Effect of fluconazole on the pharmacokinetics of fuzuloparib: an open-label, crossover study in Chinese healthy male volunteers
Purpose Fuzuloparib (AiRuiYi TM , formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has multiple pharmacological activities in breast, ovarian, and prostatic cancer. Fuzuloparib is mainly metabolized through the enzyme CYP3A4 may s...
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| Vydáno v: | Cancer chemotherapy and pharmacology Ročník 89; číslo 1; s. 141 - 148 |
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| Hlavní autoři: | , , , , , , , , , |
| Médium: | Journal Article |
| Jazyk: | angličtina |
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Berlin/Heidelberg
Springer Berlin Heidelberg
01.01.2022
Springer Nature B.V |
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| ISSN: | 0344-5704, 1432-0843, 1432-0843 |
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| Abstract | Purpose
Fuzuloparib (AiRuiYi
TM
, formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has multiple pharmacological activities in breast, ovarian, and prostatic cancer. Fuzuloparib is mainly metabolized through the enzyme CYP3A4 may slow fuzuloparib metabolism and increase its concentrations in blood. We evaluated the pharmacokinetics and tolerability of fuzuloparib by fluconazole, which is a broad antifungal agent and a moderate inhibitor of CYP3A4.
Methods
In this study, the effects of CYP3A4 inhibition on the pharmacokinetics of fuzuloparib were assessed in a total of 20 healthy Chinese male subjects in an open-label, two-period, single-sequence, crossover study.
Results
Pharmacokinetic parameters, including the maximal plasma concentration (
C
max
)
,
the plasma concentration–time curve from time 0 to last measurable area under concentration (AUC
0−t
), and from time 0 to infinity (AUC
0−∞
), were increased by 32.4%, 104.5%, and 109.6%, with corresponding 90% confidence intervals of (23–43%), (93–116%), and (98–122%), respectively, when fluconazole was combined with fuzuloparib compared to fuzuloparib alone. There was also a slight increase in the incidence of treatment emergent adverse events, including hyperlipidemia and elevated aspartate transaminase.
Conclusion
The fuzuloparib is 150 mg b.i.d in clinics use. Our results suggest that fuzuloparib could well be tolerated when administered as a single 20 mg oral dose alone or co-administered with 400 mg fluconazole in healthy male subjects. It is recommended to avoid using moderate CYP3A4 inhibitors together with fuzuloparib or instead of 50 mg when necessary. |
|---|---|
| AbstractList | Purpose
Fuzuloparib (AiRuiYi
TM
, formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has multiple pharmacological activities in breast, ovarian, and prostatic cancer. Fuzuloparib is mainly metabolized through the enzyme CYP3A4 may slow fuzuloparib metabolism and increase its concentrations in blood. We evaluated the pharmacokinetics and tolerability of fuzuloparib by fluconazole, which is a broad antifungal agent and a moderate inhibitor of CYP3A4.
Methods
In this study, the effects of CYP3A4 inhibition on the pharmacokinetics of fuzuloparib were assessed in a total of 20 healthy Chinese male subjects in an open-label, two-period, single-sequence, crossover study.
Results
Pharmacokinetic parameters, including the maximal plasma concentration (
C
max
)
,
the plasma concentration–time curve from time 0 to last measurable area under concentration (AUC
0−t
), and from time 0 to infinity (AUC
0−∞
), were increased by 32.4%, 104.5%, and 109.6%, with corresponding 90% confidence intervals of (23–43%), (93–116%), and (98–122%), respectively, when fluconazole was combined with fuzuloparib compared to fuzuloparib alone. There was also a slight increase in the incidence of treatment emergent adverse events, including hyperlipidemia and elevated aspartate transaminase.
