oncology agents
Terms
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- Etoposide, VP-16
- Vespid microtubule toxins podophyllotoxin non-intercalating Topo II inhibitor very broad act with synergistism Oral dose not used
- Etopophos
- water soluble prodrug of etoposide must be dephosphorylated to etoposide to be active. IV
- Vincristine
- Oncovin Microtubule toxin M-phase specific (inhibit mitotic spindle) Reduce dose in hyperbilirubemic patients Neurotoxicity (foot drop syndrome-irreversible, paralystic ileus) SIADH Constipation
- Vinblastine
- Velban Microtubule toxin less neurologic toxicity (but asso with chronic use)
- Vinorelbine
- Navelbine Microtubule toxin neurotoxicity and leukopenia
- Pacilitaxel
- Taxol Microtubule toxin Pacific Yew Stabilizes tubulin structures-nonfunctional Adm before cisplatin or carboplastin Allergy-rash, flushing, dyspnea, hypotension
- Docetaxel
- Taxotere Microtubule toxin Dexamethasone 8mg bid 1 day before, 2 days after
- Estramustine
- Estracyte/Emcyt Microtubule toxin Estradiol and nitrogen mustard combo Hormone refractory prostate cancer Painful gynecomastia, CV complications, thromboembolism and decreased libido/impotence
- Bleomycin
- Blenoxane Antitumor antibiotics Glycoproteins from Streptomyces S-phase, G2, DNA strand breaks Redox with Fe cofactor Inactivate by bleomycin hydrolase (lack in skin and lungs) Less myelosuppression but cutaneous toxicity and pulmonary fibrosis
- Doxorubicin
- Adriamycin Antitumor abx Topo II inhibitor Intercalates and free radical formation Broad spectrum of act Hyperbilirubinemia-dose adjustment *red urine Severe n/v, radiation recall Unique cardiotoxicity
- Mitoxantrone
- Novantrone Antitumor abx anthracenedione-intercalates into DNA and inhibits topo II less cardiotoxicity compared to doxorubicin. Blue urine
- Dactinomycin-D/Actinomycin-D
- Cosmegen Antitumor abx intercalates, forms free radicals-DNA strand breaks Elimate unchanged in urine and bile
- Cytosine Arabinoside Cytarabine
- Cytosar competitive inhibitor of DNA polymerase Misincorporates into DNA compromising DNA replication* main effect Resistance: lack of phosphorylation enzymes Decrease in cytarabine transport into cell
- Capcetibine
- Xeloda ORAL* pro-drug of 5-DFUR Metabolized in liver Tumor more efficient at converting capcetibine than normal tissue
- Floxuridine (FUDR)
- convert to FdUMP to inhibit thymidylate synthetase Administered into hepatic artery Hand-foot syndrome Hepatic metastasis of colorectal cancer
- 5-FU toxicity
- stomatitis, diarrhea, cutaneous (hand-foot syndrome)-worst with bolus infusion
- 5-FU resistance
- Changes in converting enzymes (thymidylate synthetase) loss of folate pools inhibition of polyglutamation
- 5-FU
- Antimetabolite Pyrimidine analog FdUMP-thymidylate synthetase FUTP-RNA FdUTP-DNA Leukovorin improve activity
- ARA-C toxicities
- Stomatitis Rash* High dose: conjunctivitis (dexamethasone eye drops), CNS toxicity (coma, death), non-cardiogenic pulmonary edema
- Gemcitabine
- Gemzar Antimetabolites Requires triphosphorylation inhibits ribonucleotide reductase NOT recognized by repair enzymes so has expanded activity compared to cytarabine Flu-like syndrome*
- 6-Mercaptopurine
- Purinethol Antimetabolites thiol sub monophosphate inhibit purine biosynthesis Allopurinol inhibits xanthine oxidase that metabolite 6-MP to inactive metabolite thiouric acid Redure 6-MP dose by 75% Commonly used in ALL
- 6-thioguanine
- thioguanine Antimetabolites incorporates into DNA and lead to chain termination use in ANL
- Fludarabine
- Fludara Antimetabolites Good immunosuppressive agent inhibit DNA polymerase and ribonucleotide reductase Require triphosphorylation High dose-neurotoxicity and renal failur
- Pentostatin
- 2'deoxycoformycin Nipent Antimetabolite Adenosine deaminase inhibitor, concentration of adenosine increase and inhibits ribonucleotide reductase Hairy cell leukemia High dose neurologic and renal toxicity
- Cladribine
- 2-chlorodeoxyadenosine Leustatin Antimetabolite Require triphosphorylation and incorp into DNA inhibits ribonucleotide reductase High dose-neurologic and renal toxicity
- Clofarabine
- Clolar antimetabolite Refractory or relapsed childhood ALL only IV flu-like, neurotoxicity, nephrotoxicity
- Decitabine
- Dacogen antimetabolite inhibits DNA methyltransferase-> hypomethylation and apoptosis metabolized by cytidine deaminase Electrolyte abnormality-hyperglycemia, hypomagnesemia, hypokalemia, increase LFTs
- 5-Azacitidine
- Vidaza antimetabolites low dose-hypomethylation. high dose-false base disrupting DNA function lab abnormalities
- Hydroxyurea
- Hydrea antimetabolites inhibit ribonucleotide reductase-decrease production of deoxyribonucleotides Use in CML to lower WBC, head and neck Radiation recall, megaloblastic anemia
- Nelarabine
- Arranon antimetabolites with Ara-GTP inhibiting DNA synthesis 40% with CNS toxicity