Differences in adverse events between 250mg daily gefitinib and 150mg daily erlotinib in Japanese patients with non-small cell lung cancer

Drug Interaction Studies Reveal That Simotinib Upregulates Intestinal Absorption by Increasing the Paracellular Permeability of Intestinal Epithelial Cells

“…Oral administration is the major delivery route for simotinib, and high dosage of EGFR-TKI administration results in some gastrointestinal side effects, such as nausea, vomiting, diarrhea and emaciation. 4) Simotinib also displayed the same adverse gastrointestinal effects in our preliminary studies. The maximum tolerated dose (MTD) of simotinib is 500 mg. Over this dosage range, patients would suffer from nausea, vomiting, diarrhea and emaciation.…”

Variability in bioavailability of small molecular tyrosine kinase inhibitors

“…Many anticancer drugs are known to exhibit a small therapeutic window, where the minimum therapeutic dose and the maximum tolerated dose (MTD) are close to each other [38]. The same is true for the smTKIs, with a possible exception of Dabrafenib, Imatinib, Gefitinib and Pazopanib [13,19,[39][40][41][42][43][44][45][46][47][48][49][50][51][52]. As a consequence of pharmacokinetic variation, inter-individual differences in therapeutic dose and MTD should be taken into account.…”

Semiology of skin toxicity associated with epidermal growth factor receptor (EGFR) inhibitors

“…More extensive folliculitis with a crusty, haemorrhagic clinical course, in particular on the face, has been reported with monoclonal antibodies, especially cetuximab [4,[11][12][13]31]. Among the TKI, folliculitis seems to be more severe with erlotinib than with gefitinib [32]. It could be linked to their different molecular structures that confer pharmacokinetic differences.…”