DNA Damaging Agents and Antimetabolites
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Questions and Answers

What is the primary mechanism of action of Sunitinib?

  • Blocks estrogen receptor
  • Inhibits PD-1
  • Prevents immune cell activation
  • Inhibits VEGFR (correct)
  • What types of cancer is Tamoxifen primarily used to treat?

  • Renal cell carcinoma
  • GI stromal tumors
  • Pancreatic cancer
  • Breast cancer (correct)
  • How do PD-1 inhibitors function in cancer therapy?

  • They promote tumor growth
  • They stimulate estrogen receptors
  • They activate immune cells
  • They inhibit the binding of PD-1 and PD-L1 (correct)
  • Which of the following statements regarding Hormonal Therapies is true?

    <p>Tamoxifen blocks estrogen receptor to inhibit cancer growth (C)</p> Signup and view all the answers

    Which of the following drugs is NOT classified as a PD-1 inhibitor?

    <p>Atezolizumab (B)</p> Signup and view all the answers

    Which drug is known to block DNA repair in cancer cells?

    <p>Olaparib (A)</p> Signup and view all the answers

    What is the mechanism of action of Imatinib?

    <p>Inhibits BCR and ABL (D)</p> Signup and view all the answers

    Which of the following drugs is specifically used for treating breast cancer?

    <p>Trastuzumab (C)</p> Signup and view all the answers

    For which condition is Gefitinib primarily indicated?

    <p>Non-small cell lung cancer (A)</p> Signup and view all the answers

    Which of the following drug classes has a mechanism involving the insertion between base pairs and DNA cleavage?

    <p>Antitumor Antibiotics (B)</p> Signup and view all the answers

    What is the primary mechanism of action of PARP inhibitors?

    <p>Blocking DNA repair mechanisms in cancer cells (A)</p> Signup and view all the answers

    Which drug is administered as an IV infusion for its therapeutic purpose?

    <p>Trastuzumab (B)</p> Signup and view all the answers

    What is the recommended dose of Imatinib for Chronic Myelogenous Leukemia (CML)?

    <p>400mg OD (A)</p> Signup and view all the answers

    What is the primary mechanism of action for the drug 5-fluorouracil?

    <p>It inhibits the conversion of cytidylic acid to 2-deoxycytidylic acid. (D)</p> Signup and view all the answers

    Which class of drugs does Paclitaxel belong to?

    <p>Taxanes (A)</p> Signup and view all the answers

    What effect do Vinca Alkaloids have on microtubules?

    <p>They prevent microtube polymerization, inhibiting cell division. (B)</p> Signup and view all the answers

    Which of the following drugs effectively acts during the S-phase of the cell cycle?

    <p>Cytarabine (C)</p> Signup and view all the answers

    What is a common use for Docetaxel?

    <p>Treatment of breast and lung cancers (B)</p> Signup and view all the answers

    Which type of drug is gemcitabine classified as?

    <p>Antimetabolite (D)</p> Signup and view all the answers

    Which mechanism describes how antimitotics, such as Paclitaxel, work?

    <p>By binding to free tubulin to prevent microtubule disassembly. (D)</p> Signup and view all the answers

    What is the main feature of purine or pyrimidine antimetabolites?

    <p>They inhibit normal cellular metabolite biosynthesis. (D)</p> Signup and view all the answers

    What is the primary mechanism through which Pertuzumab acts to inhibit cancer cell growth?

    <p>It prevents the activation of HER2. (B)</p> Signup and view all the answers

    Which type of cancer is specifically targeted by T-DM1 therapeutically?

    <p>HER2 breast cancer (B)</p> Signup and view all the answers

    What is the role of Bortezomib in cancer treatment?

    <p>It inhibits the 26S proteasome to trigger stress responses in cells. (B)</p> Signup and view all the answers

    Which therapeutic agent inhibits vascular endothelial growth factor (VEGF) as part of its mechanism?

    <p>Bevacizumab (A)</p> Signup and view all the answers

    In which scenario is T-DM1 recommended for use?

    <p>For HER2 breast cancer after surgery (B)</p> Signup and view all the answers

    What consequence does the inhibition of angiogenesis have on tumors?

    <p>It prevents tumors from receiving necessary blood supply. (D)</p> Signup and view all the answers

    What type of cancer is primarily treated with Angiogenesis inhibitors like Bevacizumab?

    <p>Colon and lung cancer (C)</p> Signup and view all the answers

    Which statement regarding HER2 overexpression is correct?

    <p>It leads to abnormal cell growth and proliferation. (A)</p> Signup and view all the answers

    Which drug class from the table primarily targets the N7 position of guanine in DNA?

