Commonly Used Antineoplastic Drugs

7/31/2019 Commonly Used Antineoplastic Drugs

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Pemetrexed Inhibits thymidylatesynthase

Lung cancer

Mesothelioma

Ovarian cancer

ANTIMETABOLITES: PURINE ANTAGONISTS

Cladribine Inhibits ribonucleotidereductase

Leukemia

Lymphoma

Clofarabine Inhibits DNAsynthesis

Acute lymphocyticleukemia refractory toat least 2 priorchemotherapy regimens

Fludarabine Terminates DNAsynthesis and

inhibits ribonu-cleotide reductase

Leukemia

Lymphoma

6-Mercapto-purine

Blocks de novo purinesynthesis

Acute leukemia

Nelarabine Inhibits DNAsynthesis

Leukemia

Lymphoma

Pentostatin Inhibits DNAsynthesis

Leukemia

ANTIMETABOLITES: PYRIMIDINE ANTAGONISTS

Capecitabine Inhibits thymidylate

synthase

Breast cancer

GI tumors

Bone marrowsuppression

Mucosal ulceration

Myelosuppression

Immunosuppression

Myelosuppression

Immunosuppression

Nausea

Diarrhea

Myelosuppression

ImmunosuppressionAutoimmune reactions

Myelosuppression

Immunosuppression

Myelosuppression

Immunosuppression

Myelosuppression

Immunosuppression

Nausea

Vomiting

Mucositis

Alopecia

Myelosuppression

Diarrhea

Vomiting

Hand or foot tenderness

Ulceration

COMMONLY USED ANTINEOPLASTIC DRUGS

DRUGMECHANISMOF ACTION

COMMONLYRESPONSIVE TUMORS

TOXICITY ANDCOMMENTS

ANTIMETABOLITES: FOLATE ANTAGONISTS

Methotrexate Binds to dihydrofolatereductase and inter-feres with thymidyl-ate synthesis

Acute lymphocyticleukemia

Choriocarcinoma(women)

Head and neck cancer

Malignant lymphoma

Osteogenic sarcoma

Ovarian cancer

Mucosal ulceration

Bone marrow suppres-sion

Increased toxicity withimpaired renal functionor ascitic fluid (withpooling of drug)

Reversal of toxicity withleucovorin rescue at24 h (1020 mg q6 h 10 doses)

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Principles of Cancer Therapy

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2/7

5-Fluorouracil Inhibits thymidylatesynthase

Breast cancer

GI tumors

Gemcitabine Terminates chainwhen incorporatedinto DNA andinhibits ribonu-cleotide reductase

Bladder cancer

Lung cancer

Pancreatic cancer

Hydroxyurea Inhibits ribonucleotidereductase

Chronic myelocyticleukemia

BIOLOGIC RESPONSE MODIFIERS

Interferon-alfa Has antiproliferativeeffect


Hairy cell leukemia

Kaposis sarcoma

Lymphomas

Melanoma

Renal cell cancer

BLEOMYCINS

Bleomycin Causes DNA strandsto break

Lymphoma

Squamous cell cancer

Testicular cancer

DNA ALKYLATING AGENTS: NITROSOUREAS

Carmustine Alkylates DNA with

restricted uncoilingand replication ofstrands

Brain tumors

Lymphoma

Lomustine Same as for carmus-tine

Brain tumors (astrocy-toma, glioblastoma)

Mucositis

Alopecia

Myelosuppression

DiarrheaVomiting

Myelosuppression

Hemolytic-uremicsyndrome

Myelosuppression

Fatigue

Fever

Myalgias

ArthralgiasMyelosuppression

Nephrotic syndrome(rare)

Anaphylaxis

Chills and fever

Rash

Pulmonary fibrosis atdosage > 200 mg/m2

Requires renal excretion

Myelosuppression

Pulmonary toxicity(fibrosis)

Myelosuppression

Pulmonary toxicity(delayed)

Renal toxicity

COMMONLY USED ANTINEOPLASTIC DRUGSContinued





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THE

Cytarabine Terminates chainwhen incorporatedinto DNA

Acute leukemia (espe-cially nonlymphocytic)

