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THE

SECTION SUBJECT TOPIC

Hematology and Oncology Principles of Cancer Therapy Modalities of Cancer Therapy

MERCK MANUALS

FOR HEALTHCARE ONLINE MEDICAL LIBRARY PROFESSIONALS

COMMONLY USED ANTINEOPLASTIC DRUGS


DRUG MECHANISM OF ACTION COMMONLY RESPONSIVE TUMORS TOXICITY AND COMMENTS

ANTIMETABOLITES: FOLATE Methotrexate

ANTAGONISTS

Binds to dihydrofolate Acute lymphocytic reductase and interleukemia feres with thymidyl- Choriocarcinoma ate synthesis (women) Head and neck cancer Malignant lymphoma Osteogenic sarcoma Ovarian cancer

Mucosal ulceration Bone marrow suppression Increased toxicity with impaired renal function or ascitic fluid (with pooling of drug) Reversal of toxicity with leucovorin rescue at 24 h (1020 mg q 6 h 10 doses) Bone marrow suppression Mucosal ulceration

Pemetrexed

Inhibits thymidylate synthase

Lung cancer Mesothelioma Ovarian cancer

ANTIMETABOLITES: PURINE Cladribine Clofarabine

ANTAGONISTS

Inhibits ribonucleotide Leukemia reductase Lymphoma Inhibits DNA synthesis

Myelosuppression Immunosuppression

Myelosuppression Acute lymphocytic leukemia refractory to Immunosuppression at least 2 prior chemotherapy regimens Nausea Diarrhea Myelosuppression Immunosuppression Autoimmune reactions Myelosuppression Immunosuppression Myelosuppression Immunosuppression Myelosuppression Immunosuppression Nausea Vomiting

Fludarabine

6-Mercaptopurine Nelarabine Pentostatin

Leukemia Terminates DNA synthesis and Lymphoma inhibits ribonucleotide reductase Blocks de novo purine Acute leukemia synthesis Inhibits DNA synthesis Inhibits DNA synthesis Leukemia Lymphoma Leukemia

ANTIMETABOLITES: PYRIMIDINE Capecitabine

ANTAGONISTS

Inhibits thymidylate synthase

Breast cancer GI tumors

Mucositis Alopecia Myelosuppression Diarrhea Vomiting Hand or foot tenderness Ulceration

THE

SECTION SUBJECT TOPIC

Hematology and Oncology Principles of Cancer Therapy Modalities of Cancer Therapy

MERCK MANUALS

FOR HEALTHCARE ONLINE MEDICAL LIBRARY PROFESSIONALS

COMMONLY USED ANTINEOPLASTIC DRUGSContinued


DRUG MECHANISM OF ACTION COMMONLY RESPONSIVE TUMORS TOXICITY AND COMMENTS

Cytarabine

Terminates chain when incorporated into DNA

Myelosuppression Acute leukemia (especially nonlymphocytic) Nausea Lymphoma Vomiting Cerebellar toxicity (at high doses) Conjunctival toxicity (at high doses) Rash Breast cancer GI tumors Mucositis Alopecia Myelosuppression Diarrhea Vomiting Myelosuppression Hemolytic-uremic syndrome Myelosuppression

5-Fluorouracil

Inhibits thymidylate synthase

Gemcitabine

Hydroxyurea BIOLOGIC

Terminates chain when incorporated into DNA and inhibits ribonucleotide reductase Inhibits ribonucleotide reductase

Bladder cancer Lung cancer Pancreatic cancer Chronic myelocytic leukemia

RESPONSE MODIFIERS

Interferon-alfa

Has antiproliferative effect

Chronic myelocytic leukemia Hairy cell leukemia Kaposis sarcoma Lymphomas Melanoma Renal cell cancer

Fatigue Fever Myalgias Arthralgias Myelosuppression Nephrotic syndrome (rare)

BLEOMYCINS Bleomycin Causes DNA strands to break Lymphoma Squamous cell cancer Testicular cancer Anaphylaxis Chills and fever Rash Pulmonary fibrosis at dosage > 200 mg/m2 Requires renal excretion Myelosuppression Pulmonary toxicity (fibrosis) Myelosuppression Pulmonary toxicity (delayed) Renal toxicity

DNA ALKYLATING AGENTS: NITROSOUREAS Carmustine Alkylates DNA with Brain tumors restricted uncoiling Lymphoma and replication of strands Lomustine Same as for carmustine Brain tumors (astrocytoma, glioblastoma)

THE

SECTION SUBJECT TOPIC

Hematology and Oncology Principles of Cancer Therapy Modalities of Cancer Therapy

