Anticancer Drugs Practice Questions

Q: Match the following drugs with the targets of their actions: Drugs: A. Trastuzumab B. Infliximab C. Sirolimus D. Imatinib Targets: 1. BCR-ABL tyrosine kinase 2. mTOR 3. TNF alpha 4. HER2/neu

A-4, B-3, C-2, D-1. ***Correct Answer: A-4, B-3, C-2, D-1*** - **Trastuzumab** (Herceptin) is a **monoclonal antibody** that targets the **HER2/neu receptor (4)** [1], [2], commonly overexpressed in certain breast cancers and gastric cancers. - **Infliximab** is another **monoclonal antibody** that specifically targets and neutralizes **TNF-alpha (3)**, an inflammatory cytokine, making it useful in treating autoimmune diseases like rheumatoid arthritis and Crohn's disease. - **Sirolimus** is an **immunosuppressant** drug that inhibits the mammalian target of rapamycin (**mTOR (2)**), a protein kinase involved in cell growth and proliferation, used in transplant medicine and as an anticancer agent. - **Imatinib** is a **tyrosine kinase inhibitor** that primarily targets the **BCR-ABL fusion protein (1)** [1], [2], which is characteristic of chronic myeloid leukemia. *Incorrect: A-2, B-3, C-1, D-4* - This option incorrectly matches Trastuzumab with mTOR and Sirolimus with BCR-ABL, which are not their primary targets. - Trastuzumab targets HER2/neu [1], [2], and Sirolimus targets mTOR. *Incorrect: A-3, B-4, C-2, D-1* - This option incorrectly matches Trastuzumab with TNF-alpha and Infliximab with HER2/neu. - Infliximab targets TNF-alpha, and Trastuzumab targets HER2/neu [1], [2]. *Incorrect: A-4, B-3, C-1, D-2* - This option incorrectly matches Sirolimus with BCR-ABL and Imatinib with mTOR. - Sirolimus inhibits mTOR, and Imatinib inhibits BCR-ABL [1], [2].

Q: A lady who had undergone mastectomy for breast cancer is being treated with tamoxifen. How long should it be stopped before she can conceive?

3 months. ***3 months*** - Tamoxifen has a long half-life, and it can remain in the body for up to several weeks after the last dose. A washout period of **at least 3 months** is recommended to minimize exposure of a developing fetus to the drug. - Exposure to tamoxifen during pregnancy is associated with potential risks such as **birth defects** and impaired fetal development due to its anti-estrogenic effects disrupting hormonal balance. *No need to stop* - This is incorrect because tamoxifen is **teratogenic**, meaning it can cause birth defects if taken during pregnancy. - Continuing tamoxifen during pregnancy would expose the fetus to serious risks, necessitating a planned discontinuation before conception. *Can be stopped and conceived soon after stopping* - This is incorrect because tamoxifen has a relatively **long half-life**, meaning it takes time for the drug to be completely eliminated from the body. - A washout period is necessary to ensure the drug levels are low enough to prevent fetal exposure and potential harm. *1 month* - A 1-month washout period is generally considered **insufficient** given tamoxifen's pharmacokinetic profile. - This shorter period does not adequately account for the drug's long half-life, increasing the risk of fetal exposure and potential complications.

Q: Which among the following drugs is the new FDA approved immune checkpoint inhibitor for endometrial carcinoma?

Pembrolizumab. **Pembrolizumab** * **Pembrolizumab** (Keytruda), a **PD-1 inhibitor**, received accelerated FDA approval for patients with **advanced endometrial carcinoma** that is mismatch repair deficient (dMMR) or microsatellite instability-high (MSI-H), and has progressed following prior systemic therapy or is not a candidate for curative surgery or radiation. * This approval was based on data from the KEYNOTE-158 study, demonstrating **durable responses** in these specific subsets of endometrial cancer, highlighting its role in precision oncology. *Ipilimumab* * **Ipilimumab** (Yervoy) is a **CTLA-4 inhibitor** primarily approved for the treatment of **melanoma** and renal cell carcinoma, often in combination with nivolumab. * While it is an immune checkpoint inhibitor, its primary indications and specific FDA approvals do not include **endometrial carcinoma**. *Trastuzumab* * **Trastuzumab** (Herceptin) is a **monoclonal antibody** that targets the **HER2 protein**, commonly used in the treatment of **HER2-positive breast cancer** and certain types of gastric cancer. * It is not an immune checkpoint inhibitor and its mechanism of action is distinct from blocking immune checkpoints like PD-1 or CTLA-4. *Nivolumab* * **Nivolumab** (Opdivo) is a **PD-1 inhibitor** with broad FDA approvals for various cancers, including melanoma, non-small cell lung cancer, renal cell carcinoma, classical Hodgkin lymphoma, and others. * While a potent immune checkpoint inhibitor, **pembrolizumab** received the specific accelerated approval for advanced endometrial carcinoma in the context described, making it the most direct answer for the "new FDA approved" status in this specific indication.