Lymphoma

Myelosuppression

Nausea

Vomiting

Cerebellar toxicity(at high doses)

Conjunctival toxicity(at high doses)

Rash


3/7

DNA CROSS-LINKING DRUGS AND ALKYLATING AGENTS

Bendamustine

Chlorambucil

Cyclophospha-mide

Ifosfamide

Mechloreth-amine(nitrogenmustard)

Melphalan

Form adducts withDNA, causing DNAstrands to break

Breast cancer

Chronic lymphocyticleukemia

Gliomas

Hodgkin lymphoma

Lymphoma

Multiple myeloma

Small cell lung cancer

Testicular cancer

Alopecia with high IVdosage

Nausea

Vomiting

Myelosuppression

Hemorrhagic cystitis(especially withcyclophosphamide andifosfamide), which canbe ameliorated withmesna

MutagenesisSecondary leukemias

Aspermia

Permanent sterility(possible)

Dacarbazine

Temozolomide

Form adducts withDNA

Melanoma

Malignant glioma

Procarbazine Unclear Hodgkin lymphoma

ENZYMES

Asparaginase Depletes asparagine,on which leukemiccells depend

Acute lymphocyticleukemia

HORMONES

Bicalutamide

Flutamide

Bind to androgenreceptor

Prostate cancer

Fulvestrant Binds to estrogenreceptor

Metastatic breast cancer

Neutropenia

Nausea

Vomiting

Secondary leukemias

Neutropenia

Nausea

Vomiting

Secondary leukemias

Acute anaphylaxis

Hyperthermia

Pancreatitis

Hyperglycemia

Hypofibrinogenemia

Decreased libido

Hot flushes

Gynecomastia

Nausea

VomitingConstipation

Diarrhea

Abdominal pain

Headache

Back pain

Hot flushes

Pharyngitis






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4/7

Leuprolideacetate

Inhibits gonadotropinsecretion

Prostate cancer

Anastrozole

Exemestane

Letrozole

Block conversion of

androgen to estrogen

Breast cancer

MONOCLONAL ANTIBODIES

Alemtuzumab Binds to B and T cells Lymphomas

Bevacizumab Binds to vascularendothelial growthfactor

Colon cancer

Renal cancer

Gemtuzumab Binds to CD33 onleukemic cells

Acute myelocyticleukemia

Ibritumomabtiuxetan

Binds to CD20 onlymphoid cells

Lymphomas

Iodine-131

tositumomab

Tositumomab

Binds to CD20 on

lymphoid cells

Lymphomas

Rituximab Binds to CD20 onB cells

B-cell lymphoma

Trastuzumab Binds to HER2/neureceptor

Breast cancer

OTHER ANTIBIOTICS

Mitomycin Inhibits DNA synthe-sis by acting asa bifunctionalalkylator

Breast cancer

Colon cancer

Gastric adenocarcinoma

Lung cancer

Transitional cell cancerof the bladder

Megestrolacetate

Progesterone agonist Breast cancer

Endometrial cancer

Tamoxifen Binds to estrogenreceptor

Breast cancer

HORMONES: AROMATASE INHIBITORS

Hot flushes

Decreased libido

Irritation at injection site

Osteoporosis

Hot flushes

Immunosuppression

Hypersensitivity

Bleeding

Hypertension

Myelosuppression

Delivers radiation tocancer cells

Myelosuppression

Fever

Rash

Hypersensitivity

Immunosuppression

Hypersensitivity

Cardiac toxicity

Local extravasation caus-ing tissue necrosis

Myelosuppression, withleukopenia and throm-bocytopenia 4 to 6 wkafter treatment

Alopecia

Lethargy

Fever

Hemolytic-uremicsyndrome

Weight gain

Fluid retention

Hot flushes

Hypercalcemia

Deep venous thrombosis






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THE


5/7

PLATINUM COMPLEXES

Oxaliplatin Same as forcarboplatin

Colon cancer

PROTEOSOME INHIBITORS

Bortezomib Inhibits proteosomefunctions

Multiple myeloma

SPIDLE POISON (FROM PLANTS): TAXANES