Conclusion
The fuzuloparib is 150 mg b.i.d in clinics use. Our results suggest that fuzuloparib could well be tolerated when administered as a single 20 mg oral dose alone or co-administered with 400 mg fluconazole in healthy male subjects. It is recommended to avoid using moderate CYP3A4 inhibitors together with fuzuloparib or instead of 50 mg when necessary. Fuzuloparib (AiRuiYiTM, formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has multiple pharmacological activities in breast, ovarian, and prostatic cancer. Fuzuloparib is mainly metabolized through the enzyme CYP3A4 may slow fuzuloparib metabolism and increase its concentrations in blood. We evaluated the pharmacokinetics and tolerability of fuzuloparib by fluconazole, which is a broad antifungal agent and a moderate inhibitor of CYP3A4.PURPOSEFuzuloparib (AiRuiYiTM, formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has multiple pharmacological activities in breast, ovarian, and prostatic cancer. Fuzuloparib is mainly metabolized through the enzyme CYP3A4 may slow fuzuloparib metabolism and increase its concentrations in blood. We evaluated the pharmacokinetics and tolerability of fuzuloparib by fluconazole, which is a broad antifungal agent and a moderate inhibitor of CYP3A4.In this study, the effects of CYP3A4 inhibition on the pharmacokinetics of fuzuloparib were assessed in a total of 20 healthy Chinese male subjects in an open-label, two-period, single-sequence, crossover study.METHODSIn this study, the effects of CYP3A4 inhibition on the pharmacokinetics of fuzuloparib were assessed in a total of 20 healthy Chinese male subjects in an open-label, two-period, single-sequence, crossover study.Pharmacokinetic parameters, including the maximal plasma concentration (Cmax), the plasma concentration-time curve from time 0 to last measurable area under concentration (AUC0-t), and from time 0 to infinity (AUC0-∞), were increased by 32.4%, 104.5%, and 109.6%, with corresponding 90% confidence intervals of (23-43%), (93-116%), and (98-122%), respectively, when fluconazole was combined with fuzuloparib compared to fuzuloparib alone. There was also a slight increase in the incidence of treatment emergent adverse events, including hyperlipidemia and elevated aspartate transaminase.RESULTSPharmacokinetic parameters, including the maximal plasma concentration (Cmax), the plasma concentration-time curve from time 0 to last measurable area under concentration (AUC0-t), and from time 0 to infinity (AUC0-∞), were increased by 32.4%, 104.5%, and 109.6%, with corresponding 90% confidence intervals of (23-43%), (93-116%), and (98-122%), respectively, when fluconazole was combined with fuzuloparib compared to fuzuloparib alone. There was also a slight increase in the incidence of treatment emergent adverse events, including hyperlipidemia and elevated aspartate transaminase.The fuzuloparib is 150 mg b.i.d in clinics use. Our results suggest that fuzuloparib could well be tolerated when administered as a single 20 mg oral dose alone or co-administered with 400 mg fluconazole in healthy male subjects. It is recommended to avoid using moderate CYP3A4 inhibitors together with fuzuloparib or instead of 50 mg when necessary.CONCLUSIONThe fuzuloparib is 150 mg b.i.d in clinics use. Our results suggest that fuzuloparib could well be tolerated when administered as a single 20 mg oral dose alone or co-administered with 400 mg fluconazole in healthy male subjects. It is recommended to avoid using moderate CYP3A4 inhibitors together with fuzuloparib or instead of 50 mg when necessary. Fuzuloparib (AiRuiYi , formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has multiple pharmacological activities in breast, ovarian, and prostatic cancer. Fuzuloparib is mainly metabolized through the enzyme CYP3A4 may slow fuzuloparib metabolism and increase its concentrations in blood. We evaluated the pharmacokinetics and tolerability of fuzuloparib by fluconazole, which is a broad antifungal agent and a moderate inhibitor of CYP3A4. In this study, the effects of CYP3A4 inhibition on the pharmacokinetics of fuzuloparib were assessed in a total of 20 healthy Chinese male subjects in an open-label, two-period, single-sequence, crossover study. Pharmacokinetic parameters, including the maximal plasma concentration (C ) the plasma concentration-time curve from time 0 to last measurable area under concentration (AUC ), and from time 0 to infinity (AUC ), were increased by 32.4%, 104.5%, and 109.6%, with corresponding 90% confidence intervals of (23-43%), (93-116%), and (98-122%), respectively, when fluconazole was combined with fuzuloparib compared to fuzuloparib alone. There was also a slight increase in the incidence of treatment emergent adverse events, including hyperlipidemia and elevated aspartate transaminase. The fuzuloparib is 150 mg b.i.d in clinics use. Our results suggest that fuzuloparib could well be tolerated when administered as a single 20 mg oral dose alone or