Evaluation of gefitinib systemic exposure in EGFR-mutated non-small cell lung cancer patients with gefitinib-induced severe hepatotoxicity.
Adult
Aged
Aged, 80 and over
Antineoplastic Agents
/ adverse effects
Area Under Curve
Carcinoma, Non-Small-Cell Lung
/ drug therapy
Chemical and Drug Induced Liver Injury
/ etiology
Drug-Related Side Effects and Adverse Reactions
/ etiology
ErbB Receptors
/ genetics
Female
Gefitinib
/ adverse effects
Humans
Liver
/ drug effects
Lung Neoplasms
/ drug therapy
Male
Middle Aged
Gefitinib
Non-small cell lung cancer
Pharmacokinetics
Protein binding
Severe hepatotoxicity
Systemic exposure
Journal
Cancer chemotherapy and pharmacology
ISSN: 1432-0843
Titre abrégé: Cancer Chemother Pharmacol
Pays: Germany
ID NLM: 7806519
Informations de publication
Date de publication:
03 2020
03 2020
Historique:
received:
24
09
2019
accepted:
20
01
2020
pubmed:
11
2
2020
medline:
13
11
2020
entrez:
11
2
2020
Statut:
ppublish
Résumé
Severe hepatotoxicity induced by the standard dose of gefitinib (250 mg daily) often becomes manageable by dose reduction to 250 mg every other day. Thus, we hypothesized that systemic exposure of standard-dose gefitinib in patients with experience of severe hepatotoxicity might be higher than that in patients without severe hepatotoxicity. Patients with advanced epidermal growth factor receptor-mutated non-small cell lung cancer who were receiving gefitinib either at a reduced dose (250 mg every other day) because of intolerable severe toxicity or at a standard dose (250 mg daily) were enrolled. A series of blood samples were collected to estimate pharmacokinetic parameters and calculate systemic exposure of standard-dose gefitinib (area under the concentration-time curve from 0 to 24 h at steady state, AUC Of the 38 enrolled patients, 34 (23 patients without experience of severe hepatotoxicity, 11 patients with experience of severe hepatotoxicity) were evaluable. There was no significant differences in total AUC This study suggests that reversible severe hepatotoxicity is not caused by high systemic exposure of gefitinib.
Identifiants
pubmed: 32040702
doi: 10.1007/s00280-020-04034-y
pii: 10.1007/s00280-020-04034-y
doi:
Substances chimiques
Antineoplastic Agents
0
EGFR protein, human
EC 2.7.10.1
ErbB Receptors
EC 2.7.10.1
Gefitinib
S65743JHBS
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
605-614Références
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