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The primary objective of the study is to evaluate the effect of fluconazole on pharmacokinetics of pyrotinib tablet for oral administration in healthy Chinese adult subjects. The secondary objective of the study is to compare the safety of pyrotinib alone and co-administered with fluconazole.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Pyrotinib/Fluconazole | Experimental | Durg: Pyrotinib Durg: Pyrotinib/Fluconazole Participants received a single oral dose of pyrotinib 80 milligram (mg) on day1 and day9. Participants received a loading dose of fluconazole 400 mg on day6 followed by single dose of fluconazole 200 mg for oral administration from D7 to D18. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Pyrotinib;Fluconazole | Drug | Drug: Pyrotinib Participants received a single oral dose of Pyrotinib tablet on the morning of day1 in treatment period 1. Drug: Pyrotinib/Fluconazole In treatment period 2, Participants received a single oral dose of pyrotinib tablet on the morning of day9, and received a loading dose of fluconazole capsule on day6 followed by single dose of fluconazole for oral administration from D7 to D18. |
| Measure | Description | Time Frame |
|---|---|---|
| Maximum Observed Plasma Concentration (Cmax) of Pyrotinib | Pre-dose, and 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 168 (Combined with Fluconazole), 240 (Combined with Fluconazole) Hours Post-dose | |
| Area Under the Plasma Concentration-Time Curve from Time Zero to Last Measurable Concentration (AUC0-t) of Pyrotinib | Pre-dose, and 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 168 (Combined with Fluconazole), 240 (Combined with Fluconazole) Hours Post-dose | |
| Area Under the Plasma Concentration-Time Curve from Time Zero to Infinity (AUC0-Inf) of Pyrotinib | AUC0-inf was defined as the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). | Pre-dose, and 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 168 (Combined with Fluconazole), 240 (Combined with Fluconazole) Hours Post-dose |
| Measure | Description | Time Frame |
|---|---|---|
| The Time Take to Reach Cmax (Tmax) of Pyrotinib | Pre-dose, and 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 168 (Combined with Fluconazole), 240 (Combined with Fluconazole) Hours Post-dose | |
| Elimination Half Life (t1/2) of Pyrotinib | Elimination Half Life (t1/2) was defined as the time required for the concentration or amount of drug in the body to be reduced by one-half. |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Jinan Central Hospital | Jinan | Shandong | 250013 | China |
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Pyrotinib alone and then combination with fluconazole
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| Pre-dose, and 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 168 (Combined with Fluconazole), 240 (Combined with Fluconazole) Hours Post-dose |
| The Incidence and Severity of Adverse Events (AEs) or Serious Adverse Events (SAEs) in Participants | Baseline up to Day 28 |