Oncology Exam 3

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pharmschool
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144407
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Oncology Exam 3
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2012-03-28 15:58:01
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Oncology
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Dr. Schiff
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  1. A semisynthetic derivative of sirolimus (rapamycin)
    Temsirolimus Source
  2. Macrolide (macrocyclic lactone) skeleton
    Rapamycin derivative: 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate] rapamycin
    Colorless solid
    No ionizable functional groups
    Water insoluble
    Temsirolimus Chemistry
  3. An inhibitor of the enzyme mTOR (mammalian Target Of Rapamycin – a keyregulatory kinase)
    Binds to an intracellular protein (FKBP-12)
    This protein-drug complex inhibits the activity of mTOR that controls cell division
    Inhibition of mTOR activity resulted in a G1growth arrest in treated tumor cells
    Temsirolimus, Everolimus, and Ridaforolimus MOA
  4. Renal Cell Carcinoma
    Temsirolimus Common Application
  5. Hyperlipidemia and hyperglycemia
    Temsirolimus Special AEs
  6. Macrolide (macrocyclic lactone) skeleton
    A semi-synthetic derivative of Rapamycin (Sirolimus): 42-O-(2-hydroxy)ethyl rapamycin
    Colorless solid
    No ionizable functional groups
    Water insoluble
    Everolimus Chemistry
  7. Renal Cell Carcinoma
    Pancreatic Neuroendocrine Tumors (unresectable, locally advanced or metastatic disease)

    subependymal giant cell astrocytoma (SEGA) associated with tuberous sclerosisin patients who require therapy but are not candidates for surgical resection
    Everolimus Common Applications
  8. These two drugs do not have any special adverse effects detailed
    Everolimus & Ridaforolimus (Special AEs)
  9. Macrolide (macrocyclic lactone) skeleton
    A semi-synthetic derivative of Rapamycin (Sirolimus): 42-O-dimethylphosphinate rapamycin
    Colorless solid
    No ionizable functional groups
    Water insoluble
    Ridaforolimus Chemistry
  10. In Phase 3 clinical trials for the therapy ofmetastatic soft-tissue and bone sarcomas that are responsive to chemotherapy

    In Phase 2 clinical trials ongoing for advanced endometrial cancer, prostate cancer and non-small cell lung cancer
    Ridaforolimus Common Applications
  11. A semisynthetic derivative of thepolyketide macrolactone (macrolide)Epothilone B

    The first of the epothilones, a new class ofcytotoxic compounds
    Ixabepilone Source
  12. macrolactam derivative of the macrolactone Epothilone B

    No readily ionizable functional groups; Lactam N atom is neutral; Thiazole N atom electrons are delocalized in ring current and unavailable for salt formation

    Solubility is achieved via incorporation into solution in a mixture of Polyoxyethylated castor oil (52.8%) & Dehydrated alcohol (39.8%)
    Ixabepilone Chemistry
  13. MOA similar to the taxanes: Bind directly to the αβ-tubulin heterodimersubunit on microtubules. Once bound, the rate of heterodimeric tubulin dissociation decreases ->-> stabilizes the microtubules ->-> inhibits microtubule depolymerization

    Acts as an antimitotic - blocks the metaphase -> anaphase step in mitosis which leads to apoptosis

    Binds in a unique manner to β-tubulin and appears to be active against taxane-resistant tumor cell lines
    Ixabepilone MOA
  14. Combination with Capecitabine (Xeloda®) in the therapy of metastatic or locally advanced breast cancer patients after failure of an anthracycline and a taxane

    Monotherapy of metastatic or locally advanced breast cancer in patients after failure of an anthracycline, a taxane, and capecitabine
    Ixabepilone Common Applications
  15. Causes peripheral neuropathies, mainly sensory (20%)
    Ixabepilone Special AEs
  16. identified from Micromonospora echinospora ssp. calichensis
    Calicheamicin γ1I Source
  17. Culture of Micromonospora echinospora ssp. calichensis yielded a number of metabolites, the most important being this compound

    This compound was an extremely cytotoxic substance that became the lead compound in the emerging novel family of enediynes
    Calicheamicin γ1I Chemistry
  18. Binds to DNA in the minor groove resulting in: Double-strand breaks, Inhibition of DNA synthesis and function & Cell death
    Calicheamicin γ1I MOA
  19. This drug is covalently linked to a recombinant humanized monoclonal antibody (Gemtuzumab ozogamicin) directed against the 67 kDa cellsurface glycoprotein CD33
    Calicheamicin γ1I
  20. Relapsed CD33+ AML in patients in first relapse who are 60 years or older AND who are not considered for cytotoxic chemotherapy
    Calicheamicin γ1I Common Applications
  21. Infusion-related events: Hypotension and severe allergic reactions