    <p>Alkylating Agents (A), Platinum Drugs (D)</p> Signup and view all the answers

    Which of the following drugs is a nitrogen mustard?

    <p>Melphalan (C)</p> Signup and view all the answers

    What is the primary mechanism of action of nitrosoureas?

    <p>Alkylating DNA at the O6 of guanine (B)</p> Signup and view all the answers

    Which of the following drugs is NOT an alkylating agent?

    <p>Procarbazine (D)</p> Signup and view all the answers

    Which of the following is a characteristic of platinum drugs?

    <p>They crosslink DNA by attaching to the N7 of guanine. (D)</p> Signup and view all the answers

    What is the structural feature that distinguishes nitrosoureas from other alkylating agents?

    <p>The presence of a nitrosourea group (B)</p> Signup and view all the answers

    Which of the following drugs is most likely to be used to treat multiple myeloma?

    <p>Melphalan (B)</p> Signup and view all the answers

    Based on the table, what is a common feature among all drugs listed?

    <p>They all act by directly damaging DNA. (C)</p> Signup and view all the answers

    Flashcards

    Antimetabolites

    Drugs that inhibit the biosynthesis of cellular metabolites, affecting DNA/RNA synthesis.

    5-fluorouracil

    An antimetabolite used to inhibit the conversion of cytidylic acid, affecting DNA synthesis.

    Paclitaxel

    A taxane that stabilizes microtubules, preventing their disassembly during cell division.

    Docetaxel

    A taxane that binds free tubulin to inhibit microtubule disassembly; used for various cancers.

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    Microtubules

    Cytoskeletal structures that play a crucial role in chromosome segregation during cell division.

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    Vinca Alkaloids

    A class of drugs such as Vinblastine that prevent microtubule polymerization.

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    S-phase

    The phase of the cell cycle where DNA is synthesized and chromosomes are duplicated.

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    Cytidylic acid

    A nucleotide precursor involved in RNA and DNA synthesis, targeted by 5-fluorouracil.

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    Antitumor Antibiotics

    Class of cancer treatment drugs including daunorubicin and doxorubicin that interfere with DNA.

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    PARP Inhibitors

    Block DNA repair enzymes in cancer cells to promote cell death, used in various cancers.

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    Vinorelbine

    A chemotherapy drug preventing proper spindle formation, affecting mitosis in cancer cells.

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    Tyrosine Kinase Inhibitors

    Drug class like imatinib that stops signals necessary for cancer cell growth and survival.

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    Imatinib

    A tyrosine kinase inhibitor indicated for chronic myelogenous leukemia (CML) and ALL.

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    Gefitinib

    Inhibitor of epidermal growth factor receptor (EGFR) for non-small cell lung cancer treatment.

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    Trastuzumab

    Monoclonal antibody used in breast cancer treatment by inhibiting HER2 receptor.

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    Daunorubicin

    An anthracycline antibiotic that inserts itself into DNA to disrupt cancer cell function.

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    Alkylating Agents

    Chemicals that add alkyl groups to DNA, damaging it and preventing replication.

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    DNA Crosslinking

    A process where two strands of DNA are linked together, preventing separation during replication.

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    Nitrogen Mustards

    A class of alkylating agents, including drugs like Cyclophosphamide and Melphalan.

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    Carmustine

    A nitrosourea that alkylates the O6 of guanine, causing DNA damage and crosslinks.

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    Cisplatin

    A platinum drug that crosslinks DNA by attaching to N7 of guanine.

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    Busulfan

    An alkylating agent that removes a mesylate group to alkylate guanine, causing crosslinks.

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    Ifosfamide

    An alkylating agent with a similar MOA to Cyclophosphamide, affecting DNA replication.

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    Procarbazine

    Forms ions and cations to alkylate the O6 position on guanine, causing DNA damage.

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    Sunitinib

    A tyrosine kinase inhibitor that targets VEGFR to inhibit tumor growth by starving it of nutrients.

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    PD-1 Inhibitors

    Class of drugs that inhibit PD-1, allowing T-cells to kill tumor cells by preventing tumor evasion.

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    Pembrolizumab

    A PD-1 inhibitor that enhances T-cell activity against tumors by blocking PD-1 receptor.

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    Tamoxifen

    Blocks estrogen receptors to prevent hormone-driven cancer growth, primarily used in breast cancer.

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    PD-L1 Inhibitors

    Drugs that inhibit PD-L1, preventing tumor cells from evading the immune response mediated by PD-1.

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    HER2 overexpression

    A condition where the HER2 protein is produced in excess, leading to abnormal cell growth and proliferation in cancers.

