Open Access<p>Effects of Apatinib on the Pharmacokinetics of Nifedipine and Warfarin in Patients with Advanced Solid Tumors</p>
Author(s) -
Yunting Zhu,
Teng Zhang,
Yifan Zhang,
Wei Li,
Li-xia Guo,
Yunpeng Liu,
Xiujuan Qu,
Quanren Wang,
Si-Yuan Mao,
Xiaoyan Chen,
Dafang Zhong
Publication year - 2020
Publication title -
drug design, development and therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.964
H-Index - 64
ISSN - 1177-8881
DOI - 10.2147/dddt.s237301
Subject(s) - apatinib , cmax , medicine , warfarin , pharmacology , pharmacokinetics , nifedipine , drug interaction , cyp3a4 , tyrosine kinase inhibitor , concomitant , adverse effect , cancer , cytochrome p450 , metabolism , calcium , atrial fibrillation
Apatinib is a small-molecule tyrosine kinase inhibitor for the treatment of recurrent or progressive advanced-stage gastric adenocarcinoma or gastroesophageal junction cancer. The in vitro inhibition studies suggested that apatinib exerted potent inhibition on CYP3A4 and CYP2C9. To evaluate the potential of apatinib as a perpetrator in CYP450-based drug-drug interactions in vivo, nifedipine and warfarin were, respectively, selected in the present study as the probe substrates of CYP3A4 and CYP2C9 for clinical drug-drug interaction studies. Since hypertension and thrombus are common adverse effects of vascular targeting anticancer agents, nifedipine and warfarin are usually coadministered with apatinib in clinical practice.