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60 Cards in this Set
- Front
- Back
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Cyclosporine
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Selective Inhibitor of Cytokine Production and Function - Binds Cyclophilin --> Inhibits Calcineurin, which activates NF-AT ( Nuclear, Factor Activating Tc, a T-cell Transcription Factor). Inhibits synthesis of IL-2
Used for organ transplantation SEs - Nephrotoxicity, Hypertension DIs - CYP3A4 inhibitors NSAIDS, Gentamicin: Nephrotoxic |
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Tacrolimus
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Selective Inhibitor of Cytokine Production and Function - Binds FK-binding protein, inhibits Calcineurin phosphatase, NF-AT & IL-2 --> lowers T-Cell proliferation
Used for Organ transplatation (100X more potent than Cylcosporine), Rescue therapy for GVHD SEs - Nephrotoxic, Neurotoxic DIs - CYP3A4 inhibitors NSAIDS, Gentamicin: nephrotoxic |
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Sirolimus
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Selective Inhibitor of Cytokine Production and Function - Binds FK-binding protein & inhibits mTOR --> decreases translation of mRNA and progression of T cells form G1-S phases
Used for organ transplantation, stents SEs - Hyperlipidemia |
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Azathioprine
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Cytotoxic Agent - purine analog: Inhibits DNA & RNA synthesis --> prodrug converted to 6-MP
Used for Organ transplantation, RA, SLE SEs - mild leucopenia |
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Mycophenolate mofetil
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Cytotoxic Agent - Inhibits inosine monophosphate dehydrogenase & de novo synthesis of purines --> suppresses B and T cell proliferation
Used for solid organ transplantation SEs - mild leukopenia |
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Antithymocyte globulin
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Antibody Immunosuppressant - Horse antibody, acts primarily by binding and decreasing the number of peripheral T-lymphocytes, and suppresses CMI
Used to prevent allograft rejection |
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Muromonab-CD3
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Antibody Immunosuppressant - mouse monoclonal antibody that selectively binds to CD3 glycoprotein on T lymphocytes
Used for acute rejection episodes of kidney, and steroid-resistant acute rejection of liver and heart transplants Also for depleting T cells from donor bone marrow prior to bone marrow transplantations SEs - Flu-like illness (Cytokine release syndrome), CNS problems |
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Basiliximab
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Antibody Immunosuppressant - mouse/human monoclonal antibodies that bind to the interlukin-2 (IL-2) receptor - IL-2 antagonist
Used for acute renal transplant rejection SEs - well tolerated |
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Prednisone
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Corticosteroid - Inhibit production of inflammatory mediators and cytokines; ↓ chemotaxis and phagocytic activity of neutrophils and monocytes
Used for organ trasplantation, DOC for autoimmune disorders Also used for allergic reactions SEs - Adrenal suppression, Cushing's habitus |
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Thalidomide
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Inhibits TNF-α, ↓phagocytosis by neutrophils and ↑ CMI. Inhibits angiogenesis, anti-inflammatory, immunomodulatory
Used for Multiple myeloma, erythema nodosum leprosum, Anemia due to myelodysplastic syndrome SEs - Phocomelia, teratogenic |
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Mechlorethamine
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Alkylating Agents
Nitrogen Mustard Hydroscopic, unstable, Vesicant Hodgkin's disease - MOPP |
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Cyclophosphamide
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Alkylating Agents
Nitrogen Mustard Stable, Oral Prodrug - activated by P-450 to become acrolein and phosphamide mustard For non-Hodgkin's lymphoma, Burkitt's lymphoma Hemorrhagic cystitis, alopecia, impotence, sterility |
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Chlorambucil
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Alkylating Agents
Nitrogen Mustard Slow/least toxic For CLL |
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Carmustine
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Alkylating Agents
Nitrosoureas For cancer of CNS - crosses BBB Biodegradable wafer implanted |
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Cisplatin
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Alkylating Agents
Platinum Complexes Crosslink DNA - cell-cycle nonspecific Broad therapy - Testicular cancer |
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Carboplatin
