Pharm: Antineoplastic Agents - Therapeutic Use

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USE: BROAD USE IN ADULTS AND PEDS FOR A VARIETY OF HEMATOLOGIC CANCERS AND SOLID TUMORS ; POTENT IMMUNOSUPPRESSIVE PROPERTIES --> TX OF AUTOIMMUNE DISORDERS, SUCH AS WEGENER'S GRANULOMATOSIS, R.A. AND NEPHRITIC SYNDROME

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NITROGEN MUSTARDS ; CYCLOPHASPHAMIDE

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USE: TESTICULAR CANCER, LYMPHOMAS, BONE/TISSUE SARCOMAS, BLADDER, CERVICAL, OVARIAN, LUNG Ca

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; ISOSFAMIDE

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USE: MAJOR ANTITUMOR ACTIVITY IN BROAD RANGE OF SOLID TUMORS ; USED IN SYNERGY WITH RADIATION AND CERTAIN OTHER ANTI-Ca DRUGS ; ENTER CELLS VIA Cu2+ TRANSPORTER --> AQUATION (H20 DISPLACES CHLORIDE, CYCLOHEXANE, OR OXALATE LIGANDS) --> POSITIVELY CHARGED, HIGHLY REACTIVE MOLECULE --> REACT WITH NUCLEOPHILLIC SITES ON DNA AND PROTEINS FORMING INTRA- AND INTER-STRAND CROSS-LINKS ; THE N7 OF GUANINE --> PT-GG INTRASTRAND CROSS-LINKS ; GUANINE ADENINE (N3) CROSS-LINKS CONTRIBUTE TO CYTOTOX ; INTER-STRAND CROSSLINKS FORM LESS FREQUENTLY ; DNA-Pt ADDUTS INHIBIT REPLICATION/TRANSCRIPTION --> SINGLE AND DOUBLE-STRANDED BREAKS --> MISCODING --> APOPTOSIS - IF RECOGNIZED BY p53 AND OTHER CHECKPOINT PROTEINS

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PLATINUM ANALOGS ; CISPLATIN

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USE: BROAD-SPECTRUM ACTIVITY AGAINST A WIDE RANGE OF SOLID TUMORS ; EXHIBITS SIGNIFICANTLY LESS RENAL TOXICITY AND GI TOX, AND VIGOROUS IV HYDRATION NOT REQUIRED (AN EFFECTIVE ALTERNATIVE FOR RESPONSIBE TUMORS IN PT'S UNABLE TO TOLERATE CISPLATIN) ; USED IN SYNERGY WITH RADIATION AND CERTAIN OTHER ANTI-Ca DRUGS ; ENTER CELLS VIA Cu2+ TRANSPORTER --> AQUATION (H20 DISPLACES CHLORIDE, CYCLOHEXANE, OR OXALATE LIGANDS) --> POSITIVELY CHARGED, HIGHLY REACTIVE MOLECULE --> REACT WITH NUCLEOPHILLIC SITES ON DNA AND PROTEINS FORMING INTRA- AND INTER-STRAND CROSS-LINKS ; THE N7 OF GUANINE --> PT-GG INTRASTRAND CROSS-LINKS ; GUANINE ADENINE (N3) CROSS-LINKS CONTRIBUTE TO CYTOTOX ; INTER-STRAND CROSSLINKS FORM LESS FREQUENTLY ; DNA-Pt ADDUTS INHIBIT REPLICATION/TRANSCRIPTION --> SINGLE AND DOUBLE-STRANDED BREAKS --> MISCODING --> APOPTOSIS - IF RECOGNIZED BY p53 AND OTHER CHECKPOINT PROTEINS

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; CARBOPLATIN

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USE: COLORECTAL AND GASTRIC Ca ; ACTIVITY HAS BEEN OBSERVED IN OTHER GI Ca'S ; IT’S A COMPONENT OF FIRST-LINE CHEMOTHERAPY OF ADVANCED COLORECTAL Ca (FOLFOX) ; USED IN SYNERGY WITH RADIATION AND CERTAIN OTHER ANTI-Ca DRUGS ; ENTER CELLS VIA Cu2+ TRANSPORTER --> AQUATION (H20 DISPLACES CHLORIDE, CYCLOHEXANE, OR OXALATE LIGANDS) --> POSITIVELY CHARGED, HIGHLY REACTIVE MOLECULE --> REACT WITH NUCLEOPHILLIC SITES ON DNA AND PROTEINS FORMING INTRA- AND INTER-STRAND CROSS-LINKS ; THE N7 OF GUANINE --> PT-GG INTRASTRAND CROSS-LINKS ; GUANINE ADENINE (N3) CROSS-LINKS CONTRIBUTE TO CYTOTOX ; INTER-STRAND CROSSLINKS FORM LESS FREQUENTLY ; DNA-Pt ADDUTS INHIBIT REPLICATION/TRANSCRIPTION --> SINGLE AND DOUBLE-STRANDED BREAKS --> MISCODING --> APOPTOSIS - IF RECOGNIZED BY p53 AND OTHER CHECKPOINT PROTEINS (IT BINDS AT THE FORK AND PREVENTS OPENING OF DOUBLE HELIX)