MERCK MANUALS

FOR HEALTHCARE ONLINE MEDICAL LIBRARY PROFESSIONALS

COMMONLY USED ANTINEOPLASTIC DRUGSContinued


DRUG MECHANISM OF ACTION COMMONLY RESPONSIVE TUMORS TOXICITY AND COMMENTS

DNA CROSS-LINKING DRUGS AND ALKYLATING AGENTS Breast cancer Bendamustine Form adducts with DNA, causing DNA Chronic lymphocytic Chlorambucil strands to break leukemia CyclophosphaGliomas mide Hodgkin lymphoma Ifosfamide Lymphoma Mechlorethamine Multiple myeloma (nitrogen Small cell lung cancer mustard) Testicular cancer Melphalan

Alopecia with high IV dosage Nausea Vomiting Myelosuppression Hemorrhagic cystitis (especially with cyclophosphamide and ifosfamide), which can be ameliorated with mesna Mutagenesis Secondary leukemias Aspermia Permanent sterility (possible) Neutropenia Nausea Vomiting Secondary leukemias Neutropenia Nausea Vomiting Secondary leukemias Acute anaphylaxis Hyperthermia Pancreatitis Hyperglycemia Hypofibrinogenemia Decreased libido Hot flushes Gynecomastia Nausea Vomiting Constipation Diarrhea Abdominal pain Headache Back pain Hot flushes Pharyngitis

Dacarbazine Form adducts with DNA Temozolomide

Melanoma Malignant glioma

Procarbazine

Unclear

Hodgkin lymphoma

ENZYMES Asparaginase

Depletes asparagine, on which leukemic cells depend

Acute lymphocytic leukemia

HORMONES Bicalutamide Flutamide Fulvestrant

Bind to androgen receptor

Prostate cancer

Binds to estrogen receptor

Metastatic breast cancer

THE

SECTION SUBJECT TOPIC

Hematology and Oncology Principles of Cancer Therapy Modalities of Cancer Therapy

MERCK MANUALS

FOR HEALTHCARE ONLINE MEDICAL LIBRARY PROFESSIONALS

COMMONLY USED ANTINEOPLASTIC DRUGSContinued


DRUG MECHANISM OF ACTION COMMONLY RESPONSIVE TUMORS TOXICITY AND COMMENTS

Leuprolide acetate

Inhibits gonadotropin secretion

Prostate cancer

Hot flushes Decreased libido Irritation at injection site Weight gain Fluid retention Hot flushes Hypercalcemia Deep venous thrombosis Osteoporosis Hot flushes

Megestrol acetate Tamoxifen

Progesterone agonist Binds to estrogen receptor

Breast cancer Endometrial cancer Breast cancer

HORMONES: AROMATASE INHIBITORS Anastrozole Block conversion of Breast cancer androgen to estrogen Exemestane Letrozole MONOCLONAL Alemtuzumab Bevacizumab
ANTIBODIES

Binds to B and T cells Lymphomas Binds to vascular endothelial growth factor Binds to CD33 on leukemic cells Binds to CD20 on lymphoid cells Colon cancer Renal cancer Acute myelocytic leukemia Lymphomas Lymphomas

Immunosuppression Hypersensitivity Bleeding Hypertension Myelosuppression Delivers radiation to cancer cells Myelosuppression Fever Rash Hypersensitivity Immunosuppression Hypersensitivity Cardiac toxicity Local extravasation causing tissue necrosis Myelosuppression, with leukopenia and thrombocytopenia 4 to 6 wk after treatment Alopecia Lethargy Fever Hemolytic-uremic syndrome

Gemtuzumab Ibritumomab tiuxetan

Binds to CD20 on Iodine-131 lymphoid cells tositumomab Tositumomab Rituximab Trastuzumab Binds to CD20 on B cells Binds to HER2/neu receptor

B-cell lymphoma Breast cancer

OTHER ANTIBIOTICS Mitomycin Inhibits DNA synthe- Breast cancer sis by acting as Colon cancer a bifunctional Gastric adenocarcinoma alkylator Lung cancer Transitional cell cancer of the bladder

THE

SECTION SUBJECT TOPIC

Hematology and Oncology Principles of Cancer Therapy Modalities of Cancer Therapy

MERCK MANUALS

FOR HEALTHCARE ONLINE MEDICAL LIBRARY PROFESSIONALS

COMMONLY USED ANTINEOPLASTIC DRUGSContinued


DRUG MECHANISM OF ACTION COMMONLY RESPONSIVE TUMORS TOXICITY AND COMMENTS

PLATINUM COMPLEXES Carboplatin Establishes cross links Breast cancer within and between Lung cancer DNA strands Ovarian cancer Cisplatin Same as for carboplatin Bladder cancer Breast cancer Head and neck cancer Gastric cancer Lung cancer (especially small cell) Testicular cancer Colon cancer