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Alkylating Agents
Platinum Complexes Dose-limiting Less renal and GI toxicity than cisplatin |
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Methotrexate
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Antimetabolites
Antifolate DHFR Inhibitor For ALL, Choriocarcinoma Myelosuppressor, renal/hepatic toxicity, teratogen, ulceration of the mouth |
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5-Fluorouracil
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Antimetabolites
Antipurimidines Prodrug that inhibits thymidylate synthetase Used for colorectal carcinoma, breast cancer, BLOC tumors (Bladder, Liver, Ovary, Cervix), skin cancer SEs - severe bone marrow depression |
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Cytarabine
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Antimetabolites
Antipurimidines Inhibits DNA polymerase IV, Used for acute adult myelogenous leukemias and lymphomas SEs - mucositis, rash |
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Gemcitabine
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Antimetabolites
Antipurimidines Inhibits DNA polymerase IV, DOC for metastatic adenocarcinoma of the pancreas |
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6-Mercaptopurine
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Antimetabolites
Antipurines Inhibits enzymes required for AMP and GMP synthesis Primarily for acute leukemia in children SE- cholestatic jaundice, reduce dose if using with allopurinol |
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Thioguanine
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Antimetabolites
Antipurines Inhibits enzymes required for AMP and GMP synthesis Primarily for AML SE - similar to 6-MP, no interaction with Allopurinol |
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Vinblastine
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Plant Alkyloid
Vinca Alkaloid Spindle Poison - binds tubulin in microtubules and disrupts mitotic spindle and mitosis - M phase specific Hodgekin's disease - part of ABVD Metastatic testicular cancer - part of PVB SE - bone marrow depression |
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Vincristine
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Plant Alkyloid
Vinca Alkaloid Spindle Poison - binds tubulin in microtubules and disrupts mitotic spindle and mitosis - M phase specific Acute lymphocytic leukemia in children + Prednisone Hodgkin's disease: MOPP regimen Non-Hodgkin's lymphomas: CHOP regimen SE - Neurotoxic |
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Paclitaxel
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Plant Alkaloid
Taxane Binds and stabilizes microtubules --> inhibits depolymerization and mitosis Solid tumors and metastatic breast cancer (1st line therapy in combination) SE - Peripheral neuropathy, SERIOUS ALLERGIC REACTIONS (5%) |
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Etoposide
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Plant alkaloid
Podophyllotoxin Binds and inhibits topoisomerase II, preventing repair of DNA breaks and causes DNA damage - inhibits cells in late S-G2 phase Testicular cancer - combination w/ cisplatin ALL, non-Hodgkin's lympomas |
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Topotecan
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Plant alkaloid
Camptothecin Inhibits topoisomerase I enzyme --> DNA damage Metastatic ovarian/lung cancer - alternative to paclitaxel |
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Irinotecan
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Plant alkaloid
Camptothecin Inhibits topoisomerase I enzyme --> DNA damage Colorectal cancer - DOC w/ 5-FU Mucositis and diarrhea |
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Dactinomycin
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Plant alkyloid
Antibiotic Intercolates btwn G-C bps in DNA --> inhibits DNA unwinding and DNA-dependent RNA synthesis - CCNS Wilms tumor in children - + Vincristine Rhabdomyosarcoma in children - 60-80% cure Choriocarcinoma for MTX-resistant SE - Dermatitis |
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Doxorubicin
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Plant alkyloid
Anthracycline Antibiotic Intercalates DNA, inhibits Topoisomerase II, and increases O2 free radicals Broad spectrum - AML/ALL, Non Hodge, Hodge, solid tumors SE - Red urine, cardiomyopathy (prevented by dexrazoxane) |
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Daunorubicin
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Plant alkyloid
Anthracycline Antibiotic Intercalates DNA, inhibits Topoisomerase II, and increases O2 free radicals AML/ALL SEs - Cardiomyopathy, red urine |
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Bleomycin
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Plant alkyloid
Antibiotic Binds to DNA, increases O2 free radicals --> scission of DNA Testicular carcinoma - comb in PEB SE - Pneumo probs (monitor pulmonary function) |
