Antineoplastics Flashcards
Cyclophosphamide
Nitrogen mustards
Alkylating agents
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Ifosfamide
Nitrogen mustards
Alkylating agents
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Mechlorethamine
Nitrogen mustards
Alkylating agents
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Melphalan
Nitrogen mustards
Alkylating agents
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Chlorambucil
Nitrogen mustards
Alkylating agents
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Procarbazine
Methylhydrazine derivative
Alkylating agent
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Busulfan
Alkyl sulfonate
Alkylating agent
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Carmustine
Nitrosureas
Alkylating agent
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Streptozocin
Nitrosureas
Alkylating agent
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Bendamustine
Nitrosureas
Alkylating agent
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Dacarbazine
Triazene
Alkylating agent
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Temozolomide
Triazene
Alkylating agent
covalent linkages DNA»_space;inter/intrastrand crosslinking
CCNS
Cisplatin
Platinum coordination complexes
Not really an alkylating agent, forms covalent bonds with DNA
CCNS
Carboplatin
Platinum coordination complexes
Not really an alkylating agent, forms covalent bonds with DNA
CCNS
Oxaliplatin
Platinum coordination complexes
Not really an alkylating agent, forms covalent bonds with DNA
CCNS
Methotrexate
Folic acid analog
Inhibits DHF reductase»_space; nonthymidylate or purine nucleotide synthesis
CCS- S phase
Pemetrexed
Folic acid analog
Inhibits DHF reductase»_space; no thymidylate or purine nucleotide synthesis
CCS- S phase
Fluorouracil (5-FU)
Pyrimidine analog
Prodrug, blocks thymidylate synthetase»_space; no thymidylate synthesis. Active compounds incorporated into DNA and RNA»_space; no DNA synthesis, no RNA processing, no translation
CCS- S phase
Capecitabine
Pyrimidine analog
CCS- S phase
Cytarabine
Pyrimidine analog
Inhibits DNA polymerase alpha and beta, blocks DNA synthesis and repair, incorporates into DNA and interferes with chain elongation and ligation
CCS- S phase
Gemcitabine
Pyrimidine analog
CCS- S phase
5-aza-cytidine
Pyrimidine analog
CCS- S phase
Deoxy-5-aza-cytabine
Pyrimidine analog
CCS- S phase
Mercaptopurine
Purine analog
Incorporated into triphosphates»_space;inhibits purine, DNA, RNA synthesis
CCS-S phase
Pentostatin
Purine analog
Incorporated into triphosphates»_space;inhibits purine, DNA, RNA synthesis
CCS-S phase
Fludarabine
Purine analog
Incorporated into triphosphates»_space;inhibits purine, DNA, RNA synthesis
CCS-S phase
Clofarabine
Purine analog
Incorporated into triphosphates»_space;inhibits purine, DNA, RNA synthesis
CCS-S phase
Nelarabine
Purine analog
Incorporated into triphosphates»_space;inhibits purine, DNA, RNA synthesis
CCS-S phase
Thioguanine (6-TG)
Purine analog
Incorporated into triphosphates»_space;inhibits purine, DNA, RNA synthesis
CCS-S phase
Vinblastine
Vinca alkaloid
Natural product
Binds B tubulin and inhibits microtubule assembly, destabilize
CCS-M phase
Vincristine
Vinca alkaloid
Natural product
Binds B tubulin and inhibits microtubule assembly, destabilize
CCS-M phase
Vinorelbine
Vinca alkaloid
Natural product
Binds B tubulin and inhibits microtubule assembly, destabilize
CCS-M phase
Paclitaxel
Taxane
Natural product
Binds B tubulin and promotes microtubule formation and stabilization
CCS-M phase
Docetaxel
Taxane
Natural product
Binds B tubulin and promotes microtubule formation and stabilization
CCS-M phase
Etoposide
Epipodophyllotoxin
Natural product
Inhibits topoisomerase II»_space; DNA damage by strand breakage
CCS- G2-S Phase
Teniposide
Epipodophyllotoxin
Natural product
Inhibits topoisomerase II»_space; DNA damage by strand breakage
CCS- G2-S Phase
Topotecan