Q: Osimertinib is used in NSCLC with which mutation?

T790M mutation. ***T790M mutation*** - **Osimertinib** is a third-generation **EGFR tyrosine kinase inhibitor (TKI)** specifically designed to overcome resistance to earlier generation EGFR TKIs. - The **T790M mutation** in the EGFR gene is the most common mechanism of acquired resistance to first and second-generation EGFR TKIs in non-small cell lung cancer (NSCLC). *L858R mutation* - The **L858R mutation** is an activating **EGFR mutation** typically sensitive to first and second-generation EGFR TKIs. - While patients with **L858R** may eventually develop resistance, **osimertinib** is primarily used in the setting of acquired resistance, often mediated by **T790M**. *M790T mutation* - This is not a recognized common or clinically significant activating or resistance mutation in the **EGFR gene** for NSCLC. - The correct resistance mutation that **osimertinib** targets is **T790M**, not **M790T**. *T890M mutation* - This is a typographical error for the clinically relevant **T790M mutation**. - The number sequence is critical for identifying specific amino acid substitutions in gene mutations.

Q: What is the treatment for HER-2 positive trastuzumab resistant breast cancer?

Lapatinib. ***Lapatinib*** - Lapatinib is a **dual tyrosine kinase inhibitor** that targets both **HER-2** and **epidermal growth factor receptor (EGFR)**, acting as a **small molecule inhibitor** that binds to the intracellular domain of these receptors. - Unlike trastuzumab (a monoclonal antibody targeting the extracellular domain), Lapatinib's **intracellular mechanism of action** allows it to overcome common mechanisms of trastuzumab resistance, such as receptor truncation or masking of the extracellular epitope. - It is specifically approved for the treatment of **HER-2 positive metastatic breast cancer** in combination with capecitabine after progression on trastuzumab-containing regimens. *Sorafenib* - Sorafenib is a **multi-kinase inhibitor** primarily targeting RAF, VEGFR, and PDGFR, and is used in renal cell carcinoma and hepatocellular carcinoma. - It does not specifically target HER-2 and is **not indicated** for HER-2 positive trastuzumab-resistant breast cancer. *Vemurafenib* - Vemurafenib is a **BRAF inhibitor** used for treating BRAF V600E mutation-positive melanoma. - This drug has no direct indications or demonstrated efficacy for **HER-2 positive breast cancer** and does not address trastuzumab resistance mechanisms. *Erlotinib* - Erlotinib is an **EGFR tyrosine kinase inhibitor** primarily used for non-small cell lung cancer with activating EGFR mutations. - While it targets EGFR, it does **not effectively target HER-2** and lacks the dual inhibition necessary to overcome trastuzumab resistance in HER-2 positive breast cancer.

Q: A 52-year-old female patient presents with HER-2 positive breast cancer that has become resistant to trastuzumab treatment. The oncologist is considering the next line of treatment for the patient. Which of the following options would be the most appropriate choice?

