Effect of isavuconazole on the concentration of tacrolimus in a patient with genotype CYP3A5*1/*3: a case report

Abstract Background Azole antifungals are the standard treatment for pulmonary mycosis, which may develop during long-term immunotherapy for kidney transplant. Isavuconazole (ISCZ) is a cytochrome P450 (CYP) 3 A inhibitor that has a risk of interacting with the immunosuppressive drug tacrolimus (TAC...

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Main Authors: Hayato Yokota, Yumiko Akamine, Harumi Hatakeyama, Hideaki Kagaya, Sho Sakamoto, Mitsuru Saito, Masahide Takeda, Kazuhiro Sato, Katsutoshi Nakayama, Masafumi Kikuchi
Format: Article
Language:English
Published: BMC 2025-03-01
Series:Journal of Pharmaceutical Health Care and Sciences
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Online Access:https://doi.org/10.1186/s40780-025-00427-4
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author Hayato Yokota
Yumiko Akamine
Harumi Hatakeyama
Hideaki Kagaya
Sho Sakamoto
Mitsuru Saito
Masahide Takeda
Kazuhiro Sato
Katsutoshi Nakayama
Masafumi Kikuchi
author_facet Hayato Yokota
Yumiko Akamine
Harumi Hatakeyama
Hideaki Kagaya
Sho Sakamoto
Mitsuru Saito
Masahide Takeda
Kazuhiro Sato
Katsutoshi Nakayama
Masafumi Kikuchi
author_sort Hayato Yokota
collection DOAJ
description Abstract Background Azole antifungals are the standard treatment for pulmonary mycosis, which may develop during long-term immunotherapy for kidney transplant. Isavuconazole (ISCZ) is a cytochrome P450 (CYP) 3 A inhibitor that has a risk of interacting with the immunosuppressive drug tacrolimus (TAC). We report a case of simple pulmonary aspergilloma with renal dysfunction due to increased trough levels of TAC after ISCZ coadministration. Case presentation A male in his 60s was treated with TAC 3.0 mg/day orally to prevent graft rejection after kidney transplantation. He received a loading dose of ISCZ 600 mg/day orally for two days, followed by a maintenance dose of 200 mg/day for simple pulmonary aspergilloma. The TAC trough concentration increased markedly from 2.4 to 9.9 ng/mL on day 6 after coadministration. The creatinine level increased from 0.70 to 1.08 mg/dL, suggesting renal dysfunction due to TAC. Subsequently, the TAC dosage was reduced, leading to a decreased blood TAC concentration and improved renal function. The patient’s genotype was CYP3A5*1/*3. Conclusions In the early stages of ISCZ treatment, the blood TAC concentration is higher, and CYP3A5 polymorphisms may partially explain the extent of this interaction. We recommend more careful monitoring of TAC and serum creatinine levels for approximately one week after ISCZ administration.
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spelling doaj-art-226684c6b4a142c8b87fef920e1c3e532025-08-20T02:56:21ZengBMCJournal of Pharmaceutical Health Care and Sciences2055-02942025-03-011111610.1186/s40780-025-00427-4Effect of isavuconazole on the concentration of tacrolimus in a patient with genotype CYP3A5*1/*3: a case reportHayato Yokota0Yumiko Akamine1Harumi Hatakeyama2Hideaki Kagaya3Sho Sakamoto4Mitsuru Saito5Masahide Takeda6Kazuhiro Sato7Katsutoshi Nakayama8Masafumi Kikuchi9Department of Pharmacy, Akita University HospitalDepartment of Pharmacy, Akita University HospitalDepartment of Pharmacy, Akita University HospitalDepartment of Pharmacy, Akita University HospitalDepartment of Respiratory Medicine, Akita University Graduate School of MedicineDepartment of Urology, Akita University Graduate School of MedicineDepartment of Respiratory Medicine, Akita University Graduate School of MedicineDepartment of Respiratory Medicine, Akita University Graduate School of MedicineDepartment of Respiratory Medicine, Akita University Graduate School of MedicineDepartment of Pharmacy, Akita University HospitalAbstract Background Azole antifungals are the standard treatment for pulmonary mycosis, which may develop during long-term immunotherapy for kidney transplant. Isavuconazole (ISCZ) is a cytochrome P450 (CYP) 3 A inhibitor that has a risk of interacting with the immunosuppressive drug tacrolimus (TAC). We report a case of simple pulmonary aspergilloma with renal dysfunction due to increased trough levels of TAC after ISCZ coadministration. Case presentation A male in his 60s was treated with TAC 3.0 mg/day orally to prevent graft rejection after kidney transplantation. He received a loading dose of ISCZ 600 mg/day orally for two days, followed by a maintenance dose of 200 mg/day for simple pulmonary aspergilloma. The TAC trough concentration increased markedly from 2.4 to 9.9 ng/mL on day 6 after coadministration. The creatinine level increased from 0.70 to 1.08 mg/dL, suggesting renal dysfunction due to TAC. Subsequently, the TAC dosage was reduced, leading to a decreased blood TAC concentration and improved renal function. The patient’s genotype was CYP3A5*1/*3. Conclusions In the early stages of ISCZ treatment, the blood TAC concentration is higher, and CYP3A5 polymorphisms may partially explain the extent of this interaction. We recommend more careful monitoring of TAC and serum creatinine levels for approximately one week after ISCZ administration.https://doi.org/10.1186/s40780-025-00427-4CYP3A5Drug–drug interactionsIsavuconazoleTacrolimusTherapeutic drug monitoring
spellingShingle Hayato Yokota
Yumiko Akamine
Harumi Hatakeyama
Hideaki Kagaya
Sho Sakamoto
Mitsuru Saito
Masahide Takeda
Kazuhiro Sato
Katsutoshi Nakayama
Masafumi Kikuchi
Effect of isavuconazole on the concentration of tacrolimus in a patient with genotype CYP3A5*1/*3: a case report
Journal of Pharmaceutical Health Care and Sciences
CYP3A5
Drug–drug interactions
Isavuconazole
Tacrolimus
Therapeutic drug monitoring
title Effect of isavuconazole on the concentration of tacrolimus in a patient with genotype CYP3A5*1/*3: a case report
title_full Effect of isavuconazole on the concentration of tacrolimus in a patient with genotype CYP3A5*1/*3: a case report
title_fullStr Effect of isavuconazole on the concentration of tacrolimus in a patient with genotype CYP3A5*1/*3: a case report
title_full_unstemmed Effect of isavuconazole on the concentration of tacrolimus in a patient with genotype CYP3A5*1/*3: a case report
title_short Effect of isavuconazole on the concentration of tacrolimus in a patient with genotype CYP3A5*1/*3: a case report
title_sort effect of isavuconazole on the concentration of tacrolimus in a patient with genotype cyp3a5 1 3 a case report
topic CYP3A5
Drug–drug interactions
Isavuconazole
Tacrolimus
Therapeutic drug monitoring
url https://doi.org/10.1186/s40780-025-00427-4
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