Targeted Therapy in Oncology
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Questions and Answers

Which monoclonal antibodies are used in the treatment of Ulcerative Colitis and Crohn's Disease?

  • Infliximab, Adalimumab, Certolizumab (correct)
  • Omalizumab, Etanercept
  • Rituximab, Trastuzumab
  • Cetuximab, Bevacizumab
  • What class of monoclonal antibody is Omalizumab used to treat?

  • Allergic asthma (correct)
  • Ulcerative Colitis
  • Rheumatoid arthritis
  • Crohn's Disease
  • Which monoclonal antibody is an anti-TNF-α that is used in conjunction with conventional therapies for Rheumatoid Arthritis?

  • Vedolizumab
  • Etanercept (correct)
  • Certolizumab
  • Adalimumab
  • What is one of the major drawbacks of monoclonal antibody therapies?

    <p>Serious side effects (C)</p> Signup and view all the answers

    Which type of therapy is suggested to be the closest to personalized therapy?

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

    What is the leading cause of death worldwide as per cancer statistics?

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

    Which gene is primarily responsible for DNA repair and transcription regulation?

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

    What type of cancer is associated with the BCR-ABL gene?

    <p>Chronic myeloid leukemia (C)</p> Signup and view all the answers

    Which of the following cancer types is NOT listed as being related to the HER2 gene?

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

    How much is the expected increase in new cancer cases over the next two decades?

    <p>70% (C)</p> Signup and view all the answers

    What role does the protein p53 play in cancer cell physiology?

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

    Which chromosome translocation is associated with the Philadelphia chromosome?

    <p>t(9;22) (A)</p> Signup and view all the answers

    Which cancer has the highest incidence rate among women in the provided statistics?

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

    What are the side effects commonly associated with thalidomide and its derivatives?

    <p>Orthostatic hypotension and teratogenic effects (C), Nausea and myelosuppression (D)</p> Signup and view all the answers

    Which of the following is NOT a characteristic of monoclonal antibodies (MoAB)?

    <p>Administration is mainly oral (C)</p> Signup and view all the answers

    Which indication is appropriate for the use of lenalidomide?

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

    What is a major advantage of small molecules in cancer therapy?

    <p>They can be administered at home (B)</p> Signup and view all the answers

    How do monoclonal antibodies (MoAB) primarily exert their therapeutic effects?

    <p>By inhibiting cell signaling pathways (D)</p> Signup and view all the answers

    What should be monitored during the infusion of monoclonal antibodies due to possible reactions?

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

    Which chemical component is characteristic of the nomenclature for humanized monoclonal antibodies?

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

    What is a significant drawback of monoclonal antibodies compared to small molecules?

    <p>They involve parenteral therapy with less comfort (A)</p> Signup and view all the answers

    What are the common side effects associated with BCR-ABL inhibitors?

    <p>Severe fluid retention (B)</p> Signup and view all the answers

    Which mTOR inhibitor is indicated for preventing graft rejection?

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

    What is a significant side effect of mTOR inhibitors?

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

    Which of the following conditions is treated with EGFR inhibitors?

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

    Which multikinase inhibitor is considered to be from the older generation?

    <p>Sunitinib (A), Sorafenib (B)</p> Signup and view all the answers

    What is a common adverse effect of EGFR inhibitors?

    <p>Prolongation of QT interval (C)</p> Signup and view all the answers

    What mechanism do multikinase inhibitors utilize to effect apoptosis?

    <p>Inhibition of various intracellular signaling pathways (D)</p> Signup and view all the answers

    Which side effect is associated with mTOR inhibitors?

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

    What is the primary advantage of targeted therapy over classical chemotherapy?

    <p>Targeted therapy can specifically stop disease progression. (D)</p> Signup and view all the answers

    Which of the following classes of targeted therapy includes agents that operate on extracellular components?

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

    What is the mechanism of action for BCR-ABL inhibitors like Imatinib?

