Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
57 Cards in this Set
- Front
- Back
|
Methotrexate
|
Dihydrofolate reductase inhibitor; especially decreases thymidine
|
|
|
6-Mercaptopurine
|
Inhibit de novo synthesis of purine rings
|
|
|
6-Thioguanine
|
Inhibit de novo synthesis of purine rings
|
|
|
Cladribine
|
Inhibits do novo purine synthesis by inhibiting ADA; also inhibits elongation of DNA
|
|
|
Fludarabine
|
Adenosine analog; incorporated into DNA, impairs protein function
|
|
|
5-Fluorouracil
|
Pyrimidine analog; inhibits thymidylate synthase (non-competitive)
|
|
|
Capecitabine
|
5-FU prodrug; more tumor-selective than 5-FU
|
|
|
Floxuridine
|
5-FU analog
|
|
|
Cytarabine
|
Analog of 2-deoxycytidine, a pyrimidine antagonist; inhibits DNA synthesis
|
|
|
Gemcitabine
|
Cyosine analog; incorporated into growing DNA strand, inhibiting strand elongation
|
|
|
Bleomycin
|
Forms complex with DNA and with Fe2+
Undergoes oxidation to DNA-Bleomycin-Fe3+ which produces free radicals and subsequent DNA strand breakage |
|
|
Dactinomycin
|
Intercalates into DNA - minor groove
Interferes with RNA synthesis Induces single-strand breaks |
|
|
Daunorubicin
|
Anthracycline
Intercalates into DNA Inhibits RNA and DNA synthesis Interferes with topo-II, leading to double strand breaks Interact with P450, product interacts with O2, producing free radicals |
|
|
Doxorubicin
|
Anthracycline
Intercalates into DNA Inhibits RNA and DNA synthesis Interferes with topo-II, leading to double strand breaks Interact with P450, product interacts with O2, producing free radicals |
|
|
Epirubicin
|
Anthracycline
Intercalates into DNA Inhibits RNA and DNA synthesis Interferes with topo-II, leading to double strand breaks Interact with P450, product interacts with O2, producing free radicals |
|
|
Idarubicin
|
Anthracycline
Intercalates into DNA Inhibits RNA and DNA synthesis Interferes with topo-II, leading to double strand breaks Interact with P450, product interacts with O2, producing free radicals |
|
|
Mechlorethamine
|
Nitrogen mustard
Cross-links guanine residues in DNA |
|
|
Cyclophosphamide
|
Nitrogen mustard
Undergoes biotransformation in the liver (P450) to active phosphoramide mustard Cross-links DNA |
|
|
Ifosfamide
|
Nitrogen mustard
Undergoes biotransformation in the liver (P450) to active phosphoramide mustard Cross-links DNA |
|
|
Carmustine
|
Nitrosourea
Alkylate DNA, leading to impaired replication and RNA synthesis Also facilitate carbamoylation of key enzymes, leading to defective function Relatively limited utility in brain cancers |
|
|
Lomustine
|
Nitrosourea
Alkylate DNA, leading to impaired replication and RNA synthesis Also facilitate carbamoylation of key enzymes, leading to defective function Relatively limited utility in brain cancers |
|
|
Streptozocin
|
Nitrosourea
Alkylate DNA, leading to impaired replication and RNA synthesis Also facilitate carbamoylation of key enzymes, leading to defective function Relatively limited utility in β-islet cell tumors |
|
|
Dacarbazine
|
Triazene
Undergoes biotransformation to methylcarbonium ions that can attack nucleophilic groups in DNA |
|
|
Temozolomide
|
Triazene
Similar to dacarbazine, but does not require P450 for biotransformation and has efficacy in treatment-resistant gliomas and anaplastic astrocytomas |
|
|
Melphalan
|
Nitrogen mustard
Used in multiple myeloma |
|
|
Chlorambucil
|
Nitrogen mustard
Bifunctional alkylating agent Useful in CLL |
|
|
Busuflan
|
Nitrogen mustard
Bifunctional alkylating agent Useful in chronic granulocytic leukemias |
|
|
Docetaxel
|
Binds to β-tubulin and promotes polymerization and stabilization, leading to arrest in G2/M and cell death
More potent than paclitaxel |
|
|
Paclitaxel
|
Binds to β-tubulin and promotes polymerization and stabilization, leading to arrest in G2/M and cell death
|
|
|
Vinblastine
|
Binds to tubulin and inhibits polymerization of mitotic spindles, arresting the cycle cycle in metaphase
