Abstract

Ibrutinib, an oral Bruton’s tyrosine kinase inhibitor, is a key drug for the treatment of chronic lymphocytic leukemia (CLL). It is primarily metabolized by cytochrome P450 3A. However, there are no data on the pharmacokinetics of ibrutinib in patients with severe renal impairment or on hemodialysis (HD). We evaluated the pharmacokinetics of ibrutinib in a patient with CLL undergoing HD. An 84-year-old man on HD was diagnosed with CLL and was started on ibrutinib 140 mg daily. The second day of ibrutinib administration was an HD day, and its plasma concentrations before and 1, 2, 4, and 24 hours after administration were measured and found to be 0, 6.9, 28.4, 57.1, and 0 ng/mL, respectively. The maximum plasma concentration (C_max) and time taken to reach C_max (t_max) on days 14 and 15 of ibrutinib treatment were 64.8 ng/mL (4 hours) and 48.1 ng/mL (2 hours), respectively. Thus, we concluded that HD did not have a significant effect on the pharmacokinetics of ibrutinib in this patient. Therefore, dose adjustment of ibrutinib between HD and non-HD days is not recommended. Interestingly, we found that t_max of the drug was prolonged, and C_max was higher on HD days compared to those on non-HD days.

Author Details

Authors

• Toyoji Ohtani¹
• Akiko Tani¹
• Yuki Namme¹
• Rie Namme¹
• Maki Hirose¹
• Ikuo Shingu¹
• Yusuke Kizawa²
• Akira Endo²
• Takeo Yasu³

Departments

• ¹ Department of Pharmacy,
• ² Department of Hematology, Matsue Red Cross Hospital, Shimane, and
• ³ Department of Medicinal Therapy Research, Pharmaceutical Education and Research Center, Meiji Pharmaceutical University, Tokyo, Japan

Address

Takeo Yasu, PhD
Department of Medicinal Therapy Research
Pharmaceutical Education and Research Center
Meiji Pharmaceutical University
2-522-1 Noshio, Kiyose, Tokyo, 204-8588, Japan
Email: [email protected]

Citation