Anticancer Drugs Practice Questions

Q: All of the following are true regarding Erlotinib except:

Food decreases absorption.. **Explanation:** **Erlotinib** is a targeted anticancer therapy belonging to the class of small-molecule **Tyrosine Kinase Inhibitors (TKIs)**. 1. **Why Option C is the correct answer (The Exception):** The statement "Food decreases absorption" is incorrect. In fact, **food significantly increases the bioavailability** of Erlotinib (potentially up to 100%). To ensure consistent drug levels and avoid increased toxicity, it must be taken on an empty stomach (at least 1 hour before or 2 hours after a meal). 2. **Analysis of Incorrect Options:** * **Option A:** Erlotinib is a standard first-line treatment for **Non-Small Cell Lung Carcinoma (NSCLC)**, particularly in patients with activating mutations in the EGFR gene (Exon 19 deletions or Exon 21 L858R mutations). * **Option B:** It acts by competitively inhibiting the ATP-binding site of the intracellular tyrosine kinase domain of the **Epidermal Growth Factor Receptor (EGFR/ErbB1)**, preventing downstream signaling. * **Option D:** The most common adverse effects of EGFR inhibitors are **acneiform skin rashes** (seen in >75% of patients) and **diarrhea**. Interestingly, the severity of the rash often correlates with a better therapeutic response. **High-Yield Clinical Pearls for NEET-PG:** * **Drug Interactions:** Solubility of Erlotinib is pH-dependent. **Proton Pump Inhibitors (PPIs)** and H2 blockers decrease its absorption by increasing gastric pH. * **Smoking:** Cigarette smoking induces CYP1A2, which increases the clearance of Erlotinib, necessitating higher doses in smokers. * **Resistance:** The most common mechanism of acquired resistance to Erlotinib is the **T790M mutation**, for which **Osimertinib** (a 3rd generation TKI) is used.

Q: Which of the following anti-cancer drugs is NOT S-phase specific?

Ifosfamide. **Explanation:** The cell cycle specificity of anticancer drugs is a high-yield concept for NEET-PG. Anticancer agents are broadly classified into **Cell Cycle-Specific (CCS)** and **Cell Cycle-Non-Specific (CCNS)** drugs. **Why Ifosfamide is the correct answer:** Ifosfamide is an **alkylating agent** (a nitrogen mustard derivative). Alkylating agents work by covalently bonding alkyl groups to DNA bases (primarily Guanine), leading to DNA cross-linking and strand breaks. This mechanism occurs regardless of whether the cell is actively dividing or resting. Therefore, Ifosfamide is **Cell Cycle-Non-Specific (CCNS)**. While it is most toxic to cells in the late G1 or S phase, it does not target a specific phase to exert its action. **Why the other options are incorrect:** * **Methotrexate:** An antimetabolite that inhibits *Dihydrofolate Reductase (DHFR)*. It prevents the synthesis of tetrahydrofolate, which is essential for thymidylate and purine synthesis. This process is strictly required during DNA synthesis, making it **S-phase specific**. * **Mercaptopurine (6-MP) & Thioguanine (6-TG):** These are purine analogues. They act as "fraudulent nucleotides" that incorporate into DNA/RNA or inhibit *de novo* purine synthesis. Since DNA replication occurs during the **S-phase**, these drugs are phase-specific. **High-Yield Clinical Pearls for NEET-PG:** 1. **Acrolein Toxicity:** Both Ifosfamide and Cyclophosphamide produce a toxic metabolite called **Acrolein**, which causes **Hemorrhagic Cystitis**. 2. **Prevention:** Hemorrhagic cystitis is prevented by aggressive hydration and **MESNA** (2-Mercaptoethane sulfonate Na), which neutralizes acrolein in the bladder. 3. **Mnemonic for S-phase drugs:** "It’s **S**mart to **MET** at the **PUR**ine **PYR**amid" (**MET**hotrexate, **PUR**ines like 6-MP/6-TG, **PYR**imidines like 5-FU/Cytarabine).

Q: All of the following side effects are produced by Cisplatin except?

