ANTINEOPLASTICS Flashcards
1 gram of tumor is equivalent to
10^9 or 1 billion cells
A very common adverse reaction of alkylating agents used in the tx of cancer
Alopecia
ALKYLATING AGENTS: NITROGEN MUSTARDS
Alkylating agents replace H with an alkyl group, which causes ____.
DNA strand breakage
ALKYLATING AGENTS: NITROGEN MUSTARDS
Mainstay therapy for solid tumors followed by autologous bone marrow transplantation
Thiotepa
ALKYLATING AGENTS: NITROGEN MUSTARDS
Dialkylating agent drug of choice for Hodgkin’s disease
Mechlorethamine
ALKYLATING AGENTS: NITROGEN MUSTARDS
For germ cell testicular cancer
Ifosfamide
ALKYLATING AGENTS: NITROGEN MUSTARDS
Causes sulfur stripping
Busulfan
ALKYLATING AGENTS: NITROGEN MUSTARDS
Cell cycle non-specific phosphoramide mustard (major metabolite)
Cyclophosphamide
ALKYLATING AGENTS: NITROGEN MUSTARDS
For multiple myeloma
Melphalan
ALKYLATING AGENTS: NITROGEN MUSTARDS
1st line agent for chronic lymphocytic leukemia and macroglobulinemia
Chlorambucil
ALKYLATING AGENTS: ORGANOPLATINUM
MOA of organoplatinum
DNA strands cross-linking
ALKYLATING AGENTS: ORGANOPLATINUM
Most reactive and most effective in platinating DNA
Cisplatin
ALKYLATING AGENTS: ORGANOPLATINUM
Carboplatin is administered with ____ to reduce toxicity
1,1-cyclobutane-dicarboxylate
ALKYLATING AGENTS: ORGANOPLATINUM
____ is administered with 1,1-cyclobutane-dicarboxylate to reduce toxicity
Carboplatin
ALKYLATING AGENTS: ORGANOPLATINUM
Activated in low chloride environment, not recognized by MMR
Oxaliplatin
ALKYLATING AGENTS
Alkylates DNA with restricted uncoiling and replication of strands
Nitrosoureas
ALKYLATING AGENTS: NITROSOUREAS
1st line agent for metastatic brain tumor
Lomustine
ALKYLATING AGENTS: NITROSOUREAS
2nd line agent for Hodgkin’s disease
Lomustine
ALKYLATING AGENTS: NITROSOUREAS
For brain tumors and can penetrate BBB
Carmustine
ALKYLATING AGENTS: OTHERS
3 agents for Hodgkin’s lymphoma
- Mechlorethamine
- Lomustine
- Procarbazine
ALKYLATING AGENTS: OTHERS
2 agents that form DNA adducts
- Dacarbazine
- Temozolomide
ALKYLATING AGENTS: OTHERS
Involved in hydroxylation of methyl group
Altretamine
ALKYLATING AGENTS: OTHERS
2nd line agent for ovarian cancer
Altretamine
ALKYLATING AGENTS: OTHERS
Induces hyperglycemia on animal model
Streptozocin
ALKYLATING AGENTS: OTHERS
Source of streptozocin
Streptomyces achromogenes subsp. Strepzoticus
ALKYLATING AGENTS: OTHERS
Antineoplastic that is not considered an anti-metabolite
Etoposide
Compounds closely related in structure to a cellular precursor (N-base)
Anti-metabolites
ANTI-METABOLITES
MOA of anti-metabolites
Prevention of biosynthesis by enzyme inhibition
ANTI-METABOLITES
Designed to interact at cofactor sites for enzymes involve in the biosynthesis of nucleic acid bases
Folates (Anti-folates)
ANTI-METABOLITES: FOLATES
First drug to produce substantial remissions in leukemia
Methrotrexate
(MTX)
ANTI-METABOLITES: FOLATES
MOA of Methrotrexate (MTX)
- Dihydrofolate reductase binding (DHFR)
- Thymidylate synthase (TS) interference
ANTI-METABOLITES: FOLATES
A pyrrolopyrimidine analog
Pemetrexed
