Cancer drugs Flashcards
Cisplatin
Category:
Alkylators/cross-linkers
Related drugs:
Oxaliplatin, carboplatin
MOA:
Cross-linking of DNA
Dose limiting toxicity:
Peripheral Neuropathy
Other toxicity:
ototoxicity, myelosuppression
Clinical use-examples:
testicular, bladder, lung, colon, ovarian CA
Cylcophosphamide
Category:
Alkylators/cross-linkers
Related drugs:
(alkylating agents) ifosfamide, busulfan, carmustine
MOA:
Alkylation and cross-linking of DNA
Dose limiting toxicity:
myelosuppression
Other toxicity:
hemorrhagic cystitis
Clinical use-examples:
many regimens: leukemias, lymphomas, solid tumors
Cytarabine
Category:
Antimetabolites
Related drugs:
(pyrimidine antimetabolites) gemcitabine
MOA:
inhibitor of DNA polymerase, misincorporation into DNA
Dose limiting toxicity:
myelosuppression
Clinical use examples:
leukemias, lymphomas
Flurouracil (5-Fluoruracil)
Category:
Antimetabolites
Related drugs:
Capecitabine
MOA:
activated to FdUMP which inhibits thymidylate synthetase, also misincorporated into RNA
Dose limiting toxicity:
myelosuppression
Other toxicity:
GI
Clinical use examples:
colon CA, many solid tumors
Hydroxyurea
Category:
Antimetabolites
MOA:
inhibitor of ribonucleotide reductase which is required to convert ribonucleotides to deoxyribonucleotides
Dose limiting:
myelosuppression
Other toxicity:
GI
Clinical use examples:
melanoma, CML
Methotrexate
Category:
Antimetabolites
MOA:
DHFR inhibitor
Dose limiting toxicity:
myelosuppression
clinical-use examples:
ALL, choriocarcinoma, lymphomas, many solid tumors
Thioguanine (6-thioguanine)
Category:
Antimetabolites
Related drugs:
mercaptopurine, cladribine
MOA:
inhibitor of purine metabolism
Other toxicity:
myelosuppression
Clinical use:
acute leukemias, chronic myelocytic leukemia
Bleomycin
MOA:
interacts with DNA and catalyzes free radical formation and DNA destruction
Dose limiting:
Pulmonary Fibrosis
Other toxicity:
radiation recall, skin lesions
use:
Hodgkin’s lymphoma, testicular CA
Bevacizumab
MOA :
antibody against VEGF, inhibits angiogenesis
Other toxicity: vascular toxicity (e.g. stroke or myocardial infarction)
use:
epithelial cancers in combo with std therapy
Cetuximab
Related drugs:
panitumumab
MOA:
monoclonal antibody against the extracellur domain of EGFR (a receptor tyrosine kinase)
other toxicity:
skin lesions
use:
colon CA, head/neck tumors
Crizotinib
Related drugs:
Ceritinib
MOA:
ALK (anaplastic lymphoma kinase) inhibitor
Other toxic:
bradycardia, visual disturbances
Use:
non-small cell lung CA
Erlotinib
Related drugs:
Gefitinib
MOA:
EGFR inhibitor
other toxic:
skin lesions
use:
colon CA
Imatinib
Related drugs:
dasatinib, nilotinib
MOA:
inhibitor of ABL, Kit, PDGF-R tyrosine kinases
Other toxic;
fluid retention, some myelosuppression
Use:
CML, GIST
Rituximab
MOA:
binds to CD20 on the surface of B cells and leads to antibody dependent cellular cytotoxicity
Toxic:
myelosuppression
other toxic:
sensitivity reactions
use:
non-Hodgkin’s lymphoma, B cell leukemias
Sunitinib
Related drugs:
sorafenib, pazopanib
MOA:
inhibitor of RTKs including VEGF-R, PDGF-R, cKit
other toxic:
vascular toxicity
use:
inhibits angiogenesis and some growth factor dependent tumors: renal cell carcinoma
Trastuzumab
MOA:
binds to Her2 on cancer cells and stimulates antibody-dependent cellular cytotoxicity (ADCC)
Other toxicity:
cardiac
Use:
breast CA
Vemurafenib
MOA:
inhibitor of mutant BRAF kinase
Toxic:
skin lesions
Use:
melanoma
Paclitaxel
Related drugs:
Docetaxel
MOA:
binds tubulin and stabilizes microtubules
Toxic:
myelosuppression
Other toxic:
Sensory neuropathy
Use:
ovarian, breast, lung, GI tumors
Vincristine
Related drugs:
vinblastine
MOA:
interacts with tubulin and prevents microtubule polymerization
Toxic:
Peripheral Neuropathy, myelosuppression
Use:
leukemias, lymphomas, solid tumors
Bortezomib
MOA:
a boronic acid containing dipeptide that inhibits the proteasome and stimulates apoptosis
Toxic:
peripheral neuropathy, mylesuppression
Use:
multiple myeloma
Asparaginase (L-asparaginase)
Related drugs:
pegaspargase (pegylated version of asparaginase) with a longer half life
MOA:
degrades asparagine in the circulation and starves tumor cells that can not synthesize asparagine
Toxic:
Hypersensitivity reactions
Use:
ALL and lymphomas
Anastrozole
Related drugs;
letrozole
MOA:
aromatase inhibitor
Toxic:
estrogen withdrawl symptoms
Use:
post-menopausal breast CA
Leuprolide
Related drugs:
goserelin, nafarelin
MOA:
GnRH analog that causes GnRH receptor down regulation and decreased LH and testosterone
Toxic:
steroid withdrawl effects
Use:
metastatic prostate, pre-menopausal breast CA
Tamoxifen
Related drugs:
toremifene
MOA:
selective estrogen receptor modulator (SERM)-acts to inhibit ER in breast CA
Toxic;
estrogen withdrawl symptoms, risk increase for endometrial CA
Use:
pre and post-menopausal breast CA
Dactinomycin
MOA:
intercalates into DNA and blocks RNA and DNA synthesis
toxic:
myelosuppression
other toxic;
radiation recall
use:
choriocarcinoma, rhabdomyosarcoma, Wilms tumor
Doxorubicin
Related drugs:
(anthracyclines) daunorubicin, idarubicin, epirubicin
MOA:
inhibitor of the topoisomerase II-DNA complex
Toxic:
myelosuppression cardiomyopathy
other toxic:
radiation recall
Use:
lyphomas, breast CA, other solid tumors
Etoposide
related:
teniposide
MOA;
inhibitor of the topoisomerase II-DNA complex
Toxic:
myelosuppression
Use:
testicular, small cell lung, lymphomas, leukemias
Irinotecan
Related drugs:
topotecan
MOA:
inhibitor of topoisomerase I-DNA complex
Toxic:
myelosuppression
Other toxic:
severe diarrhea
Use:
colon, ovarian, small cell lung CA
Allopurinol
Related drugs:
Rasburicase
MOA:
allopurinol: xanthine oxidase inhibitor rasburicase: urate oxidase [both drugs reduce uric acid levels during tumor cell breakdown]
use:
often used when treating leukemias and lymphomas
Aprepitant
Related drugs:
casopitant, netupitant, rolapitant
MOA:
Neurokinin 1 receptor antagonists that help control emesis
Dexrazoxane
MOA:
iron chelating agent that can help prevent doxorubicin induced cardiac toxicity
use:
antidote to cardiotox of doxorubicin
Filgrastim
related:
other hematopoietic stimulators
MOA:
granulocyte colony-stimulating factor analog, stimulates neutrophil production
Toxicity:
bone pain
Use:
treat neutropenia secondary to chemotherapy or bone marrow transplantation
Leucovorin (folinic acid)
MOA:
a tetrahydrofolate analog that can rescue cells from methotrexate toxicity, also binds with FdUMP to covalently inhibit thymidylate synthetase
Use:
with high dose methotrexate therapy
Mesna
MOA:
2-mercaptoethanesulfonate that inactivates toxic metabolites like acrolein in the urine
Use:
antidote to prevent bladder cystitis from cyclophosphamide
Ondansetron
MOA:
serotonin 5-HT3 receptor inhibitor used to treat nausea and vomiting
Prednisone
Related:
Dexamethasone
MOA:
direct suppression of lymphomas and leukemias, also inhibits leukotriene and prostaglandin synthesis, inhibits leukocyte function and traffic control to produce strong antiinflammatory effects
Toxic:
many toxicities if used chronically (hyperglycemia, osteoporosis, fat redistribution)
use:
often used in leukemia/lymphoma regimens