    <p>Inhibition of tyrosine kinase activity (A)</p> Signup and view all the answers

    Which of the following statements about small molecules in targeted therapy is incorrect?

    <p>They primarily target extracellular ligands. (D)</p> Signup and view all the answers

    What characterizes the newer generation of BCR-ABL inhibitors like Dasatinib and Nilotinib compared to Imatinib?

    <p>They are targeted at Imatinib-resistant cells. (C)</p> Signup and view all the answers

    Which pathway do targeted drugs primarily aim to disrupt in cancer cells?

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

    In which conditions are BCR-ABL inhibitors indicated?

    <p>Ph chromosome positive CML and gastrointestinal stromal tumors (C)</p> Signup and view all the answers

    What is a distinguishing feature of classical chemotherapy compared to targeted therapy?

    <p>Classical chemotherapy lacks specificity and may affect normal cells. (C)</p> Signup and view all the answers

    What is a significant side effect associated with Rituximab?

    <p>Infusion and hypersensitivity reactions (A)</p> Signup and view all the answers

    Which of the following MoABs acts as a conjugate and inhibits microtubules?

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

    What condition is primarily treated with Pembrolizumab?

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

    What therapy is indicative of an immune-induced disorder resulting in pneumonitis or hepatitis?

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

    Which MoAB is known for its role as an anti-VEGF antibody?

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

    What is the primary action of Trastuzumab in cancer therapy?

    <p>Interference with HER2 receptors (B)</p> Signup and view all the answers

    What common side effect can occur with Brentuximab Vedotin treatment?

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

    Which of the following statements is true regarding Alemtuzumab?

    <p>Can cause opportunistic infections (B)</p> Signup and view all the answers

    Flashcards

    Targeted Therapy in Oncology

    Treatment strategies focusing on specific molecular targets within cancer cells, aiming to disrupt their abnormal growth and spread without harming healthy cells.

    Oncogenes

    Genes that, when mutated, can cause cells to grow and divide uncontrollably, contributing to cancer development.

    EGFR

    Epidermal Growth Factor Receptor, a protein involved in cell signaling and growth .Mutations in EGFR can lead to overactivation, promoting cancer growth.

    Tumor Suppressor Genes

    Genes that normally regulate cell growth and prevent uncontrolled division. If mutated, their protective functions are lost, promoting cancer development.

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    Philadelphia Chromosome

    A specific chromosomal abnormality resulting from a translocation between chromosomes 9 and 22, which creates a fusion protein (BCR-ABL) driving uncontrolled cell growth.

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    BCR-ABL

    A fusion protein formed by translocation of chromosomes 9 and 22, resulting in tyrosine kinase activity, often linked to chronic myelogenous leukemia (CML).

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    Cancer Cell Physiology

    The study of the biological processes within a cancer cell that differs from a healthy cell, including genetic and cellular changes leading to uncontrolled growth and metastasis.

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    World Health Organization (WHO)

    International organization that monitors global health and provides information.

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    Targeted Therapy

    Treatment that targets specific pathways, processes, or physiology uniquely disrupted in cancer cells.

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    Small Molecules

    Drugs with molecular weight around 500 Da that enter cells and block signaling pathways.

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    Monoclonal Antibodies (mAbs)

    Drugs with a molecular weight around 150,000 Da targeting extracellular components (ligands and receptors on the cell surface).

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    Protein Kinase Inhibitors (PKIs)

    Small molecules targeting intracellular receptor domains to block signaling pathways.

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    BCR-ABL Inhibitors

    A class of PKIs targeting the BCR-ABL protein, common in chronic myeloid leukemia (CML).

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    Chronic Myeloid Leukemia (CML)

    A type of cancer where uncontrolled production of white blood cells occurs.

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    Imatinib

    An important first-generation small molecule drug used to treat CML.

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    Targeted vs. Classical Chemotherapy

    Targeted therapy specifically targets the cancer cell while classical chemotherapy affects normal and cancer cells. This difference often leads to reduced side effects.