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Amifostine
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Plant alkaloid
Cytoprotective agent Thiophosphate that converts to free thiol, which scavenges for free radicals and superoxide anions Used to reduce nephrotoxicity of cisplatin in ovarian and non-small cell lung cancer |
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Mesna
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Plant alkaloid
Cytoprotective agent Thiol forming compound - prophylactic agent to decrease cyclophosphamide - induced hemorrhagic cystitis |
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Dexrazoxane
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Plant alkaloid
Cytoprotective agent EDTA derivative - cardioprotective agent used with doxorubicin Potent intracellular chelating agent that interferes with Fe-mediated free radical formation though to be responsible for anthracycline-induced cardiomyopathy |
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Tamoxifen
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Antiestrogen
Competitive ER antagonist and partial agonist - ER+ tumors only Advanced breast cancer who are ER+ Chemoprophylaxis for high risk women - decrease risk by 50% SE - well tolerated, increased incidence of endometrial cancer and thromboemobolic events |
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Fulvestrant
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Antiestrogen
Competitive ER antagonist - ER+ tumors only Advanced breast cancer who are ER+ Chemoprophylaxis for high risk women - decrease risk by 50% SEs - well tolerated |
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Flutamide
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Antiandrogen
A-agonist - blocks androgen R Prostate cancer - comb w/ estrogen or gonadotropin-releasing hormone SEs - gynecomastia (man-boobs), impotence |
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Leuprolide acetate
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GnRH Agonist
Binds LH-RH in pituitary --> feedback inhibition - lowers levels of Gn and testosterone --> MEDICAL CASTRATION Prostate cancer - IM injection monthly SEs - well tolerated, hot flushes, depression, muscular atrophy |
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Abarelix
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GnRH Antagonist
Binds to pituitary GnRH R --> lowering LH, FSH, and testosterone resease by testes Advanced prostate cancer SEs - HSN |
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Aminoglutethimide
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Aromatase (estrogen synthetase) Inhibitor
Prevents peripheral conversion of adrenal adrogens to estrone and estradiol - given with a corticosteroid to prevent adrenal insufficiency Breast cancer SEs - NVD |
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Anastrozole
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Aromatase (estrogen synthetase) Inhibitor
Prevents peripheral conversion of adrenal androgens to estradiol Advanced or early (ER+) Breast Cancer in postmenopausal women SEs - NVD |
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L-Asparaginase
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Bacterial Enzyme
Hydrolyzes asparagine to aspartate and ammonia, depleting tumor cells of AA ALL in children SEs - Allergic rxns - fever, rash, anaphylaxis CNS - confusion, sedation Defects in blood coagulation |
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Imatinib mesylate
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Tyrosine Kinase inhibitor
Binds Bcr-Abl and inhibits the TK enzyme and cell proliferation CML - First line for all stages of Ph+, 80% effective SEs - pleural effusion, ascites, neutro/thrombocytopenia - severe |
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Dasatinib
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Tyrosine Kinase inhibitor
Binds Bcr-Abl and inhibits the TK enzyme and cell proliferation CML (Ph+) - if intolerant to imatinib SEs - myelosuppresive |
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Sunitinib
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Tyrosine Kinase inhibitor
Inhibits transmembrane receptor TKs (VEGFRs and PDGFRs) involved in tumor proliferation and angiogenesis Advanced renal cell carcinoma - 1st line tx GI stromal tumor SEs - fatigue and diarrhea |
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Gefitinib
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Epidermal GFR Antagonist
Decreases phosphorylation of TK associated with EGFR found on the surface of many normal and cancer cell and involved in regulation of cell proliferation and survival Metastatic non-small cell lung cancer SEs - Intersitial pneumonia |
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Lapatinib
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Epidermal GFR Antagonist