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    Pertuzumab

    A drug that binds to HER2 subdomain II to inhibit dimerization, preventing cancer cell signaling.

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    Dimerization

    The process where two receptor proteins join together, which can activate cancer signaling pathways.

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    T-DM1

    A cytotoxic agent that targets HER2 breast cancer cells, triggering apoptosis after being cleaved.

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    Apoptosis Inducing Agents

    Drugs that trigger programmed cell death in cancer cells.

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    Bortezomib

    A drug that inhibits the 26S proteasome, leading to protein build-up and stress responses to kill cancer cells.

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    Angiogenesis inhibitors

    Drugs that block the formation of new blood vessels, starving tumors of nutrients.

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    Bevacizumab

    A monoclonal antibody that inhibits VEGF to prevent blood vessel formation in tumors.

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    Study Notes

    DNA Damaging Agents

    • Alkylating Agents: Alkylate DNA, creating cyclic structures and attaching to guanine's N7. Can also cause crosslinking of DNA.
      • Nitrogen Mustards: Melphalan, cyclophosphamide, ifosfamide, chlorambucil, estramustine, carmustine, lomustine, nimustine, streptozocin.
      • Nitrosoureas: Carmustine, Lomustine, Nimustine
      • Platinum Drugs: Carboplatin, cisplatin, oxaliplatin. Alkylate the O6 of guanine, causing crosslinking and DNA damage. Crosslinks DNA by attaching to guanine's N7.
      • Miscellaneous: Busulfan, procarbazine. Busulfan removes a mesylate group to form R-CH2, alkylates N7 of guanine, and causes DNA crosslinking. Procarbazine forms an ion, cation, and alkylates at the O6, potentially inhibiting protein, RNA, and DNA synthesis.

    Antimetabolites

    • Pyrimidine or Purine Antimetabolites: Interfere with normal cellular metabolites by inhibiting the conversion of cytidylic acid to 2-deoxycytidylic acid, which is effective during S-phase.
      • 5-fluorouracil, capecitabine, gemcitabine, cytarabine, azacitidine

    Antimitotics

    • Taxanes: Bind to free tubulin to form stable microtubules, stopping microtubule disassembly, essential for cell division.
      • Paclitaxel, Docetaxel

    Targeted Therapy Agents

    • Tyrosine Kinase Inhibitors: Inhibit BCR, ABL, used for cancer cell proliferation, movement, and apoptosis avoidance. Inhibit EPFR for DNA synthesis, proliferation, migration, and survival.
      • Imatinib, Gefitinib
    • Monoclonal Antibodies: Inhibits HER2 to prevent abnormal cell growth, survival, and proliferation, impacting its dimerization.
      • Trastuzumab, Pertuzumab

    Antitumor Antibiotics

    • Vinca Alkaloids: Bind to tubulin preventing microtubule formation thus preventing cell division.
      • Vinblastine, vincristine, vindesine, vinorelbine
    • Anthracyclines: Insert themselves between base pairs of DNA.
      • Daunorubicin, doxorubicin, epirubicin, idarubicin, mitoxantrone

    DNA Repair Enzyme Inhibitors

    • Inhibit DNA repair in cancer cells to cause cancer cell death.
      • Olaparib, rucaparib, niraparib, iniparib, talazoparib

    Apoptosis-Inducing Agents

    • Induce apoptosis (programmed cell death).
      • Bortezomib

    Angiogenesis Inhibitors

    • Inhibit angiogenesis (formation of blood vessels), depriving tumors of essential nutrients.
      • Bevacizumab

    Multiple Targeted Tyrosine Kinase Inhibitors

    • Inhibit various tyrosine kinases, impacting numerous pathways.
      • Sunitinib

    Immunotherapies

    • PD-1 Inhibitors: Inhibit PD-1, reducing the ability of the tumor cell to evade killing.
      • Pembrolizumab, Nivolumab, Cemiplimab, Atezolizumab
    • PD-L1 Inhibitors: Inhibit PD-L1 and the ability of the tumor cells to avoid killing.
      • Avelumab, Durvalumab

    Hormonal Therapies

    • Tamoxifen: Blocks estrogen receptor (ER), preventing hormone binding and cancer growth.

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    Cancer Drugs PDF

    Description

    This quiz covers key concepts related to DNA damaging agents, including alkylating agents like nitrogen mustards and platinum drugs, as well as antimetabolites such as pyrimidine and purine analogs. Test your knowledge on how these compounds interact with DNA and disrupt cellular processes. Explore the mechanisms of action and clinical implications of these important chemotherapy agents.

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