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    Side Effects of BCR-ABL Inhibitors

    Common side effects include severe fluid retention (leading to swelling), low blood cell counts, liver problems, muscle cramps, headaches, and skin issues.

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    mTOR Inhibitors

    Drugs that block mTOR, a protein involved in cell growth and division. They work by preventing the 'on' switch of cancer cells.

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    Uses of mTOR Inhibitors

    Used in treating various cancers, including renal cell carcinoma, lymphoma, breast cancer, and neuroendocrine tumors. They also help prevent organ transplant rejection.

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    EGFR/HER Inhibitors

    Drugs targeting EGFR and HER receptors, key proteins involved in cancer cell growth and proliferation. They block the signal that tells cancer cells to grow.

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    Examples of EGFR/HER Inhibitors

    Common examples include erlotinib, gefitinib, afatinib, and lapatinib. They are often used for lung cancer, breast cancer, and pancreatic cancer.

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    Multikinase Inhibitors

    Drugs that target multiple signaling pathways within cancer cells, preventing their growth and spread. They work like multi-tasking agents.

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    Uses of Multikinase Inhibitors

    Used in treating several cancer types, including gastrointestinal stromal tumors (GIST), renal cell carcinoma, neuroendocrine tumors, and liver cancer.

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    Small Molecules in Cancer

    Drugs with low molecular weight that target specific pathways inside cancer cells, often blocking signaling pathways.

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    Imatinib and CML

    Imatinib is a small molecule drug that specifically targets the BCR-ABL protein, a key driver of chronic myeloid leukemia (CML).

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    MoAB Groups: Naked vs. Conjugated

    MoABs can be either ‘naked’ (unmodified) or attached to toxins, chemotherapy drugs, or radioactive particles for enhanced targeting and cell killing.

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    MoAB Mechanism: How They Work

    MoABs can disable cancer cells through various mechanisms: complement-dependent cytotoxicity, antibody-dependent cytotoxicity, and inhibition of cell signaling.

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    MoAB Side Effects

    Side effects depend on the extent of foreign components in the MoAB, with humanized MoABs generally having fewer side effects.

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    MoAB Therapy: Challenges

    MoAB therapy may require parenteral administration (injections or infusions), making it less convenient than oral medications.

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    Targeted vs. Classical Chemotherapy: Key Difference

    Unlike classical chemotherapy, which targets both healthy and cancerous cells, targeted therapy specifically attacks cancer cells, often minimizing side effects.

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    What are Monoclonal Antibodies?

    Monoclonal Antibodies (MoAbs) are a type of targeted therapy that focus on specific molecular targets within cancer cells. They are large proteins with greater specificity and affinity for their target compared to traditional chemotherapy.

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    What are the key differences between Classical Chemotherapy and Targeted Therapy?

    Classical chemotherapy targets rapidly dividing cells, which includes both cancer cells and healthy cells, leading to broader side effects. Targeted therapies focus on unique molecular targets in cancer cells, minimizing damage to healthy cells.

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    What are the basic groups of MoAbs?

    MoAbs can be grouped based on their targets. Examples include:

    • TNF-α inhibitors, for inflammatory diseases like ulcerative colitis and rheumatoid arthritis
    • Anti-adhesion molecules, blocking T-lymphocyte adhesion
    • Anti-IgE antibodies, used in allergic asthma
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    What are the benefits of MoAbs over traditional chemotherapy?

    MoAbs offer several advantages:

    • Greater specificity for cancer cells, leading to fewer side effects.
    • They can be used for a broader range of conditions, including inflammatory diseases.
    • MoAbs represent a more personalized approach to therapy.
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    Why are costs a major concern with MoAbs?

    MoAbs are complex to develop, manufacture, and administer, resulting in high costs. Their effectiveness is still being researched, leading to cost-benefit questions for patients and healthcare systems.

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    What are MoAbs?

    Monoclonal antibodies (MoAbs) are specifically designed antibodies that target and bind to specific molecules on the surface of cancer cells.