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; OXALIPLATIN

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USE: USED IN COMBINATION PROTOCOLS: ALL (CURATIVE), CHORIOCARCINOMA AND RELATED TROPHOBLASTIC TUMORS ; BURKITT'S LYMPHOMA IN CHILDREN, OTHER NON-HODGKIN'S LYMPHOMAS ; CARCINOMAS OF BREAST Ca, HEAD AND NECK Ca, OVARY, BLADDER ; OSTEOSARCOMA ; IMMUNOSUPPRESSANT: R.A., POLYARTICULAR JUVENILA ARTHRITIS, SEVERE RECALCITRANT PSORIASIS, CROHN'S Dz, WEGENER'S GRANULOMATOSIS, DERMATOMYOSITIS, GVHD IN ALLOGENEIC BONE MARROW TRANSPLANTATION ; ABORTIFACIENT!

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FOLATE ANTAGONISTS ; METHOTREXATE

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USE: USED IN COMBINATION PROTOCOLS FOR A WIDE VARIETY OF SOLID TUMORS (SYNERGY WITH LEUCOVORIN (FOLINIC ACID) --> TERNARY COMPLEX THYMIDYLATE SYNTHASE - LECOVORIN - 5-FdUMP) ; COLORECTAL Ca, FIRST-LINE TX (FOLFOX - FOLINIC ACID, 5-FU, OXALIPLATIN) AND FOLFIRI (FOLINIC ACID, 5-FU, IRINOTECAN) ; ACTIVE AGAINST A WIDE VARIETY OF SOLID TUMORS SUCH AS BREAST, OVARIAN, PANCREATIC, GASTRIC CARCINOMAS, TOPICAL CREAM FOR SUPERFICIAL BASAL CELL CARCINOMAS

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FLUROPYRIMIDINES ; FLUORORURACIL (5-FU)

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USE: METASTATIC BREAST Ca OR COLORECTRAL Ca RESISTANT TO FIRST-LINE DRUGS

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; CAPECITABINE

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USE: AML (DOC, MAY BE USED WITH DAUNORUBICIN OR IDRUBICIN) ; OTHER LEUKEMIAS, HIGH-GRADE LYMPHOMAS - HAS NO ACTIVITY IN SOLID TUMORS

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DEOXYCYTIDIDINE ANALOGS ; CYTARABINE (ARA-C)

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USE: AML (WITH CYTARABINE) ; ITS EFFICACY IN SOLID TUMORS IS LIMITED

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ANTHRACYCLINES ; DAUNORUBICIN

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USE: BROAD SPECTRUM ; LYMPHOMAS, MULTIPLE MYELOMA, SARCOMAS, WIDE RANGE OF SOLID TUMORS ; ONE OF THE MOST WIDELY USED IN Ca CHEMOTHERAPIES

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; DOXORUBICIN

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USE: HODGKIN'S Dz, NON-HODGKIN'S LYMPHOMAS, TESTICULAR Ca, BREAST Ca, MYCOSIS FUNGOIDES (CUTANEOUS T CELL LYMPHOMA), KAPOSI'S SARCOMA, HISTIOCYTOSIS (LETTERER-SIWE Dz), CHORIOCARCINOMA, AND OTHER TUMORS

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MICROTUBULE INHIBITORS ; VINBLASTINE (VINKA ALKALOIDS)

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USE: ALL IN CHILDREN (WITH GLUCOCORTICOIDS), PEDIATRIC SARCOMAS (WITH ALKYLATING AGENT AND DOXORUBICIN)

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; VINCRISTINE (VINCA ALKALOIDS)

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USE: BROAD RANGE OF SOLID TUMORS ; OVARIAN, ADVANCED BREAST, NON-SMALL CELL AND SMALL CELL LUNG, HEAD AND NECK, ESOPHAGEAL, PROSTATE, BLADDER AND AIDS-RELATED KAPOSI'S SARCOMA

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; PACLITAXEL (TAXANES)

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USE: BROAD RANGE OF SOLID TUMORS: ADVANCED BREAST Ca, NON-SMALL CELL LUNG Ca, HEAD AND NECK Ca, SMALL CEL LUNG Ca, GASTRIC Ca, ADVANCED PLATINUM-REFRACTORY OVARIAN Ca, BLADDER Ca

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; DOCETAXEL (TAXANES)

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USE: METASTATIC COLORECTAL Ca (FOLFIRI) WITH CETUXIMAB (FOLFOX FAILURE)