ANTI-METABOLITES: FOLATES
MOA of Pemetrexed
Thymidylate synthase (TS) inhibition
ANTI-METABOLITES: FOLATES
Structually similar to MTX and approved for the tx of pneumocystis carinii pneumonia (PCP) in HIV/AIDS patients
Trimetrexate
ANTI-METABOLITES: FOLATES
MOA of hydroxyurea
Ribonucleotide Reductase inhibition
ANTI-METABOLITES: PURINES
MOA of 6-mercaptopurine
De Novo Purine synthesis blocking
ANTI-METABOLITES: PURINES
Primary treatment for acute leukemia
6-mercaptopurine + 6-thioguanine
ANTI-METABOLITES: PURINES
For chronic lymphocytic leukemia and non-Hodgkin’s lymphoma
Fludarabine
ANTI-METABOLITES: PURINES
Deoxyadenosine analog for hairy cell leukemia
Cladribine
ANTI-METABOLITES: PURINES
MOA of Pentostatin
Adenosine deaminase inhibition -> increase dATP
ANTI-METABOLITES: PYRIMIDINES
Palliative tx of carcinoma of the breast, colon, pancreas, rectim, and stomach
5-Fluorouracil
(5-FU)
ANTI-METABOLITES: PYRIMIDINES
Fluoropyrimidine deoxynucleoside analog for GI adenocarcinoma metastatic to the liver
Floxuridine
(FUDR)
ANTI-METABOLITES: PYRIMIDINES
MOA of 5-FU and FUDR
Thymidylate synthase (TS) inhibition -> DNA synthesis inhibition
ANTI-METABOLITES: PYRIMIDINES
Fluoropyrimidine carbamate prodrug of 5-FU for metastatic breast and colorectal cancer
Capecitabine
ANTI-METABOLITES: PYRIMIDINES
Drug of choice for locally advanced or metastatic adenocarcinoma of the pancreas
Gemcitabine
(+) Cisplatin
ANTI-METABOLITES: PYRIMIDINES
Drug of choice for inoperable locally advanced or metastatic NSCLC
Gemcitabine
ANTI-METABOLITES: PYRIMIDINES
A potent radiosensitizer
Gemcitabine
ANTI-METABOLITES: PYRIMIDINES
Cytosine arabinoside tx for acute agranulocytic leukemia
Cytarabine
ANTIBIOTICS
Antibiotic that do not possess clinically useful anti-malignant property
Streptomycin
ACTINOMYCIN
Source of dactinomycin
Strep. parvilus
ACTINOMYCIN
Tx of rhabdomyosarcoma and Wilms’ tumor in children
Dactinomycin
ACTINOMYCIN
Lifesaving tx for women with choriocarcinoma resistant to MTX
Dactinomycin
ANTHRACYCLINES
MOA of anthracyclines
- Topoisomerase II inhibition
- Intercalation of the planar ring system
ANTHRACYCLINES
Isolated from Strep. peucetius for non-lymphocytic and lymphocytic leukemia
Daunorubicin
ANTHRACYCLINES
Cardiotoxic isolated from Strep. peucetius var. caesius
Doxorubicin
ANTHRACYCLINES
No 4-methoxy group and terminal side chain for blast phase chronic myelogenous carcinoma
Less cardiotoxic than doxorubicin
Idarubicin
ANTHRACYCLINES
4’-epimer of doxorubicin
Epirubicin
ANTHRACYCLINES
BCG-refractory carcinoma of urinary bladder
Valrubicin
ANTHRACYCLINES
Tint urine blue
Mitoxantrone
GLYCOPEPTIDES
Isolated from Streptomyces verticillus
Bleomycin
GLYCOPEPTIDES
Palliative treatment of squamous cell carcinoma with no myelotoxicity (bone marrow)
Bleomycin
GLYCOPEPTIDES
Isolated from Streptomyces caespitosus
Mitomycin C
GLYCOPEPTIDES
Bioreductive alkylating agents
Mitomycin C
EPIPODOPHYLLOTOXIN (PLANT PRODUCTS)
Source of epipodophyllotoxins
Mayapple (Mandrake) Root
EPIPODOPHYLLOTOXIN (PLANT PRODUCTS)
MOA of epipodophyllotoxins
Inhibition of microtubule function (topoisomerase II)