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    CD20 target for MoAbs

    CD20 is a protein found on the surface of B lymphocytes, making it a target for MoAbs like Rituximab. CD20 is a cluster of differentiation (CD) protein.

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    Rituximab: Mechanism of action

    Rituximab binds to CD20 on B-cells, triggering apoptosis (programmed cell death).

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    Brentuximab Vedotin: Target & Action

    Brentuximab Vedotin targets CD30, a protein found on Hodgkin's lymphoma cells. It enters the cell and disrupts microtubule function, stopping cell division.

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    Alemtuzumab: Target & Action

    Alemtuzumab targets CD52, a protein found on multiple cell types, including T cells, B cells, and NK cells. Binds to CD52 on the cells and triggers apoptosis.

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    Cetuximab: Target & Action

    Cetuximab targets the EGFR receptor on cancer cells, blocking cell growth, proliferation, and metastasis.

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    Bevacizumab: Target & Action

    Bevacizumab targets the VEGF protein, which promotes blood vessel growth (angiogenesis) in tumors.

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    Ipilimumab: Target & Action

    This antibody targets CTLA-4, a protein that acts as a 'brake' on the immune system's T-cells. It takes the brake off, allowing T-cells to attack cancer cells effectively.

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    Study Notes

    Targeted Therapy in Oncology

    • Tumours are the second leading cause of death globally, with one in every six deaths caused by a malignancy.
    • The number of new cancer cases is projected to increase by 70% in the next two decades.
    • Malignant diseases have a significant and growing impact on the global economy.

    Cancer Statistics (World)

    • Data from 2018 shows the frequency and localization of tumours in the USA, Great Britain, and Serbia.
      • USA: Prostate and lung cancer were most frequent cancers in men; breast and lung cancer were most frequent in women
      • Great Britain: Prostate and lung cancer were most frequent in men; breast and lung cancer were most frequent in women
      • Serbia: Lung cancer was most frequent for both men and women.

    Cancer Statistics (US)

    • Estimated cancer deaths in the US for 2020 (males & females, by type) are listed.
    • Lung, bronchus, prostate, colon, rectum, and pancreas are among the most common cancer types, both for males and females.

    Essential Changes in Cancer Cell Physiology

    • Key changes in cancer cell function, including self-sufficiency in growth signals, evasion of apoptosis, insensitivity to anti-growth signals, sustained angiogenesis, tissue invasion/metastasis, and limitless replicative potential.
    • Diagram (or image) illustrating these changes.
    • The target for new cancer drugs is highlighted.

    Examples of Oncogenes and Tumor Suppressor Genes

    • Table listing examples of oncogenes (EGFR, HER2, BCR-ABL, p53, BRCA) and the cancers types they are associated with.

    Example of Changes in the Cancer Cell

    • Philadelphia chromosome (t(9;22) translocation).
    • Diagram showing the translocation.
    • Describes the formation of a fusion protein due to the translocation.

    What is Targeted Therapy?

    • Drugs target specific pathways, processes, and physiology uniquely disrupted in cancer cells.
    • Focuses on receptors, genes, and angiogenesis.
    • A "smart" bomb versus a "cluster" bomb metaphor for targeted therapy.

    Targeted vs. Classical Chemotherapy

    • Targeted therapy is designed to precisely target the disease, while classical chemotherapy affects a broader range of cells.
    • Example of Chronic Myeloid Leukemia (CML) treatment highlights the contrast between targeted and classical therapy.
    • Targeted therapy has the potential to stop the progression of CML, in contrast to classical chemotherapy.

    Targeted Therapy - Classes

    • Small molecules (molecular mass ~500 Da) enter cells and block downlink signaling.
    • Monoclonal antibodies (mAbs) (molecular weight ~150,000 Da) target extracellular components and cell surface receptors.

    Targeted Therapy - Small Molecules (Protein Kinase Inhibitors)

    • Types of small molecule inhibitors: BCR-ABL inhibitors, mTOR inhibitors, EGFR inhibitors, multikinase inhibitors, BRAF inhibitors, ALK inhibitors, proteasome inhibitors, and other small molecule inhibitors.