    Premedicate with acetaminophen + diphenhydramine (and sometimes methylprednisolone)
    Calicheamicin γ1I Special AEs
  22. A chemically modified tetracycline: 4-dedimethylamino, 6-demethyl-6-deoxytetracycline
    Incyclinide Chemistry
  23. Clinical evaluations ongoing in patients with: Kaposi’s sarcoma, Rosacea, Acne & Acute respiratory distress syndrome
    Incyclinide Common Applications
  24. A plant commonly known as Mayapple or American Mandrake
    Podophyllum Source
  25. Lignan (dimeric phenylpropanoid)

    Biological activity is dependent upon the lactone ring existing in the trans-configuration
    Podophyllotoxin Chemistry
  26. INHIBIT MICROTUBULE FUNCTION; BINDS TO TUBULIN AND ARRESTS MITOSIS IN METAPHASE - ANTIMITOTIC
    Podophyllotoxin MOA
  27. Topical therapy of: Anogenital warts due to papillomavirus or condyloma acuminata warts
    Podophyllotoxin Common Applications
  28. Semi-synthetic lignan derivative of podophyllotoxin

    Phosphate ester is useful in high-dose chemotherapy regimens ---- Lessens volume of solution administered & Lessens time of administration
    Etoposide Source/Chemistry
  29. COMPLEXES WITH TOPOISOMERASE II TO PRODUCE DOUBLE-STRANDED DNA BREAKS; ANTIMITOTIC - G2
    Etoposide MOA
  30. Refractory testicular tumors (germ cell tumors)
    Small cell and non-small cell lung cancer
    Hodgkin’s and non-Hodgkin’s lymphomas
    Etoposide Common Applications
  31. Special AEs not documented ---- Increased risk of secondary malignancies, typically developing within 5-8 years
    Etoposide Special AEs
  32. Semi-synthetic lignan derivative of podophyllotoxin
    Teniposide Source/Chemistry
  33. MOA is the same as etoposide
    Teniposide MOA
  34. Refractory acute leukemia (ALL)
    Teniposide Common Application
  35. Semi-synthetic lignan derivative of podophyllotoxin that does not have any special adverse effects
    Teniposide
  36. Source is the fruits of Ammi visnaga Lam.(Apiaceae), a Mediterranean herb
    Methoxsalen
  37. A furanocoumarin
    Pale yellow color
    Low water solubility
    Methoxsalen Chemistry
  38. Noncancer-related applications include:
    – Severe idiopathic vitiligo (acquiredleukoderma): Vitiligo
    – Enhance tolerance to sunlight in blond persons with fair complexations who suffer “sun allergy” (severe sunburns)
    – Severe, recalcitrant, disabling psoriasis
    Methoxsalen Common Applications
  39. Cancer-related applications include:
    –Cutaneous T-cell Lymphoma (CTCL)(Mycosis fungoides)
    –Cervical dysplasia: Application of psoralen-containing gel in photodynamic therapy; Limits need for surgical treatment
    Methoxsalen Common Applications
  40. INTERCALATES WITH DNA FORMING ADDUCTS (WHEN LIGHT ACTIVATED, ACTS AS ALKYLATING AGENT)
    Methoxsalen MOA
  41. SEVERE BURNS AND BLISTERING IFTHERE IS POST-PUVA LIGHT EXPOSURETOO SOON AFTER THERAPY
    Methoxsalen Special AEs
  42. Isolated from the Seeds of the plant Euphorbia lathyris (Fam.Euphorbiaceae) or the Sap of the plant Euphorbia peplus (Fam.Euphorbiaceae)
    Ingenol Source
  43. Diterpene alcohol (4 x C5 units) that is alsoa tetraol
    Ingenol Chemistry
  44. Activates protein kinase isoforms, inducing apoptosis
    Ingenol MOA
  45. Applied as a gel in the short-course topical therapy of actinic keratosis and non-melanoma skin cancers – Phase 3

    Great benefit in treating actinic keratosis before this lesion progresses to invasive squamous carcinoma
    Ingenol Common Applications
  46. Physiological metabolite of retinol

    Prepared by oxidation of retinal
    Tretinoin Source
  47. Carotene derivative

    Lipophilic, with low water solubility
    Tretinoin Chemistry
  48. MOA is unknown; Not cytolytic