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TOPOISOMERASE I INHIBITORS ; IRINOTECAN (CAPTOTHECINS)

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USE: SMALL CELL LUNG Ca ; TESTICULAR Ca (WITH BLEOMYCIN AND CISPLATIN) ; ACTIVITY SEEN IN LEUKEMIA, LYMPHOMA, AND KAPOSI'S SARCOMA

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TOPOISOMERASE II INHIBITORS ; ETOPOSIDE (EPIPODOPHYLLOTOXINS)

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USE: CML; PHILADELPHIA CHROMOSOME POSITIVE (Ph+) ALL ; GI STROMAL TUMOR (GIST) ASSOCIATED WITH c-Kit MUTATION, AGGRESSIVE SYSTEMIC MASTOCYTOSIS WITHOUT D815V c-Kit MUTATION (OR UNKNOWN c-Kit STATUS) ; HYPEREOSINOPHILLIC SYNDROME AND/OR CHRONIC EOSINOPHILIC LEUKEMIA ; MYELODISPLACTIC / MYELOPROLIFERATIVE Dz ASSOCIATED WITH PLATELET-DERIVED GROWTH FACTOR RECEPTOR (PDGFR) GENE ARRANGEMENTS

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BCR-ABL KINASE INHIBITORS ; IMATINIB (GLEEVAC)

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USE: CM ; Ph+ALL RESISTANT OR INTOLERANT TO PRIOR THERAPY

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; DASATINIB (SPRYCEL)

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USE: CML, INCLUDING PT'S REFRACTORY OR INTOLERANT TO PRIOR THERAPY INCLUDING IMATINIB

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; NILOTINIB (TASIGNA)

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USE: NSCLC WITH KNOWN SENSITIZING EGFR MUTATION ; PANCREATIC Ca, LOCALLY ADVANCED UNRESECTABLE OR METASTATIC (FIRST-LINE GEMCITABINE) ; HEAD AND NECK CANCER

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EPIDERMAL GROWTH FACTOR INHIBITORS ; ERLOTINIB (TARCEVA)

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USE: METASTATIC COLORECTAL Ca (FIRST LINE WITH FOLFOX OR IRINOTECAN) ; HEAD AND NECK Ca (SQUAMOUS CELL)

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; CETUXIMAB (ERBITUX)

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USE: TUMORS OVEREXPRESSING HER2/NEU: BREAST Ca, METASTATIC (WITH PACLITAXEL, OR MONOTHERAPY AFTER CHEMO RELAPSE) ; GASTRIC OR GASTROESOPHAGEAL JUNCTION ADENOCARCINOMA, METASTATIC

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HER2 / NEU INHIBITORS ; TRASTUZUMAB (HERCEPTIN)

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USE: TX OF HER2 OVEREXPRESSING: BREAST, ADVANCED OR METASTATIC (WITH CAPECITABINE) ; BREAST Ca WITH LETROZOLE (POST-MENOPAUSAL WOMEN - HORMONE RECEPTOR POSITIVE)

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; LAPATINIB (TYKERB)

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USE: COLORECTAL Ca, METASTATIC WITH FOLFOX OR FOLFIRI ; NONSQUAMOUS NSCLC, UNRESECTABLE ; BREAST Ca, METASTATIC, HER-2 NEGATIVE WITH DOCETAXEL ; PROGRESSIVE GLIOBLASTOMA ; CLEAR-CELL RENAL CELL CANCER, METASTATIC ; AGE-RELATED MACULAR DEGENERATION (OFF-LABEL)

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ANGIOGENESIS INHIBITORS ; BEVACIZUMAB (AVASTIN)

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USE: GI STROMAL TUMOR (GIST) - DISEASE PROGRESSION ON IMATINIB) ; RENAL CELL Ca (ADVANCED) ; THYROID Ca (ADVANCED)

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; SUNITINIB (SUTENT)

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USE: MM, MANTLE CELL LYMPHOMA (RELAPSED OR REFRACTORY)

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PROTEASOME INHIBITOR ; BORTEZOMIB

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USE: NON-HODGKIN'S LYMPHOMA (R-CHOP - RITUXIMAB, CYCLOPHOSPHAMIDE, DOXORUBICIN, VINCRISTINE, PREDNISONE) ; ALSO FOR OTHER Ca'S: STEROID-REFRACTORY CHRONIC GVHD, POST-TRANSPLANT LYMPHOPROLIFERATIVE DISORDER (PTLD), AUTOIMMUNE Dz'S (RA, AUTOIMMUNE HEMOLYTIC ANEMIA (AIHA) IN HCILDREN, CHRONIC IMMUNE THROMBOCYTOPENIC PURPURA (ITP), REFRACTORY PHEMPHIGUS VULGARIS

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ANTI-CD20 MONOCLONAL ANTIBODY ; RITUXIMAB

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USE:

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; CYTIDINE ANALOGS