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The purpose of this study is to characterize the effect of rifampin (Part A) and itraconazole(Part B) on the single-dose pharmacokinetics (PK) of Larotinib in healthy adult participants.
The drug being tested in this study is called Larotinib (Z650). The study assessed the drug-drug interaction of Larotinib with either a strong cytochrome P-450 (CYP)3A inducer, rifampin (Part A) , or with a strong CYP3A inhibitor itraconazole (Part B) in healthy adult participants.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part A, Treatment Sequence(Larotinib-Larotinib/Rifampin) | Experimental | Larotinib , capsules (150mg*2+50mg*1), at Hour 0 on Day 1 followed by an overnight fast. On Days 15 to 26, participants received rifampin 600 mg as capsules, orally, once daily (QD) and Larotinib 350 mg as capsules, orally was coadministered on Day 20. There was a washout period of 13 days between the two treatments. |
|
| Part B, Treatment Sequence(Larotinib-Larotinib/itraconazole) | Experimental | Larotinib , capsules (150mg*2+50mg*1), at Hour 0 on Day 1 followed by an overnight fast. On Days 15 to Day 25, participants received itraconazole 200 mg solution, orally, once daily (QD) on Days 15 to Day 25 and a single oral dose of Larotinib 350 mg as capsule was coadministered on Day 19 (Treatment B). There was a washout period of 13 days between the two treatments. |
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| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Larotinib | Drug | Larotinib Capsules |
|
| Measure | Description | Time Frame |
|---|---|---|
| Cmax | Maximum Observed Plasma Concentration of Larotinib | Day 1 pre-dose at multiple time points (up to 192 hours) post-dose |
| AUC∞ | Area Under the Plasma Concentration-time Curve from Time 0 to Infinity, calculated using the observed value of the last quantifiable concentration for Larotinib | Day 1 pre-dose at multiple time points (up to 192 hours) post-dose |
| Measure | Description | Time Frame |
|---|---|---|
| AUClast | Area Under the Concentration-time Curve from Time 0 to the Time of the Last Quantifiable Concentration for Larotinib | Day 1 pre-dose at multiple time points (up to 192 hours) post-dose |
| Tmax |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Yanhua Ding | The First Hospital of Jilin University | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| First Hospital of Jilin University | Changchun | Jilin | 130000 | China |
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| ID | Term |
|---|---|
| D012293 | Rifampin |
| D017964 | Itraconazole |
| ID | Term |
|---|---|
| D012294 | Rifamycins |
| D006576 | Heterocyclic Compounds, 4 or More Rings |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D006571 | Heterocyclic Compounds |
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|
| Rifampin | Drug | Rifampin Capsules |
|
|
| Itraconazole | Drug | Itraconazole Capsules |
|
|
Time to Reach the Maximum Plasma Concentration (Cmax) for Larotinib
| Day 1 pre-dose at multiple time points (up to 192 hours) post-dose |
| D047029 | Lactams, Macrocyclic |
| D047028 | Macrocyclic Compounds |
| D011083 | Polycyclic Compounds |
| D014230 | Triazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D010879 | Piperazines |