    Induces the maturation of acute promyelocytic leukemia cells in culture
    Tretinoin MOA
  49. Induction of remission (ONLY) in patients with acute promyelocytic leukemia (APL)(Classification M3 [genetic]) who:
    - Are refractory or have relapsed from anthracycline (doxorubicin family) therapy
    - Anthracycline-based therapy is contraindicated
    Tretinoin Common Application
  50. Effects commonly associated with highdoses of Vitamin A (nearly universal): Headache, fever, dryness of skin and mucous membranes

    Serious/grave (25-40%): Rapid leukocytosis & Cardiovascular/respiratory multiorgan failure (Retinoic acid-APL Syndrome)
    Tretinoin Special AEs
  51. A second generation retinoid

    Oral capsules useful for the therapy of severe psoriasis in adults
    Acitretin (Soriatane)
  52. Synthetic
    Lipophilic
    Weak acid
    A “rexinoid”
    Bexarotene Source/Chemistry
  53. PRECISE MOA - UNKNOWN

    SELECTIVELY BINDS AND ACTIVATES RETINOID X RECEPTOR SUBTYPES --- ACTIVATED RECEPTORS FUNCTION AS TRANSCRIPTION FACTORS --- REGULATE GENE EXPRESSION THAT CONTROLS CELL DIFFERENTIATION AND PROLIFERATION
    Bexarotene MOA
  54. Cutaneous manifestations of Cutaneous Tcell Lymphoma (CTCL) in patients refractory to one or more prior systemic therapies
    Bexarotene Common Application
  55. Hyperlipidemia
    Hypercholesterolemia
    Hypothyroidism
    Bexarotene Special AEs
  56. Light-sensitive polyporphyrin oligomer
    Purified product of a hematoporphyrin derivative
    Red-orange color
    Porfimer Sodium Source/Chemistry
  57. Use of a laser light elevates this compound to an excited state which causes radical initiation resulting in ischemic necrosis within a tumor
    Porfimer Sodium MOA
  58. PhotoDynamic Therapy (PDT) of: Esophageal cancer, Endobronchial non-small cell lung cancer, and Barrett’s Esophagus
    Porfimer Sodium Common Applications
  59. Many (CV, CNS, GI, Resp. systems)
    Porfimer Sodium Special AEs
  60. Fermentation product of Streptomyces antibioticus
    Pentostatin Source
  61. Colorless nucleoside
    Weak base
    Water soluble
    Pentostatin Chemistry
  62. TRANSITION STATE INHIBITOR OF ADENOSINE DEAMINASE which results in INHIBITION OF RIBONUCLEOTIDE REDUCTASE

    (antimetabolite)
    Pentostatin MOA
  63. Adult patient therapy
    Alpha-interferon-refractory hairy cell leukemia
    Pentostatin Common Application
  64. Neurologic: Nervousness and insomnia, Depression, Hallucinations
    Pentostatin Special AEs
  65. Fermentation product of Escherichia coli & Erwinia carotovoras
    Enzyme composed of 4 identical subunits
    FW = About 136,000 Da
    White
    Water-soluble
    Active at pH 5-9
    Asparaginase Source/Chemistry
  66. INHIBITS GROWTH OF MALIGNANT CELLS THAT ARE ASPARAGINE-DEPENDENT

    Results in INHIBITION OF TUMOR PROTEIN SYNTHESIS
    Asparaginase MOA
  67. Pediatric acute lymphocytic leukemia (ALL)
    Asparaginase Common Application
  68. Decreased Vitamin K-dependent clotting factors --> hemorrhage

    Hypersensitivity
    Asparaginase Special AEs
  69. Found in various ores, one of which is orpiment
    Obtained as a by-product of smelting copper
    White solid
    Long known in traditional Chinese medicine as Pi Shuang
    Two mineral forms exist: Arsenolite (Commonly occurring form–Octahedral or cubic form) & Claudetite (Thermodynamically stable–Monoclinic form)
    Arsenic Trioxide Source/Chemistry
  70. Precise MOA not fully elucidated
    Induces differentiation of APL cells by degrading PML/RAR-α protein
    Induces apoptosis
    Inhibits angiogenesis
    Arsenic Trioxide MOA
  71. Induction of remission and consolidation in acute promyelocytic leukemia (APL)
    - Relapsed from or refractory to retinoid and anthracycline chemotherapy
    - Whose APL is characterized by the expression of the t(15;17) translocation or PML/RAR-alpha gene expression
    Arsenic Trioxide Common Application
  72. Prolonged QT interval
    APL differentiation syndrome: rash, dyspnea, fluid retention, pleural or pericardial effusions
    Leukocytosis
    Arsenic Trioxide Special AEs

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