Docetaxel Promotes assembly of microtubules

Breast cancer


Lung cancer

Ovarian cancer

Paclitaxel Same as for docetaxel Bladder cancer

Breast cancer


Lung cancer

Ovarian cancer

SPIDLE POISON (FROM PLANTS): VINCAS

Vinblastine Arrests mitosis byinhibiting polymer-ization of micro-tubules

Breast cancer

Ewings sarcoma

Leukemia

Lymphomas

Testicular cancer

Vincristine Same as forvinblastine

Acute leukemia

Lymphoma

Carboplatin Establishes cross linkswithin and betweenDNA strands

Breast cancer

Lung cancer

Ovarian cancer

Cisplatin Same as forcarboplatin

Bladder cancer

Breast cancer


Gastric cancer

Lung cancer (especiallysmall cell)

Testicular cancer

Myelosuppression

Neuropathic throat pain

Peripheral neuropathy

Myelosuppression

Diarrhea

Nausea

Constipation


Myelosuppression

Alopecia

Rash

Fluid retention

Myelosuppression

Alopecia

Myalgia

Arthralgia

Neuropathy

Alopecia

Myelosuppression



Ileus

Syndrome ofinappropriateantidiuretic hormonesecretion

Myelosuppression


Anemia

Ototoxicity

Nausea

Vomiting


Myelosuppression






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Vinorelbine Same as forvinblastine

Breast cancer

Lung cancer

Myelosuppression

Neuropathy


6/7

Daunorubicin(dauno-mycin)

Inhibits topoisomeraseII and causes DNAstrands to break

Leukemia

Doxorubicin Same as fordaunorubicin

Acute leukemia

Breast cancer

Lung cancer

Lymphoma

Epirubicin Same as fordaunorubicin

Acute myelocyticleukemia

Breast cancer

Gastric cancer

TOPOISOMERASE INHIBITORS: CAMPTOTHECINS

Irinotecan Inhibitstopoisomerase I

Colon cancer

Lung cancer

Rectal cancer

Topotecan Same as for irinotecan Ovarian cancer

Small cell lung cancer

TOPOISOMERASE INHIBITORS: PODOPHYLLOTOXINS

EtoposideTeniposide

Inhibit topoisomeraseII and cause DNAstrands to break

Acute leukemiaHodgkin lymphoma

Lymphoma

Lung cancer (especiallysmall cell)

Testicular cancer

Mitoxantrone Same as for etoposide Acute leukemia

Lymphoma

TYROSINE KINASE INHIBITORS

Erlotinib

Gefitinib

Inhibit epidermalgrowth factorreceptor

Nonsmall cell lungcancer

Imatinib Inhibits Bcr-Ablkinase and c-kitkinase


GI stromal tumors

TOPOISOMERASE INHIBITORS: ANTHRACYCLINES

Myelosuppression

Cardiac toxicity atcumulative dosage> 1000 mg/m2

Nausea

Vomiting

Alopecia

Myelosuppression

Cardiac toxicity atcumulative dosage

> 550 mg/m

2

Myelosuppression

Cardiac toxicity at cumu-lative dosage > 1000mg/m2

Diarrhea

Myelosuppression

Alopecia

Myelosuppression

NauseaVomiting

Myelosuppression


Increased toxicity inrenal failure

Neutropenia

Cleared by liver andkidneys

Neutropenia

Nausea

Vomiting

Acne

Diarrhea

Leukopenia

Hepatocellular toxicity

Edema






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7/7

Lapatinib Inhibits Her2/neuactivity

Breast cancer

Sunitinib Inhibits receptortyrosine kinases

GI stromal tumors

Renal cancer

Sorafenib Inhibits intracellularand cell surfacekinases (eg, vascularendothelial growthfactor receptors)

Hepatocellular cancer

Renal cancer

Diarrhea

Nausea

Rash

Vomiting

Fatigue

Hypertension

Proteinuria

Hypertension

Proteinuria






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THE

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Commonly Used Antineoplastic Drugs