Lapatinib. ***Lapatinib*** - Lapatinib is an oral **dual tyrosine kinase inhibitor** that targets both **HER2** and **EGFR** receptors, specifically approved for **trastuzumab-resistant HER2-positive breast cancer**. - Unlike trastuzumab (a monoclonal antibody that binds the extracellular domain), lapatinib inhibits the **intracellular tyrosine kinase domain** of HER2, providing an **alternative mechanism** to overcome resistance. - Often used in combination with capecitabine for patients who have progressed on trastuzumab-containing regimens. - **Clinical evidence**: The EGF100151 trial demonstrated efficacy in trastuzumab-refractory disease. *Vemurafenib* - Vemurafenib is a **BRAF V600E/K inhibitor** used primarily for **metastatic melanoma** with BRAF mutations. - It has **no activity against HER2** and is not indicated for breast cancer. - Would not provide benefit in this clinical scenario. *Erlotinib* - Erlotinib is a selective **EGFR tyrosine kinase inhibitor** used for **EGFR-mutant non-small cell lung cancer** and **pancreatic cancer** (with gemcitabine). - While it inhibits EGFR (which lapatinib also targets), erlotinib has **insufficient HER2 inhibition** to be effective in HER2-driven breast cancer. - Not approved or effective for trastuzumab-resistant HER2-positive breast cancer. *Sorafenib* - Sorafenib is a **multi-kinase inhibitor** targeting **RAF kinases, VEGFR-2/3, and PDGFR-β**, approved for **hepatocellular carcinoma, renal cell carcinoma, and thyroid cancer**. - It does **not specifically target HER2** signaling and has no established role in HER2-positive breast cancer. - Would not address the mechanism of disease in this patient.

Q: What is the MOA of thalidomide?

Angiogenesis inhibitor. ***Angiogenesis inhibitor*** - Thalidomide is known to **inhibit angiogenesis** [1] by blocking the formation of new blood vessels, a key mechanism in its anti-cancer effects. - It also has **immunomodulatory** [1], [2], [3] and **anti-inflammatory** properties, affecting cytokine production and immune cell function [1], [3]. *Inhibits factor Xa* - This is the mechanism of action for **direct oral anticoagulants (DOACs)** like rivaroxaban and apixaban, used to prevent blood clot formation. - Thalidomide does not primarily act on the **coagulation cascade** at this step. *Prevents folic acid synthesis in bacteria* - This is the classic mechanism of action for **sulfonamide antibiotics**, which target bacterial enzymes involved in folate metabolism. - Thalidomide is an **immunomodulatory drug** [2], [3], not an antibiotic that interferes with bacterial folic acid synthesis. *Inhibits leukotrienes* - **Leukotriene inhibitors**, such as montelukast and zafirlukast, are used to treat asthma and allergies by blocking inflammatory pathways. - Thalidomide's primary mechanism is not the direct inhibition of **leukotriene synthesis or receptor binding**.

Q: Nivolumab is used as checkpoint inhibitor in

Hodgkin's lymphoma. ***Hodgkin's lymphoma*** - **Nivolumab** is an **immune checkpoint inhibitor** targeting **PD-1**. It has shown significant efficacy in treating relapsed or refractory Hodgkin's lymphoma, particularly in patients who have failed prior therapies. - Hodgkin's lymphoma cells, specifically **Reed-Sternberg cells**, often overexpress PD-L1, which allows them to evade the immune system, making PD-1 blockade a rational therapeutic strategy. *Medulloblastoma* - **Medulloblastoma** is a common malignant brain tumor in children, and while immunotherapy research is ongoing, Nivolumab is **not a standard treatment** for this condition. - Treatment typically involves **surgery, radiation, and chemotherapy**, with targeted therapies under investigation. *Retinoblastoma* - **Retinoblastoma** is a malignant tumor of the retina, most commonly affecting young children. Treatment usually involves **chemotherapy, laser therapy, cryotherapy, or enucleation**. - There is **no established role for Nivolumab** or PD-1 inhibitors in the routine management of retinoblastoma. *Pleuropulmonary blastoma* - **Pleuropulmonary blastoma** is a rare, malignant lung tumor of childhood. Treatment primarily consists of **surgery and chemotherapy**. - While experimental, there is **no current evidence** supporting the use of Nivolumab as a standard treatment for pleuropulmonary blastoma.

Q: Which is the most cardiotoxic anti-cancer drug among the following?

