Podcast
Questions and Answers
Which monoclonal antibodies are used in the treatment of Ulcerative Colitis and Crohn's Disease?
Which monoclonal antibodies are used in the treatment of Ulcerative Colitis and Crohn's Disease?
What class of monoclonal antibody is Omalizumab used to treat?
What class of monoclonal antibody is Omalizumab used to treat?
Which monoclonal antibody is an anti-TNF-α that is used in conjunction with conventional therapies for Rheumatoid Arthritis?
Which monoclonal antibody is an anti-TNF-α that is used in conjunction with conventional therapies for Rheumatoid Arthritis?
What is one of the major drawbacks of monoclonal antibody therapies?
What is one of the major drawbacks of monoclonal antibody therapies?
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Which type of therapy is suggested to be the closest to personalized therapy?
Which type of therapy is suggested to be the closest to personalized therapy?
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What is the leading cause of death worldwide as per cancer statistics?
What is the leading cause of death worldwide as per cancer statistics?
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Which gene is primarily responsible for DNA repair and transcription regulation?
Which gene is primarily responsible for DNA repair and transcription regulation?
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What type of cancer is associated with the BCR-ABL gene?
What type of cancer is associated with the BCR-ABL gene?
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Which of the following cancer types is NOT listed as being related to the HER2 gene?
Which of the following cancer types is NOT listed as being related to the HER2 gene?
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How much is the expected increase in new cancer cases over the next two decades?
How much is the expected increase in new cancer cases over the next two decades?
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What role does the protein p53 play in cancer cell physiology?
What role does the protein p53 play in cancer cell physiology?
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Which chromosome translocation is associated with the Philadelphia chromosome?
Which chromosome translocation is associated with the Philadelphia chromosome?
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Which cancer has the highest incidence rate among women in the provided statistics?
Which cancer has the highest incidence rate among women in the provided statistics?
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What are the side effects commonly associated with thalidomide and its derivatives?
What are the side effects commonly associated with thalidomide and its derivatives?
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Which of the following is NOT a characteristic of monoclonal antibodies (MoAB)?
Which of the following is NOT a characteristic of monoclonal antibodies (MoAB)?
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Which indication is appropriate for the use of lenalidomide?
Which indication is appropriate for the use of lenalidomide?
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What is a major advantage of small molecules in cancer therapy?
What is a major advantage of small molecules in cancer therapy?
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How do monoclonal antibodies (MoAB) primarily exert their therapeutic effects?
How do monoclonal antibodies (MoAB) primarily exert their therapeutic effects?
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What should be monitored during the infusion of monoclonal antibodies due to possible reactions?
What should be monitored during the infusion of monoclonal antibodies due to possible reactions?
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Which chemical component is characteristic of the nomenclature for humanized monoclonal antibodies?
Which chemical component is characteristic of the nomenclature for humanized monoclonal antibodies?
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What is a significant drawback of monoclonal antibodies compared to small molecules?
What is a significant drawback of monoclonal antibodies compared to small molecules?
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What are the common side effects associated with BCR-ABL inhibitors?
What are the common side effects associated with BCR-ABL inhibitors?
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Which mTOR inhibitor is indicated for preventing graft rejection?
Which mTOR inhibitor is indicated for preventing graft rejection?
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What is a significant side effect of mTOR inhibitors?
What is a significant side effect of mTOR inhibitors?
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Which of the following conditions is treated with EGFR inhibitors?
Which of the following conditions is treated with EGFR inhibitors?
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Which multikinase inhibitor is considered to be from the older generation?
Which multikinase inhibitor is considered to be from the older generation?
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What is a common adverse effect of EGFR inhibitors?
What is a common adverse effect of EGFR inhibitors?
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What mechanism do multikinase inhibitors utilize to effect apoptosis?
What mechanism do multikinase inhibitors utilize to effect apoptosis?
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Which side effect is associated with mTOR inhibitors?
Which side effect is associated with mTOR inhibitors?
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What is the primary advantage of targeted therapy over classical chemotherapy?
What is the primary advantage of targeted therapy over classical chemotherapy?
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Which of the following classes of targeted therapy includes agents that operate on extracellular components?
Which of the following classes of targeted therapy includes agents that operate on extracellular components?
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What is the mechanism of action for BCR-ABL inhibitors like Imatinib?
What is the mechanism of action for BCR-ABL inhibitors like Imatinib?
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Which of the following statements about small molecules in targeted therapy is incorrect?
Which of the following statements about small molecules in targeted therapy is incorrect?
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What characterizes the newer generation of BCR-ABL inhibitors like Dasatinib and Nilotinib compared to Imatinib?
What characterizes the newer generation of BCR-ABL inhibitors like Dasatinib and Nilotinib compared to Imatinib?
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Which pathway do targeted drugs primarily aim to disrupt in cancer cells?
Which pathway do targeted drugs primarily aim to disrupt in cancer cells?
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In which conditions are BCR-ABL inhibitors indicated?
In which conditions are BCR-ABL inhibitors indicated?
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What is a distinguishing feature of classical chemotherapy compared to targeted therapy?
What is a distinguishing feature of classical chemotherapy compared to targeted therapy?
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What is a significant side effect associated with Rituximab?
What is a significant side effect associated with Rituximab?
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Which of the following MoABs acts as a conjugate and inhibits microtubules?
Which of the following MoABs acts as a conjugate and inhibits microtubules?
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What condition is primarily treated with Pembrolizumab?
What condition is primarily treated with Pembrolizumab?
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What therapy is indicative of an immune-induced disorder resulting in pneumonitis or hepatitis?
What therapy is indicative of an immune-induced disorder resulting in pneumonitis or hepatitis?
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Which MoAB is known for its role as an anti-VEGF antibody?
Which MoAB is known for its role as an anti-VEGF antibody?
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What is the primary action of Trastuzumab in cancer therapy?
What is the primary action of Trastuzumab in cancer therapy?
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What common side effect can occur with Brentuximab Vedotin treatment?
What common side effect can occur with Brentuximab Vedotin treatment?
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Which of the following statements is true regarding Alemtuzumab?
Which of the following statements is true regarding Alemtuzumab?
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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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Description
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.