co-administered with 400 mg fluconazole in healthy male subjects. It is recommended to avoid using moderate CYP3A4 inhibitors together with fuzuloparib or instead of 50 mg when necessary. PurposeFuzuloparib (AiRuiYiTM, formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has multiple pharmacological activities in breast, ovarian, and prostatic cancer. Fuzuloparib is mainly metabolized through the enzyme CYP3A4 may slow fuzuloparib metabolism and increase its concentrations in blood. We evaluated the pharmacokinetics and tolerability of fuzuloparib by fluconazole, which is a broad antifungal agent and a moderate inhibitor of CYP3A4.MethodsIn this study, the effects of CYP3A4 inhibition on the pharmacokinetics of fuzuloparib were assessed in a total of 20 healthy Chinese male subjects in an open-label, two-period, single-sequence, crossover study.ResultsPharmacokinetic parameters, including the maximal plasma concentration (Cmax), the plasma concentration–time curve from time 0 to last measurable area under concentration (AUC0−t), and from time 0 to infinity (AUC0−∞), were increased by 32.4%, 104.5%, and 109.6%, with corresponding 90% confidence intervals of (23–43%), (93–116%), and (98–122%), respectively, when fluconazole was combined with fuzuloparib compared to fuzuloparib alone. There was also a slight increase in the incidence of treatment emergent adverse events, including hyperlipidemia and elevated aspartate transaminase.ConclusionThe fuzuloparib is 150 mg b.i.d in clinics use. Our results suggest that fuzuloparib could well be tolerated when administered as a single 20 mg oral dose alone or co-administered with 400 mg fluconazole in healthy male subjects. It is recommended to avoid using moderate CYP3A4 inhibitors together with fuzuloparib or instead of 50 mg when necessary. |
| Author | Zhao, Jiao Zhang, Jin Deng, Jun Tang, Qi Li, Kunyan Heng, Jianfu Chen, Yong Wang, Jing Yang, Feng Chen, Xue |
| Author_xml | – sequence: 1 givenname: Xue orcidid: 0000-0002-4441-9159 surname: Chen fullname: Chen, Xue email: chenxue@hnca.org.cn organization: Early Clinical Trial Center, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University – sequence: 2 givenname: Feng surname: Yang fullname: Yang, Feng organization: Office of National Drug Clinical Trial Institution, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University – sequence: 3 givenname: Jiao surname: Zhao fullname: Zhao, Jiao organization: Early Clinical Trial Center, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University – sequence: 4 givenname: Qi surname: Tang fullname: Tang, Qi organization: Office of National Drug Clinical Trial Institution, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University – sequence: 5 givenname: Jianfu surname: Heng fullname: Heng, Jianfu organization: Office of National Drug Clinical Trial Institution, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University – sequence: 6 givenname: Jun surname: Deng fullname: Deng, Jun organization: Early Clinical Trial Center, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University – sequence: 7 givenname: Jin surname: Zhang fullname: Zhang, Jin organization: Early Clinical Trial Center, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University – sequence: 8 givenname: Yong surname: Chen fullname: Chen, Yong organization: Early Clinical Trial Center, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University – sequence: 9 givenname: Kunyan surname: Li fullname: Li, Kunyan organization: Office of National Drug Clinical Trial Institution, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University – sequence: 10 givenname: Jing surname: Wang fullname: Wang, Jing email: wangjing0081@hnca.org.cn organization: Early Clinical Trial Center, Hunan Cancer Hospital and The Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/34851444$$D View this record in MEDLINE/PubMed |
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| Cites_doi | 10.1038/nrc1457 10.1111/cas.13947 10.1186/bcr3670 10.1038/nature03445 10.1086/598327 10.1038/sj.clpt.6100054 10.1002/cpt.1103 10.1080/17425255.2021.1881480 10.1016/S0140-6736(10)60893-8 10.1007/s40265-021-01541-x 10.1111/bcp.14926 10.21147/j.issn.1000-9604.2020.03.08 10.1111/j.1365-2125.2011.04007.x |
| ContentType | Journal Article |
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| Keywords | Fluconazole CYP3A4 Drug–drug interaction (DDI) Fuzuloparib PARP inhibitor |
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Fuzuloparib (AiRuiYi
TM
, formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has... Fuzuloparib (AiRuiYi , formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has multiple... PurposeFuzuloparib (AiRuiYiTM, formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has... Fuzuloparib (AiRuiYiTM, formerly fluzoparib, SHR3162) is a new orally active poly adenosine diphosphate ribose polymerase (PARP) inhibitor. It has multiple... |
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