Myelosuppresion is dose-limiting toxicity |
|
|
Vincristine
|
Binds to tubulin and inhibits polymerization of mitotic spindles, arresting the cycle cycle in metaphase
Peripheral neuropathy is dose-limiting toxicity |
|
|
Vinorelbine
|
Binds to tubulin and inhibits polymerization of mitotic spindles, arresting the cycle cycle in metaphase
Myelosuppression is dose-limiting toxicity |
|
|
Prednisone
|
Generally immunosuppressive
Used to induce remission in ALL and in Hodgkin's and non-Hodgkin's lymphoma |
|
|
Tamoxifen
|
Estrogen antagonist (Selective Estrogen Receptor Modulator - SERM)
Binds to ER but is transcriptionally inactive Estrogen competes, therefore, co-administration with leuprolide is usually indicated |
|
|
Toremifene
|
Estrogen antagonist (Selective Estrogen Receptor Modulator - SERM)
Binds to ER but is transcriptionally inactive Estrogen competes, therefore, co-administration with leuprolide is usually indicated |
|
|
Aminoglutethimide
|
Aromatase inhibitor
Inhibits both adrenal and extra-adrenal synthesis of pregnenolone Requires coadministration of cortisol Rarely used now |
|
|
Anastrazole
|
Non-steroidal aromatase inhibitor
Favorable because of: 1) More potent - inhibit aromatization by >96% 2) More selective than aminoglutethimide 3) Do not need to be supplemented with cortisol 4) Do not predispose to endometrial cancer 5) Devoid of androgenic side effects |
|
|
Letrozole
|
Non-steroidal aromatase inhibitor
Favorable because of: 1) More potent - inhibit aromatization by >96% 2) More selective than aminoglutethimide 3) Do not need to be supplemented with cortisol 4) Do not predispose to endometrial cancer 5) Devoid of androgenic side effects |
|
|
Exemestane
|
Steroidal, irreversible inhibitor of aromatase
|
|
|
Megestrol acetate
|
Progestin
|
|
|
Leuprolide
|
GnRH analog
Constant levels binding to pituitary GnRH receptors lead to receptor down-regulation and resultant decreased FSH and LH secretion |
|
|
Goserelin
|
GnRH analog
Constant levels binding to pituitary GnRH receptors lead to receptor down-regulation and resultant decreased FSH and LH secretion |
|
|
Flutamide
|
Non-steroidal anti-androgen
Compete for binding to AR; prevent translocation of receptor into cell nucleus |
|
|
Nilutamide
|
Non-steroidal anti-androgen
Compete for binding to AR; prevent translocation of receptor into cell nucleus |
|
|
Bicalutamide
|
Non-steroidal anti-androgen
Compete for binding to AR; prevent translocation of receptor into cell nucleus |
|
|
Bevacizumab
|
Monoclonal antibody directed against VEGF
|
|
|
Cetuximab
|
Monoclonal antibody directed against epidermal growth factor receptor
Colorectal cancer treatment |
|
|
Rituximab
|
Chimeric monoclonal antibody directed against CD20 found on B lymphocytes
R-CHOP |
|
|
Trastuzamab
|
Humanized monoclonal antibody directed against HER2 growth receptor
|
|
|
Cisplatin
|
Binds to guanine residues in DNA and induces cross-linking
Inhibits DNA and RNA synthesis Cells are most sensitive in G1 and S phases |
|
|
Carboplatin
|
Binds to guanine residues in DNA and induces cross-linking
Inhibits DNA and RNA synthesis Cells are most sensitive in G1 and S phases |
|
|
Oxaliplatin
|
Binds to guanine residues in DNA and induces cross-linking
Inhibits DNA and RNA synthesis Cells are most sensitive in G1 and S phases |
|
|
Irinotecan
|
Inhibition of topoisomerase I
S-phase specific Prevents repair of single-strand breaks |
|
|
Topotecan
|
Inhibition of topoisomerase II
Block cells in late S/G2 phase Renders DNA susceptible to irreversible double strand breaks |
|
|
Etoposide
|
Inhibition of topoisomerase II
Block cells in late S/G2 phase Renders DNA susceptible to irreversible double strand breaks |
|
|
Imatinib
|
Small molecule inhibitor
Inhibits constitutive tyrosine kinase BCR-ABL |
|
|
Gefinitib
|
Small molecule inhibitor
Targets epidermal growth factor receptor in NSCLC |