Pulmonary fibrosis. **Explanation:** **Cisplatin** is a potent platinum-based alkylating agent used for various solid tumors. The correct answer is **Pulmonary fibrosis**, as this is a classic dose-limiting toxicity associated with **Bleomycin** and **Busulfan**, not Cisplatin. **Why the other options are incorrect (Side effects of Cisplatin):** * **Nephrotoxicity:** This is the most significant dose-limiting toxicity of Cisplatin. It causes acute tubular necrosis. It is managed with aggressive **amifostine** (a cytoprotective agent) and pre-treatment hydration. * **Ototoxicity:** Cisplatin causes high-frequency hearing loss and tinnitus due to damage to the hair cells in the cochlea. This is often irreversible. * **Coasting Effect:** This refers to a unique phenomenon seen with Cisplatin-induced peripheral neuropathy where the neurological symptoms continue to worsen for several weeks even after the drug has been discontinued. * **Emetogenicity:** Though not listed as an option, Cisplatin is the most highly emetogenic chemotherapy drug, requiring prophylaxis with 5-HT3 antagonists (e.g., Ondansetron) and Aprepitant. **High-Yield Clinical Pearls for NEET-PG:** * **Mnemonic for Cisplatin toxicity:** "PON" – **P**eripheral neuropathy, **O**totoxicity, **N**ephrotoxicity. * **Carboplatin** is a related drug that is less nephrotoxic and ototoxic but causes more significant **myelosuppression** (thrombocytopenia). * **Oxaliplatin** is notorious for causing **cold-induced peripheral neuropathy**. * To prevent Cisplatin-induced nephrotoxicity, always remember: **Hydration + Chloride diuresis + Amifostine.**

Q: What is the best single-drug chemotherapy agent for the treatment of carcinoma of the cheek?

Cisplatin. **Explanation:** **1. Why Cisplatin is the Correct Answer:** Carcinoma of the cheek (Squamous Cell Carcinoma of the Oral Cavity) is primarily managed surgically or with radiotherapy. However, when chemotherapy is indicated—either as a radiosensitizer or for palliative/recurrent cases—**Cisplatin** is considered the "gold standard" single-drug agent. It is a platinum-based alkylating-like agent that causes DNA cross-linking, leading to apoptosis. In Head and Neck Squamous Cell Carcinoma (HNSCC), Cisplatin demonstrates the highest response rates among single agents and is the backbone of most combination regimens (e.g., PF regimen: Cisplatin + 5-Fluorouracil). **2. Why the Other Options are Incorrect:** * **Cyclophosphamide (A):** An alkylating agent primarily used in lymphomas, breast cancer, and certain pediatric tumors. It has minimal efficacy in epithelial head and neck cancers. * **Vincristine (B):** A vinca alkaloid that inhibits microtubule formation. It is used in leukemias, lymphomas, and sarcomas (like rhabdomyosarcoma), but is not a primary agent for oral SCC. * **Daunorubicin (C):** An anthracycline used almost exclusively in acute leukemias (AML/ALL). It has no role in the management of solid tumors like cheek carcinoma. **3. NEET-PG High-Yield Pearls:** * **Drug of Choice:** Cisplatin is the most effective single agent for HNSCC. * **Radiosensitization:** Low-dose weekly Cisplatin is the standard concurrent chemotherapy given during radiotherapy to enhance local control. * **Side Effects:** Always remember the "C" triad for Cisplatin: **C**hemoreceptor trigger zone stimulation (highly emetogenic), **C**ochlear toxicity (ototoxicity), and **C**onvoluted tubule damage (nephrotoxicity). * **Amifostine** is used to reduce Cisplatin-induced nephrotoxicity.

Q: Which of the following statements about Tacrolimus is incorrect?