EPIPODOPHYLLOTOXIN (PLANT PRODUCTS)
For testicular cancer and small cell lung cancer
Etoposide
EPIPODOPHYLLOTOXIN (PLANT PRODUCTS)
A more potent inhibitor of topoisomerase II for acute lymphoblastic leukemia
Teniposide
CAMPTOTHECINS (PLANT PRODUCTS)
MOA of camptothecins
Inhibitors of topoisomerase I
CAMPTOTHECINS (PLANT PRODUCTS)
Source of camptothecins
Camptotheca acuminata
CAMPTOTHECINS (PLANT PRODUCTS)
Semi-synthetic analog of camptotechin
Irinotecan
CAMPTOTHECINS (PLANT PRODUCTS)
Drug of choice for metastatic colon cancer
5-FU + Leucovorin + Irinotecan
CAMPTOTHECINS (PLANT PRODUCTS)
2nd line single agent in colorectal cancer
Irinotecan
CAMPTOTHECINS (PLANT PRODUCTS)
A/E: Microscopic hematuria (blood in urine)
Topotecan
VINCA ALKALOIDS (PLANT PRODUCTS)
Source of vinca alkaloids
Catharanthus roseus (periwinkle)
VINCA ALKALOIDS (PLANT PRODUCTS)
MOA of vinca alkaloids
Arrest of mitosis
(Inhibition of microtubule polymerization)
VINCA ALKALOIDS (PLANT PRODUCTS)
Dihydroindole nitrogen attached to vincristine
Formyl
VINCA ALKALOIDS (PLANT PRODUCTS)
Dihydroindole nitrogen attached to vinblastine
Methyl
VINCA ALKALOIDS (PLANT PRODUCTS)
ABVD regimen used in the treatment of
Hodgkin’s lymphoma
- Adriamycin
- Bleomycin
- Vinblastine
- Dacarbazine
VINCA ALKALOIDS (PLANT PRODUCTS)
Extravasation with the use of vincas is managed by ____.
Hyaluronic Acid + Heat
VINCA ALKALOIDS (PLANT PRODUCTS)
Semi-synthetic agent for NSCLC
Vinorelbine
TAXANES (PLANT PRODUCTS)
Source of taxanes
Taxus brevifolia or Taxus baccatta (pacific yew tree)
TAXANES (PLANT PRODUCTS)
Taxanes are administered with ____ and ____ due to poor water solubility
- Cremophor EL
- Ethanol
TAXANES (PLANT PRODUCTS)
MOA of taxanes
β-tubulin binding
same with vincas
TAXANES (PLANT PRODUCTS)
Highly plasma protein bound drug that promotes assembly of microtubules and may cause bradycardia
Paclitaxel
TAXANES (PLANT PRODUCTS)
Semi-synthetic taxane that can cause reversible fluid retention
Docetaxel
TAXANES (PLANT PRODUCTS)
Semisynthetic amide analog of epothilone B from Sorangium cellulosum
Ixabepilone
PROTEIN (TYROSINE) KINASE INHIBITORS
Enzymes that add a phosphate (PO4) group to a protein or other organic molecule, which can turn a protein off
Protein kinases
PROTEIN (TYROSINE) KINASE INHIBITORS
Inhibits epidermal growth factor receptor
Erlotinib
A/E: Acne, Diarrhea
PROTEIN (TYROSINE) KINASE INHIBITORS
Inhibits BCR-ABL kinase and c-kit kinase
Imatinib
PROTEIN (TYROSINE) KINASE INHIBITORS
Inhibits HER2/NEU activity
Lapatinib
PROTEIN (TYROSINE) KINASE INHIBITORS
Inhibits intracellular and cell surface kinase like VEGFR
Sorafenib
PROTEIN (TYROSINE) KINASE INHIBITORS
Inhibits receptor tyrosine kinases
Sunitinib
HORMONES
Androgen receptor antagonist for advance prostate cancer
Bicalutamide and Flutamide
HORMONES
Binds to estrogen receptor for the tx of metastatic breast cancer
Fulvestrant
HORMONES
Inhibits gonadotropin secretion for prostate cancer
Leuprolide acetate
HORMONES
A progesterone antagonist for advanced breast or endometrial cancer
Megestrol acetate
HORMONES
