Cancer Chemotherapy Flashcards
Alkylating Agents
CELL CYCLE NON-SPECIFIC Mechlorethamine Cyclophosphamide Isofosfamide Carmustin/Lomustin Busulfan Cisplatin
Antimetabolites
CELL CYCLE SPECIFIC Methotrexate 6-MP Fluorouracil Capecitabine Cytarabine
Antibiotics
CELL CYCLE NON-SPECIFIC - except Bleo Doxorubicin Epirubicin Dactinomycin Bleomycin
From plants
CELL CYCLE SPECIFIC Vincristine Vinblastine Paclitaxel (Taxol) Docetaxel Etoposide
Aromatase Inhibitors
Exemestane
Letrozole
Anastrozole
RTK Inhibitors
Tamoxifen
Imatinib
Monoclonal Antibodies (RTK)
Trastuzumab
Cetuximab
Bevacizumab
Raf/Mek Inhibitors
Sorafenib
Vemurafenib
Mechlorethamine
Reactive nitrogen mustard
Must be mixed right before administration
Nausea, vomiting, BM toxicity
(not in FA)
Cyclophosphamide
Crosslink DNA at guanine N7
Prodrug that is activated by CYP450 in liver
TX: Highly effective against Burkitt’s
Acrolein - toxic compound that causes hemorrhagic cystitis. Must take with lots of water.
MESNA - will bind toxic acrolein and reduce its effects
SE: Hematuria
Myelosuppression
Isofosfamide
Greater activity than Cyclophosphamide, must give with MESNA
SE: Neurotoxicity, Nephrotoxicity, Hematuria, Cardiac tox at high dose
Myelosuppression
Carmustin/Lomustin
Nitrosoureas
Lipid soluble - can cross BBB
TX: Brain tumors
SE: Delayed myelosuppression, PULMONARY FIBROSIS, CNS toxicity
Busulfan
TX: CML
SE: Myelosuppression, Pulmonary Fibrosis
Cisplatin
Cross-links GC base pairs with platinum
TX: Treat testicular cancer
(Bleomycin, Etoposide, Vinblastine - 85% cure)
SE: Renal damage, Ototoxicity, Peripheral neuropathy
Methotrexate
Folate analog - Inhibits DHFR
No THF (dTMP) generated
S-phase specific
TX: Pediatric ALL, Choriocarcinoma
(Psoriasis, IBD, RA, Vasculitis)
SE: Hepatic Necrosis, Myelosuppression, Pulmonary Fibrosis, Mucositis
Reversal: Leucovorin
6-Mercaptopurine
(same as Azathioprine - Aza is metabolized to 6-MP)
Inhibits guanine synthesis
TX: Maintenance of ALL
SE: Myelosuppression
Fluorouracil (5-FU)
Pyrimidine analog
Inhibits Thymidylate Synthase - prevent dTMP
Potentiated by leucovorin
TX: Colon cancer, Pancreatic cancer, Basal Cell Carcinoma
SE: PHOTOSENSITIVITY, Oral/GI ulcers, Hand Foot Syndrome, Myelosuppression
Capecitabine
Orally prodrug of 5-FU
not GI toxic
Cytarabine
Cytosine analog - Inhibits DNA polymerase
TX: AML, Hairy Cell Leukemia
SE: Myelosuppression with Megaloblastic anemia, Pancytopenia
Doxorubicin
Free radicals that bind to topo II nicked DNA
TX: Solid tumors, breast cancer
SE: Dilated Cardiomyopathy, severe local tissue damage with extravasation, Myelosuppression
Dexrazoxane - Prevents cardiac myopathy. Iron chelating agent
Epirubicin
Doxorubicin analog
Can use it at higher doses than Doxorubicin
SE: Chronic cardiac toxicity
Interacts with Cimetidine (H2 Receptor blocker) - serum concentration will rise
Dactinomycin
Intercalates DNA between adjacent GC base pairs
Inhibits RNA pol
Blocks topo II nicked strands
TX: Pediatric Rhabdomyosarcoma, Wilm’s Tumor, Ewing’s sarcoma
(along with surgery, Vincristine/Cyclophosphamide)
SE: Severe tissue damage with extravasation, Myelosuppression
Bleomycin
Generates free radicals (O2 and OH-) that fragment DNA
TX: Hodgkin lymphoma, squamous cell carcinomas, testicular cancer, germ cell tumor of ovary
SE: PULMONARY FIBROSIS, Minimal Myelosuppression
Mild Bone Marrow Suppression
Bleomycin and Vincristine
Vincristine
Inhibits tubulin polymerization
M-Phase specific
TX: Pediatric leukemia, Non-Hodgkin lymphomas
SE: Sensory neuropathy, paralytic ileus
Mild myelosuppression
Vinblastine
TX: Testicular cancer (w/ Bleo and cisplatin)
SE: Myelosuppression, less neurotoxic
Paclitaxel/Docetaxel
Stabilizes polymerized microtubules
TX: Cisplatin resistant solid tumors
SE: Peripheral neuropathy
Etoposide
Inhibits topoisomerase II - causes ds breaks
TX: Testicular cancer, SCLC
leukemias, lymphomas
SE: Myelosuppression
Vinblastine/Cisplatin/Bleomycin/Etoposide
Testicular Cancer
Exemestane, Letrozole, Anastrozol
Aromatase inhibitors - block conversion of androgen to estrogen
TX: Estrogen receptor positive breast cancer
SE: MSK pain, Headache, Fatigue, Difficulty breathing
Tamoxifen
Inhibits Estrogen Receptor directly
TX: Estrogen dependent breast cancer
SE: Can increase the risk of endometrial cancer
Prevents bone loss and reduces serum cholesterol
Imatinib
Inhibits BCR-ABL
TX: CML, CMML
SE: Inhibits platelet derived growth factor
Trastuzumab
Inhibits Her2
TX: Her2 positive metastatic breast cancer
SE: Weakening of heart muscle, CHF, neutropenia, anemia, hypersensitivity reactions
Cetuximab
Inhibits EGFR (Her1)
TX: EGFR positive colorectal cancer
SE: Severe infusion reactions, Hypotension, Serum sickness, Papulopustular acneiform rash
Bevacizumab
Inhibits VEGF
Blocks angiogenesis and neovascularization
TX: Colorectal Cancer
SE: Hypertension, CHF, Proteinuria, Hemorrhage, GI perforation
Sorafenib
C-Raf, VEGF, PDGFR inhibitor
TX: Kidney, Liver, Thyroid cancer
SE: Hemorrhage, Hypertension
Vemurafenib/Dabrafenib
B-Raf inhibitor
TX: METASTATIC MELANOMA carrying V600E B-Raf mutation
Given with Trametinib