It can be safely administered with any nephrotoxic drug.. **Explanation:** **1. Why Option B is the Correct (Incorrect Statement):** Tacrolimus is a **calcineurin inhibitor** (CNI). Its most significant and dose-limiting toxicity is **nephrotoxicity**, which occurs due to potent vasoconstriction of the afferent arterioles. Administering Tacrolimus with other nephrotoxic drugs (such as Aminoglycosides, Amphotericin B, or NSAIDs) creates a synergistic toxic effect, significantly increasing the risk of acute kidney injury (AKI). Therefore, it cannot be "safely administered" with such drugs; close monitoring of serum creatinine and drug levels is mandatory. **2. Analysis of Other Options:** * **Option A:** Tacrolimus is chemically classified as a **macrolide**, though it lacks antibacterial activity. It is derived from the fungus *Streptomyces tsukubaensis*. * **Option C:** Tacrolimus is known to cause **post-transplant diabetes mellitus (PTDM)**. It impairs glucose tolerance by inhibiting insulin secretion from pancreatic beta cells more significantly than Cyclosporine. * **Option D:** It is a first-line immunosuppressant used for the **prophylaxis of organ rejection** in liver, kidney, and heart transplants. **3. High-Yield Clinical Pearls for NEET-PG:** * **Mechanism of Action:** Binds to **FKBP-12** (FK-binding protein) $\rightarrow$ inhibits Calcineurin $\rightarrow$ prevents dephosphorylation of **NFAT** $\rightarrow$ inhibits IL-2 transcription. * **Side Effect Profile (The "3 H's"):** **H**yperglycemia, **H**yperkalemia, and **H**ypertension. * **Neurotoxicity:** Tacrolimus is more neurotoxic than Cyclosporine (causing tremors, seizures, and headache). * **Comparison:** Unlike Cyclosporine, Tacrolimus does **not** cause hirsutism or gum hyperplasia; it may actually cause alopecia.

Q: Which adverse effect of Bleomycin is exacerbated by radiation exposure?

Pulmonary toxicity. ***Pulmonary toxicity*** - Bleomycin is well-known for causing dose-dependent **pulmonary fibrosis**. It damages **type I pneumocytes**, leading to inflammation, proliferation of **type II pneumocytes**, and eventual fibrosis, impairing gas exchange. - The risk of pulmonary toxicity is significantly increased by concurrent or prior **chest radiation therapy** and administration of high concentrations of supplemental **oxygen**, as both are also injurious to lung tissue. *Gastric toxicity* - Bleomycin is not typically associated with significant gastric toxicity. Common side effects are milder and include **mucositis** and **stomatitis** rather than severe gastric damage. - There is no evidence of a synergistic toxic effect on the gastric mucosa when Bleomycin is combined with radiation therapy. *Neural toxicity* - Neurotoxicity is not a characteristic side effect of Bleomycin. Chemotherapeutic agents like **vincristine** and **cisplatin** are more commonly associated with peripheral neuropathy. - While radiation can cause nerve damage, this is not a known interaction that is specifically exacerbated by Bleomycin administration. *Hepatotoxicity* - Severe liver damage (**hepatotoxicity**) is a rare side effect of Bleomycin. Mild and transient elevations of liver enzymes may occur but are not clinically significant. - Unlike the lungs, the liver is not a primary site for synergistic toxicity between Bleomycin and radiation therapy.

Q: Which of the following statements regarding Thalidomide is correct? a. It acts as an antimetabolite and is useful as an immunosuppressant b. It is used in the treatment of multiple myeloma c. It is used in the management of Type 2 lepra reaction (ENL) d. It is teratogenic

b, c, d. ***b, c, d*** - Statements b, c, and d are correct: Thalidomide is an **Immunomodulatory Drug (IMiD)** used effectively in the treatment of **multiple myeloma**, it is the drug of choice for **Erythema Nodosum Leprosum (ENL)** (Type 2 lepra reaction), and it is historically significant for causing **phocomelia** (teratogenicity). - Its mechanism involves downregulation of **pro-inflammatory cytokines** like TNF-alpha, which underlies its use in ENL, and anti-angiogenic/anti-proliferative effects against myeloma cells. *a, b, c* - Statement 'a' is incorrect because Thalidomide is an **Immunomodulatory Drug (IMiD)**, not an **antimetabolite** (a class of drugs that inhibit DNA/RNA synthesis). - Inclusion of the incorrect mechanism ('a') invalidates this set, despite 'b' (multiple myeloma) and 'c' (ENL) being correct clinical applications. *a, c, d* - This combination is incorrect primarily because it includes statement 'a', which wrongly defines Thalidomide as an **antimetabolite**. - Crucially, this option omits statement 'b', which is a major, current indication for Thalidomide in **multiple myeloma**. *a, b, d* - This combination wrongly includes the factual error of statement 'a' (it is not an **antimetabolite**). - It also misses statement 'c', which is the prominent use of Thalidomide in **Type 2 lepra reaction (ENL)**.

