
inhib topoisomerase I - prevent DNA unwinding & replication
use: colon cancer, ovarian, small cell lung CA
irinotecan for colon CA
topotecan for ovarian & small cell lung CA
inhib ribonucleotide reductase - less DNA synth; S phase specific
use: melanoma, CML, sickle cell (increases HbF)
Hydroxyurea
bind intracytoplasmic receptor to alter gene transcription
use: CLL, non Hodgkin’s, AI diseases
Prednisone
prednisolone
MoAb against VEGF, inhib angiogenesis
use: solid tumor (colorectal, renal cell carcinoma)
Bevacizumab
EGFR tyrosine kinase inhibitor
use: non small cell lung carcinoma
Erlotinib
tyrosine kinase inhibitor of BCR-ABL (philadelphia chrom fusion gene in CML) + c-kit (GI stromal tumors)
Imatinib
MoAb against CD20 on most B cell neoplasms
use: non Hodgkin’s, CLL, IBD, RA
Rituximab
selective estrogen receptor modulators - receptor antagon in breast & agonists in bone to block binding of estrogen to ER+ cells
use: breast CA tx & prevention, prevent osteoporosis
Tamoxifen for breast CA
Raloxifene for osteoporosis
MoAb against HER2 (c-erbB2 tyrosine kinase inhibitor) - kills cancer cells overexpressing HER2 via inhib HER2 cell signaling & ADCC
use: HER2+ breast CA, gastric CA
Trastuzumab (Herceptin)
small molecule inhib of BRAF oncogene+ melanoma
use: metastatic melanoma
Vemurafenib
