Pharmacology of Anthracycline DNA Binding Agents

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What is the mechanism of action of receptor tyrosine kinase inhibitors such as imatinib?

They bind to docking sites for downstream signaling proteins

They inhibit the conversion of testosterone to estradiol

They bind to tyrosine residues and prevent phosphorylation

They bind to ATP binding sites and prevent phosphorylation (correct)

What is the common cancer mutation that leads to constitutive phosphorylation and signaling?

Mutation in the estrogen receptor

Mutation in the tyrosine residues

Mutation in the ATP binding site

Mutation in the receptor tyrosine kinase (correct)

What is the therapeutic priority in breast cancers that express estrogen receptors?

Inhibition of receptor tyrosine kinase

Reduction of estrogen production (correct)

Reduction of testosterone production

Inhibition of downstream signaling proteins

What is the mechanism of action of aromatase inhibitors such as anastrozole and letrozole?

They inhibit the conversion of testosterone to estradiol Signup and view all the answers

What is the mechanism of action of selective estrogen receptor modulators (SERMs) such as tamoxifen?

They bind to estrogen receptors and antagonize estrogen Signup and view all the answers

What is the mechanism of action of selective estrogen receptor downregulators (SERDs) such as fulvestrant?

They cause degradation of the estrogen receptor Signup and view all the answers

What is the mechanism of action of anthracyclines, such as doxorubicin, on DNA?

They intercalate between DNA strands, inhibiting DNA repair and leading to fragmentation and apoptosis Signup and view all the answers

Which of the following is a common side effect of anthracyclines?

Cardiotoxicity Signup and view all the answers

What is the mechanism of action of microtubular inhibitors, such as vincristine and vinblastine?

They bind to beta tubulin and inhibit polymerisation into microtubules Signup and view all the answers

What is the effect of taxanes, such as paclitaxel, on microtubules?

They antagonise depolymerisation of microtubules, halting mitosis Signup and view all the answers

What is the common side effect of taxanes, such as paclitaxel, that requires pre-treatment with antihistamines or corticosteroids?

Hypersensitivity Signup and view all the answers

Which of the following is NOT a type of microtubular inhibitor?

Topoisomerase inhibitors Signup and view all the answers

What is the primary mechanism of action of alkylating agents like cyclophosphamide?

Formation of covalent cross-links between nucleotide bases Signup and view all the answers

What is a common side effect of platinum-based compounds like cisplatin?

Nephrotoxicity Signup and view all the answers

Which type of anticancer drug works by mimicking essential structures within the cell?

Antimetabolites Signup and view all the answers

What is the primary advantage of using regimens of more than one drug?

Improved cell cytotoxicity and reduced development of resistance Signup and view all the answers

Why are alkylating agents often used in combination with other drugs?

They are less specific and require combination therapy Signup and view all the answers

What is the mode of administration of cyclophosphamide?

Either oral or IV Signup and view all the answers