Q: Treatment with Herceptin in breast cancer is indicated for

Tumours with over-expressed HER2/C-erbB-2 protein. **tumours with over-expressed C-erb B-2 protein** - **Herceptin** (trastuzumab) is a monoclonal antibody that specifically targets the **HER2/neu receptor**, which is encoded by the *ERBB2* gene. - Its efficacy depends on the **overexpression of C-erbB-2 protein** (also known as HER2/neu) on the surface of breast cancer cells, which indicates **HER2-positive breast cancer**. *K : 67 stain +ve tumours* - **Ki-67** is a proliferation marker that indicates the **growth fraction of a tumor**, and a positive stain suggests a rapidly dividing tumor. - While Ki-67 positivity is associated with more aggressive tumors, it does **not directly indicate suitability for Herceptin** treatment. *PR receptor +ve tumours* - Tumors positive for the **progesterone receptor (PR)** are typically treated with **hormonal therapies**, such as tamoxifen or aromatase inhibitors. - **PR positivity** does not indicate responsiveness to Herceptin, which targets the HER2 receptor. *ER receptor +ve tumours* - Tumors positive for the **estrogen receptor (ER)** are also treated with **hormonal therapies** due to their dependence on estrogen for growth. - Similarly to PR-positive tumors, **ER positivity** does not determine eligibility for Herceptin therapy.

Question 1

All of the following are true regarding Erlotinib except:

Accepted Answer

Food decreases absorption.

Answer

Used in non-small cell carcinoma of the lung.

Answer

It is a small molecule tyrosine kinase inhibitor acting as an EGFR antagonist.

Answer

It causes skin rashes and diarrhea.

Question 2

Which of the following anti-cancer drugs is NOT S-phase specific?

Accepted Answer

Ifosfamide

Answer

Methotrexate

Answer

Mercaptopurine

Answer

Thioguanine

Question 3

All of the following side effects are produced by Cisplatin except?

Accepted Answer

Pulmonary fibrosis

Answer

Ototoxicity

Answer

Nephrotoxicity

Answer

Coasting effect

Question 4

What is the best single-drug chemotherapy agent for the treatment of carcinoma of the cheek?

Accepted Answer

Cisplatin

Answer

Cyclophosphamide

Answer

Vincristine

Answer

Danorubicin

Question 5

Which of the following statements about Tacrolimus is incorrect?

Accepted Answer

It can be safely administered with any nephrotoxic drug.

Answer

It is a macrolide antibiotic.

Answer

Glucose intolerance is a well-known side effect.

Answer

It is used for prophylaxis of transplant rejection.

Question 6

What is the key difference between Cisplatin and Carboplatin?

Accepted Answer

Cisplatin has more nephrotoxic side effects compared to Carboplatin

Answer

Cisplatin is less neurotoxic than Carboplatin

Answer

Carboplatin is more neurotoxic than Cisplatin

Answer

Cisplatin causes fewer gastric issues compared to Carboplatin

Question 7

Which adverse effect of Bleomycin is exacerbated by radiation exposure?

Accepted Answer

Pulmonary toxicity

Answer

Neural toxicity

Answer

Hepatotoxicity

Answer

Gastric toxicity

Question 8

What is the primary mechanism of action of methotrexate?

Accepted Answer

Inhibits dihydrofolate reductase, leading to decreased DNA synthesis

Answer

Inhibits RNA synthesis by blocking RNA polymerase

Answer

Interferes with microtubule formation during cell division

Answer

Inhibits DNA synthesis by blocking thymidylate synthase

Question 9

Which of the following statements regarding Thalidomide is correct?
a. It acts as an antimetabolite and is useful as an immunosuppressant
b. It is used in the treatment of multiple myeloma
c. It is used in the management of Type 2 lepra reaction (ENL)
d. It is teratogenic

Accepted Answer

b, c, d

Answer

a, b, d

Answer

a, b, c

Answer

a, c, d

Question 10

Treatment with Herceptin in breast cancer is indicated for

Accepted Answer

Tumours with over-expressed HER2/C-erbB-2 protein

Answer

PR receptor +ve tumours

Answer

ER receptor +ve tumours

Answer

Ki-67 stain +ve tumours

Anticancer Drugs — MCQs

Anticancer Drugs — MCQs

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