Camptothecin
Natural product
Inhibits topoisomerase I»_space; DNA damage and block replication and transcription
CCS
Irinotecan
Camptothecin
Natural product
Inhibits topoisomerase I»_space; DNA damage and block replication and transcription
CCS
Doxorubicin
Anthracycline
Natural product
Inhibits topoisomerase II, intercalates DNA and blocks synthesis of DNA and RNA, generates O2 free radicals, alter cell membrane fluidity
CCNS
Daunorubicin
Anthracycline
Natural product
Inhibits topoisomerase II, intercalates DNA and blocks synthesis of DNA and RNA, generates O2 free radicals, alter cell membrane fluidity
CCNS
Dactinomycin
Antibiotic
Natural product
Binds double strand DNA and intercalates between G-C base pairs, prevents transcription
CCNS
Bleomycin
Anthracenedione
Natural product
Binds DNA»_space; double and single strand breaks, prevents DNA synthesis
CCS- G2 phase
Mitoxantrone
Anthracenedione
Natural product
Mitomycin
Anthracenedione
Natural product
Yondelis
Echinocandin
Natural product
L-Asparaginase
Enzyme Natural product Hydrolyzes asparagine >> no protein synthesis in cells that can't make their own asparagine Active against ALL CCS-G1
Pegaspargase
Enzyme Natural product Hydrolyzes asparagine >> no protein synthesis in cells that can't make their own asparagine Active against ALL CCS-G1
Hydroxyurea
Substituted urea
Inhibits ribonucleoside diphosphate reductase»_space; can’t make deoxyribonucelotides
CCS- S phase
Tretinoin
Differentiating agent
All trans retinoic acid
Binds nuclear receptors»_space; granulocyte differentiation
Active against Acute promyelocytic leukemia with t(15:17)
CCNS
Arsenic Trioxide
Differentiating agent
Unknown MOA, degrades PML/RAR alpha chimeric protein and induces apoptosis using caspase and cytochrome C activation
Active against Acute promyelocytic leukemia with t(15:17)
CCNS
Vorinostat
Histone deacetylase inhibitor
Differentiating agent
Alterations in chromatin structure and transcription factor activation»_space; cell death
CCNS
Interferon alpha
Biological response modifier
Inhibit cell growth, alter differentiation, interferes with oncogene expression, alters cell surface Ag expression, increases phagocytic activity of macrophages, augments cytotoxic lymphocytes
CCNS
Interleukin 2
Biological response modifier
Proliferation of activated T cells, secretion of cytokines from NKs and monocytes»_space; increased cytotoxic killing by T cells and NK cell
CCNS
Thalidomide
Immunomodulator
Anti-angiogenic and immunomodulatory, inhibits TNF alpha signaling
CCNS
Lenalidomide
Immunomodulator
Anti-angiogenic and immunomodulatory, inhibits TNF alpha signaling
CCNS
Leucovorin
Methotrexate rescue
Mesna
Cyclophosphamide recue bladder
Sargramostim
GMCSF
Filgrastim
GCSF
Pegfilgrastim
GCSF
Oprelvekin
IL-11, thrombopoietic
Erythropoietin
Erythropoiesis
Darbepoeitin
Erythropoiesis
Ondansetron
Serotonin antagonist
Imatinib
BCR-ABL
also PDGFR, cKit, stem cell factor
Dasatinib
BCR-ABL
also Src, cKit, PDGFR
Nilotinib
BCR-ABL
also cKit, PDGFR
Gefitinib
EGFR
Erlotinib
EGFR
Sorafenib
multikinase inhibitor
RAF kinases and cell surface kinase receptors
Sunitinib
multikinase inhibitor
RAF kinases and cell surface kinase receptors
Lapatinib
Her2/Neu internal domain
Bortezomib
Proteosome inhibitor
Temsirolimus
mTOR inhibitor
Immunosuppresant, inhibit cell cycle and angiogenesis, promotes apoptosis
Everolimus
mTOR inhibitor
Immunosuppresant, inhibit cell cycle and angiogenesis, promotes apoptosis
Rituximab
CD20
B lymphocytes
Alemtuzumab
CD52
B and T lymphocytes, NKs, monocytes, macrophages, come granulocytes
Gemtuzumab
CD33
internalization of antibody +ozogamicin»_space; DNA ds breaks and cell death
Leukemic blast cells
Trastuzumab
Her2/Neu
Ibritumomab
CD20
Combined with a chelator, acts as delivery of radioactive isotopes to cancer cells
Tositumomab
CD20
Combined with a chelator, acts as delivery of radioactive isotopes to cancer cells
Cetuximab
EGFR
Bevacizumab
VEGF