Selective Estrogen Receptor Modulator (SERM) for advanced breast cancer in postmenopausal women
Tamoxifen
HORMONES
Selective Estrogen Receptor Modulator (SERM) for advanced breast cancer in postmenopausal women
Tamoxifen
HORMONES
A non-steroidal triphenylethylene agent for advanced breast cancer
Tamoxifen
HORMONES
Benzothiophene derivative SERM
Raloxifene
HORMONES
Palliative treatment for advanced prostate carcinoma, breast cancer, and endometriosis
Goserelin
HORMONES
For inoperable adrenal cortical carcinoma
Mitotane
HORMONES
Palliative treatment for metastatic breast cancer
Dromostanolone
HORMONES
Palliative treatment for advanced or disseminated breast cancer
Testolactone
HORMONES
For Cushing’s syndrome
Aminoglutethimide
HORMONES
SERM for metastatic breast cancer
Toremifene
HORMONES
Blocks conversion of androgen to estrogen
Aromatase Inhibitors
AROMATASE INHIBITORS (HORMONES)
For hormone dependent breast cancer
Exemestane
AROMATASE INHIBITORS (HORMONES)
First specific aromatase inhibitor for locally advanced or metastatic breast cancer
Anastrozole
AROMATASE INHIBITORS (HORMONES)
Nonsteroidal aromatase inhibitors for locally advanced or metastatic breast cancer
Letrozole
IMMUNOTHERAPY
For hairy cell leukemia and hairy cell leukemia in patients 18 years old or older
Interferon Alfa-2A
IMMUNOTHERAPY
For hairy cell leukemia and malignant melanoma
Interferon Alfa-2B
IMMUNOTHERAPY
Stimulates T-Cell growth and regulation, proliferation and immunoglobulin production in B lymphocytes, and macrophage activity enhancement
Aldesleukin
MONOCLONAL ANTIBODIES
Binds to B and T cells
Alemtuzumab
MONOCLONAL ANTIBODIES
Binds to vascular endothelial growth factor
Bevacizumab
MONOCLONAL ANTIBODIES
Binds to CD33 on leukemic cells
Gemtuzumab
MONOCLONAL ANTIBODIES
Binds to CD20 on lymphoid cells
Tositumomab
MONOCLONAL ANTIBODIES
Genetically engineered chimeric monoclonal antibody against CD20 antigen expressed on the surfaces of malignant B lymphocytes
Rituximab
MONOCLONAL ANTIBODIES
Single agent for metastatic breast cancer
Trastuzumab
MONOCLONAL ANTIBODIES
Binds with human epidermal growth factor receptor type 2 (HER2) and neu receptor
Trastuzumab
PROTEOSOME INHIBITOR
2 proteosome inhibitors
- Bortezomib
- Vorinostat
MISCELLANEOUS
For acute promyelocytic leukemia (APL)
Arsenic Trioxide
MISCELLANEOUS
For cutaneous T-cell lymphoma in patient refractory prior to systemic theraphy
Bexarotene
MISCELLANEOUS
Adjunct therapy to prevent rejection of renal heterotransplants
Azathioprine
MISCELLANEOUS
Enzyme from E. coli
Asparaginase
MISCELLANEOUS
MOA of Asparaginase
Reduces asparagine in plasma makng it unavailable for leukemic cells
MISCELLANEOUS
Promotes bone marrow recovery in patients who underwent autologous bone marrow transplantation
Sargramostim
MISCELLANEOUS
GM-CSF from Saccharomyces cerevisiae or E. Coli
Sargramostim
CYTOPROTECTIVES
For ifosfamide-induced hemorrhagic cystitis
Mesna
CYTOPROTECTIVES
Reduce accumulative toxicity from cisplatin and xerostoma
Amifostine
CYTOPROTECTIVES
Potent intracellular chelating agent to reduce doxurubicin toxicity
Dexrazoxane