Anthracyclines. ***Anthracyclines*** - **Anthracyclines** (e.g., doxorubicin, daunorubicin) are notorious for causing **dose-dependent cardiotoxicity**, leading to **irreversible dilated cardiomyopathy** and **heart failure**. - Their cardiotoxic effect is primarily due to the generation of **reactive oxygen species** and interference with cardiac topoisomerase IIβ. *Cyclophosphamide* - Cyclophosphamide can cause cardiotoxicity, particularly at **high doses**, manifesting as **hemorrhagic myocardial necrosis** or **pericarditis**. - However, its cardiotoxicity is generally considered **less frequent and severe** than that of anthracyclines. *Tamoxifen* - Tamoxifen is primarily associated with an **increased risk of thromboembolic events** and **endometrial cancer**. - While some cardiac effects like **QT prolongation** can occur, it is not considered a primary cardiotoxic agent leading to cardiomyopathy. *Imatinib* - Imatinib, a **tyrosine kinase inhibitor**, has been linked to **cardiac dysfunction** including heart failure in some patients. - However, the incidence and severity of cardiotoxicity with imatinib are **lower** compared to anthracyclines, which are broadly cardiotoxic.

Question 1

Match the following drugs with the targets of their actions:

Drugs:
A. Trastuzumab
B. Infliximab  
C. Sirolimus
D. Imatinib

Targets:
1. BCR-ABL tyrosine kinase
2. mTOR
3. TNF alpha
4. HER2/neu

Accepted Answer

A-4, B-3, C-2, D-1

Answer

A-2, B-3, C-1, D-4

Answer

A-3, B-4, C-2, D-1

Answer

A-4, B-3, C-1, D-2

Question 2

A lady who had undergone mastectomy for breast cancer is being treated with tamoxifen. How long should it be stopped before she can conceive?

Accepted Answer

3 months

Answer

No need to stop

Answer

Can be stopped and conceived soon after stopping

Answer

1 month

Question 3

Which among the following drugs is the new FDA approved immune checkpoint inhibitor for endometrial carcinoma?

Accepted Answer

Pembrolizumab

Answer

Ipilimumab

Answer

Trastuzumab

Answer

Nivolumab

Question 4

Osimertinib is used in NSCLC with which mutation?

Accepted Answer

T790M mutation

Answer

L858R mutation

Answer

M790T mutation

Answer

T890M mutation

Question 5

What is the treatment for HER-2 positive trastuzumab resistant breast cancer?

Accepted Answer

Lapatinib

Answer

Sorafenib

Answer

Vemurafenib

Answer

Erlotinib

Question 6

A 52-year-old female patient presents with HER-2 positive breast cancer that has become resistant to trastuzumab treatment. The oncologist is considering the next line of treatment for the patient. Which of the following options would be the most appropriate choice?

Accepted Answer

Lapatinib

Answer

Vemurafenib

Answer

Erlotinib

Answer

Sorafenib

Question 7

What is the MOA of thalidomide?

Accepted Answer

Angiogenesis inhibitor

Answer

Inhibits factor Xa

Answer

Prevents folic acid synthesis in bacteria

Answer

Inhibits leukotrienes

Question 8

Nivolumab is used as checkpoint inhibitor in

Accepted Answer

Hodgkin's lymphoma

Answer

Medulloblastoma

Answer

Retinoblastoma

Answer

Pleuropulmonary blastoma

Question 9

A 54-year-old woman with metastatic breast cancer comes to the physician for a follow-up examination. She had a mastectomy 6 months ago and received chemotherapy with doxorubicin and paclitaxel. A CT scan of the chest shows new metastases in the lungs and liver. Adjuvant therapy is initiated with a drug that inhibits the formation of deoxythymidine monophosphate and results in the accumulation of deoxyuridine triphosphate. The patient is advised to avoid folic acid supplementation while receiving this drug in order to prevent the toxic effects of this drug. Which of the following drugs was most likely given?

Accepted Answer

Capecitabine

Answer

Leflunomide

Answer

Mycophenolate mofetil

Answer

Hydroxyurea

Answer

Azathioprine

Question 10

Which is the most cardiotoxic anti-cancer drug among the following?

Accepted Answer

Anthracyclines

Answer

Cyclophosphamide

Answer

Tamoxifen

Answer

Imatinib

Anticancer Drugs — MCQs

Anticancer Drugs — MCQs

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