Oral inhibitor of EGFR-1 and HER-2 receptor - inhibiting the TK domains, inducing apoptosis and tumor cell death Metastatic breast cancer SEs - rash Substrate for CYP3A4 |
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Bortezomib
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Proteosome Inhibitor
Inhibits proteosome that degrades proteins and activates factors involved in signal transduction and cell cycle regulation Multiple Myeloma SEs - ND, asthenia, neutro/thrombocytopenia Peripheral neuropathy |
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Interferon alpha-2a
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Biological response modifier
Type I - acid stable, virus induced, produced in leukocytes Bind to specific membrane R --> decreased cell proliferation and decreased viral replication Also has immunomodulatory effects by increasing antigen presentation and macrophage, decreasing synthesis and release of cytokines, and increasing cytotoxic T-cell activity Used in Hairy CL, melanoma, CML, Kaposi's sarcovoma Hepatitis B and C Fever, thrombocytopenia, leucopenia, NVD |
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Interferon alpha-2b
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Biological response modifier
Type I - acid stable, virus induced, produced in leukocytes Bind to specific membrane R --> decreased cell proliferation and decreased viral replication Also has immunomodulatory effects by increasing antigen presentation and macrophage, decreasing synthesis and release of cytokines, and increasing cytotoxic T-cell activity Used in Hairy CL, melanoma, CML, Kaposi's sarcovoma Hepatitis B and C Fever, thrombocytopenia, leucopenia, NVD |
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Interferon beta-1a
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Biological response modifier
Type I- acid stable, virus induced, produced by fibroblasts and epithelial cells Bind to specific membrane R --> decreased cell proliferation and decreased viral replication Also has immunomodulatory effects by increasing antigen presentation and macrophage, decreasing synthesis and release of cytokines, and increasing cytotoxic T-cell activity Used in relapsing multiple sclerosis Fever, thrombocytopenia, leucopenia, NVD |
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Peginterferon alpha-2a
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Biological response modifier
Type I - acid stable, virus induced, produced in leukocytes Bind to specific membrane R --> decreased cell proliferation and decreased viral replication Also has immunomodulatory effects by increasing antigen presentation and macrophage, decreasing synthesis and release of cytokines, and increasing cytotoxic T-cell activity Used in Hairy CL, melanoma, CML, Kaposi's sarcovoma Hepatitis B and C Fever, thrombocytopenia, leucopenia, NVD |
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Aldesleukin
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Biological response modifier
IL-2 - lymphokine produced by activated T cells --> induction of T cell proliferation and differentiation Renal cell carcinoma and malignant melanoma Severe toxicity - anemia, pulmonary edema, cardiac arrhythmias |
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Trastuzumab
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Monoclonal Antibody
Binds to HER-2 growth factor R and inhibits proliferation Metastatic breast cancer - combo w/ paclitaxel or doxorubicin SEs - CHF, acute HSN |
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Rituximab
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Monoclonal Antibody
Binds to CD20 antigen found on surface of normal and malignant B lymphocytes --> causes lysis Non-Hodgkin's lymphoma SEs - Infusion reactions |
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Gemtuzumab ozogamicin
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Monoclonal antibody
Binds to CD33 found on leukemic blasts, which releases calichemicin --> damages DNA AML SEs - Infusion reaction (prophylaxis with acetomenophen and antihistamines), severe neutropenia |
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Alemtuzumab
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Monoclonal antibody
Binds to CD52 --> induces lysis in normal and leukemic cells Used for B cell CLL SEs - Lympho/neutropenic, anemia |
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Cetuximab
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Monoclonal antibody
Binds to EGFR and blocks activation of R-associated kinases --> inhibits cell growth --> apoptosis Colon cancer - may combo w/ irinotecan SEs - rash, infusion rxn |
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Bevacizumab
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Monoclonal antibody
Binds to Vascular Endothelial GF --> prevents binding --> inhibits formation of new blood vessels Metastatic colorectal cancer - DOC w/ 5FU HER2-negative metastatic breast cancer - DOC w/ paclitaxol Metastatic non-small cell lung cancer, age-related macular degeneration SEs - GI bleeding, proteinuria |