Myelosuppression Peripheral neuropathy Anemia Ototoxicity Nausea Vomiting Peripheral neuropathy Myelosuppression Myelosuppression Neuropathic throat pain Peripheral neuropathy Myelosuppression Diarrhea Nausea Constipation Peripheral neuropathy Myelosuppression Alopecia Rash Fluid retention Myelosuppression Alopecia Myalgia Arthralgia Neuropathy Alopecia Myelosuppression Peripheral neuropathy

Oxaliplatin

Same as for carboplatin

PROTEOSOME Bortezomib

INHIBITORS

Inhibits proteosome functions

Multiple myeloma

SPIDLE POISON (FROM PLANTS): TAXANES Docetaxel Promotes assembly of Breast cancer microtubules Head and neck cancer Lung cancer Ovarian cancer Paclitaxel Same as for docetaxel Bladder cancer Breast cancer Head and neck cancer Lung cancer Ovarian cancer

SPIDLE POISON (FROM PLANTS): VINCAS Breast cancer Vinblastine Arrests mitosis by inhibiting polymer- Ewings sarcoma ization of microLeukemia tubules Lymphomas Testicular cancer Vincristine Same as for vinblastine Acute leukemia Lymphoma

Peripheral neuropathy Ileus Syndrome of inappropriate antidiuretic hormone secretion Myelosuppression Neuropathy

Vinorelbine

Same as for vinblastine

Breast cancer Lung cancer

THE

SECTION SUBJECT TOPIC

Hematology and Oncology Principles of Cancer Therapy Modalities of Cancer Therapy

MERCK MANUALS

FOR HEALTHCARE ONLINE MEDICAL LIBRARY PROFESSIONALS

COMMONLY USED ANTINEOPLASTIC DRUGSContinued


DRUG MECHANISM OF ACTION COMMONLY RESPONSIVE TUMORS TOXICITY AND COMMENTS

TOPOISOMERASE INHIBITORS: ANTHRACYCLINES Daunorubicin Inhibits topoisomerase Leukemia (daunoII and causes DNA mycin) strands to break Doxorubicin Same as for daunorubicin Acute leukemia Breast cancer Lung cancer Lymphoma

Myelosuppression Cardiac toxicity at cumulative dosage > 1000 mg/m2 Nausea Vomiting Alopecia Myelosuppression Cardiac toxicity at cumulative dosage > 550 mg/m2 Myelosuppression Cardiac toxicity at cumulative dosage > 1000 mg/m2

Epirubicin

Same as for daunorubicin

Acute myelocytic leukemia Breast cancer Gastric cancer

TOPOISOMERASE INHIBITORS: CAMPTOTHECINS Irinotecan Inhibits Colon cancer topoisomerase I Lung cancer Rectal cancer Topotecan Same as for irinotecan Ovarian cancer Small cell lung cancer

Diarrhea Myelosuppression Alopecia Myelosuppression

TOPOISOMERASE INHIBITORS: PODOPHYLLOTOXINS Inhibit topoisomerase Acute leukemia Etoposide II and cause DNA Hodgkin lymphoma Teniposide strands to break Lymphoma Lung cancer (especially small cell) Testicular cancer

Nausea Vomiting Myelosuppression Peripheral neuropathy Increased toxicity in renal failure Neutropenia Cleared by liver and kidneys Neutropenia Nausea Vomiting Acne Diarrhea Leukopenia Hepatocellular toxicity Edema

Mitoxantrone

Same as for etoposide Acute leukemia Lymphoma

TYROSINE Erlotinib Gefitinib Imatinib

KINASE INHIBITORS

Inhibit epidermal growth factor receptor Inhibits Bcr-Abl kinase and c-kit kinase

Nonsmall cell lung cancer Chronic myelocytic leukemia GI stromal tumors

THE

SECTION SUBJECT TOPIC

Hematology and Oncology Principles of Cancer Therapy Modalities of Cancer Therapy

MERCK MANUALS

FOR HEALTHCARE ONLINE MEDICAL LIBRARY PROFESSIONALS

COMMONLY USED ANTINEOPLASTIC DRUGSContinued


DRUG MECHANISM OF ACTION COMMONLY RESPONSIVE TUMORS TOXICITY AND COMMENTS

Lapatinib

Inhibits Her2/neu activity

Breast cancer

Diarrhea Nausea Rash Vomiting Fatigue Hypertension Proteinuria

Sorafenib

Hepatocellular cancer Inhibits intracellular and cell surface Renal cancer kinases (eg, vascular endothelial growth factor receptors) Inhibits receptor tyrosine kinases GI stromal tumors Renal cancer

Sunitinib

Hypertension Proteinuria