    Small Molecules - BCR-ABL Inhibitors

    • Older generation: Imatinib.
    • Newer generation: Dasatinib, Nilotinib, Bosutinib, Ponatinib.
    • Mechanism of action: Targeting the BCR-ABL fusion protein.
    • Indications: CML, ALL, sarcomas, GISTs.

    Small Molecules - mTOR Inhibitors

    • Types: Temsirolimus, everolimus.
    • Mechanism of action: Selective inhibition of mTOR, which controls cell division and growth.
    • Indications: Renal cell carcinoma, lymphoma, HER2-positive breast cancers, and others.

    Small Molecules - EGFR, HER Inhibitors

    • Types: Erlotinib, gefitinib, afatinib, and lapatinib.
    • Mechanism of action: Tyrosine kinase inhibition for EGFR and HER1/HER2.
    • Indications: Non-small-cell lung cancer, pancreatic cancer, and breast cancer.

    Small Molecules - Multikinase Inhibitors

    • Types: Sunitinib, sorafenib, pazopanib, axitinib
    • Mechanism of action: Inhibition of various intracellular signaling pathways
    • Indication: GISTs, metastatic renal cell carcinoma, neuroendocrine tumors, hepatocellular carcinoma

    Small Molecules - B-RAF Inhibitors

    • Types: Vemurafenib, dabrafenib.
    • Mechanism of action: Inhibition of mutated B-RAF kinase.
    • Indication: Unresectable melanoma with a BRAF mutation.

    Small Molecules - ALK Inhibitors

    • Types: Crizotinib, ceritinib, alectinib, brigatinib.
    • Mechanism of action: Inhibition of ALK autophosphorylation.
    • Indication: Non-small cell lung cancer with ALK mutation.

    Small Molecules - Proteasome Inhibitors

    • Types: Bortezomib, carfilzomib.
    • Mechanism of action: Inhibition of the proteasome, leading to cancer cell death.
    • Indication: Multiple myeloma and some types of lymphoma.

    Small Molecules - Other

    • Thalidomide, lenalidomide, pomalidomide.
    • Mechanism of action: Angiogenesis inhibition, direct cytotoxicity, and TNF-alpha inhibition.
    • Indications: Multiple myeloma, myelodysplastic syndromes, and others.

    Advantages of Small Molecules

    • Revolutionary change in treatment for some tumors.
    • Convenient administration (mostly tablets and capsules).
    • Prolong progression-free survival.
    • Fewer serious side effects compared to classical chemotherapy, but considerable cost.

    Targeted Therapy - Monoclonal Antibodies (mAbs)

    • Types: Naked, conjugated with toxin, chemotherapy drug, or radioactive particle.
    • Mechanism of action: Complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC) and inhibition of cell signaling
    • General side effects depend on the component.
    • Types of mAbs targeting specific growth factors: Cetuximab(EGFR), Trastuzumab/Pertuzumab(HER2), Bevacizumab (anti-VEGF).

    Targeted Therapy - mAbs (Continued)

    • Types specifically targeting different parts of cellular immune system: Ipilimumab (CTLA4), Pembrolizumab (PD-1), and other.
    • Indications: Diverse, including non-oncological conditions such as inflammatory bowel disease, rheumatic diseases, and allergic asthmas.

    Advantages of mAbs

    • High investments in Research and Development, promising approach to personalized therapy
    • Safe for patients but also expensive
    • Still have serious side effects

    Questions

    • Key differences between classical chemotherapy and targeted small molecules.
    • Key differences between small molecules and mAbs.
    • The principal groupings of small molecules and monoclonal antibodies.
    • Non-oncological applications of mAbs.

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    This quiz covers key statistics and information regarding targeted therapy in oncology. Explore cancer prevalence in different regions, focusing on the most common types of cancer, and learn about the increasing impact of malignancies on global health. Test your knowledge on cancer statistics and the future projections of cancer cases.

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