Medical Pharmacology Practice Questions: Chapter 33-34 Protein Tyrosine Kinase Inhibitors of EGFR: Neratinib (Nerlynx)

Medical Pharmacology Practice Questions: Protein Tyrosine Kinase Inhibitors of EGFR: Neratinib (Nerlynx)

Neratinib (Nerlynx): Nerlynx is classified as in irreversible tyrosine kinase inhibitor.
1. True
2. False
Neratinib irreversibly inhibits which one(s) of the following?
1. Human epidermal growth factor receptor 1 (HER1)
2. Human epidermal growth factor receptor 2 (HER2)
3. Human epidermal growth factor receptor 4 (HER4)
4. A & B
5. B & C
6. A & C
7. A, B & C
Neratinib irreversibly inhibits epidermal growth factor receptor (EGFR).
1. True
2. False
Neratinib:
1. Decreases EGFR and HER2 autophosphorylation
2. Reduces MAPK and AKT downstream signaling pathways
3. Both
4. Neither
Neratinib administration results in antitumor effects in EGFR and/or HER2 expressing cancer cell lines (in vitro).
1. True
2. False
Neratinib:
1. Therapeutic indication similar to that for lapatinib.
2. Neratinib does not exhibit cross-resistance with trastuzumab (monoclonal antibody), allowing for coadministration benefit.
3. Both
4. Neither
Neratinib pharmacokinetic/pharmacodynamics:
1. A high-fat meal is likely to increase neratinib Cmax.
2. Volume of distribution at steady-state is about 6400 L.
3. Both
4. Neither
Neratinib metabolism:
1. Mainly hepatic, utilizing the P450 drug metabolizing system relying principally on the CYP3A4 enzyme isoform.
2. Some metabolism also catalyzed by flavin-containing monooxygenase
3. Both
4. Neither
Neratinib adverse effect concerns:
1. GI toxicity
2. Hepatotoxicity
3. Both
4. Neither
Neratinib dose reductions may be needed in patients with significant, pre-existing liver disease.
1. True
2. False