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The purpose of this study is to assess the safety and tolerability of single increasing doses of intravenously administered rolapitant in healthy male and female subjects.
Part 1 of the study is designed to evaluate the safety and tolerability of a SAD, up to 6 cohorts,of rolapitant IV (2 mg/mL solution) administered as an IV infusion over 30 minutes.
In Part 2 of the study, the safety and tolerability of the highest safe and well-tolerated dose established in Part 1 will be evaluated in an expanded cohort. The highest safe and well-tolerated dose established in Part 1 will be ascertained by the following criteria: an upper limit of 90% confidence interval (CI) for Cmax. A minimum of 40 subjects will be enrolled in Part 2.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Rolapitant Cohort 1 | Experimental | Investigational Product: Rolapitant Dose 1 administered IV as a 30-minute infusion Dosage Form: 2 mg/mL solution |
|
| Rolapitant Cohort 2 | Experimental | Investigational Product: Rolapitant Dose 2 administered IV as a 30-minute infusion Dosage Form: 2 mg/mL solution |
|
| Rolapitant Cohort 3 | Experimental | Investigational Product: Rolapitant Dose 3 administered IV as a 30-minute infusion Dosage Form: 2 mg/mL solution |
|
| Rolapitant Cohort 4 | Experimental | Investigational Product: Rolapitant Dose 4 administered IV as a 30-minute infusion Dosage Form: 2 mg/mL solution |
|
| Rolapitant Cohort 5 | Experimental | Investigational Product: Rolapitant Dose 5 administered IV as a 30-minute infusion Dosage Form: 2 mg/mL solution |
|
| Rolapitant Cohort 6 |
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Rolapitant | Drug |
|
| Measure | Description | Time Frame |
|---|---|---|
| Part 1 Dose Escalation: Safety and Tolerability (adverse events) | To evaluate the safety and tolerability of rolapitant IV (30 minutes infusion) in healthy adult volunteers as assessed by the incidence and severity of AEs | 0-30 days after administration of study drug |
| Part 2 Dose Treatment: Safety and Tolerability (adverse events) | To evaluate the safety and tolerability of rolapitant IV (30 minutes infusion) to an expanded cohort of healthy adult volunteers at the highest safe and well-tolerated dose established in Part 1 as assessed by the incidence and severity of AEs. | : 0-30 days after administration of study drug |
| Measure | Description | Time Frame |
|---|---|---|
| 1. AUC0-last: area under the plasma concentration-time curve from time 0 to the time of the last quantifiable concentration | 0-21 days | |
| 2. Cmax = observed maximum plasma concentration | 0-21 days |
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Main Inclusion Criteria:
Subject must be a healthy male or female aged 18 to 55 years at Screening
A female subject must have a negative pregnancy test at Screening and on Day -1.
A female subject of childbearing potential must agree to use an accepted method of birth control (excluding hormonal birth control methods) from Screening through 30 days after final study drug administration.
Subject must have a body mass index (BMI) from 18.5 to 32.0 kg/m2 and a weight of
≥ 50 kg at Screening.
Subject must be able to provide informed consent after risks and benefits have been explained. Subject must also be willing and able to comply with the protocol requirements.
Subject must be in general good health as determined by the Investigator based on pre-study medical, medication, and surgical history; physical examination; and clinical laboratory tests.
Main Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Dennis Vargo, MD | Tesaro, Inc. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Parexel | Baltimore | Maryland | 21225 | United States |
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| Experimental |
Investigational Product: Rolapitant Dose 6 administered IV as a 30-minute infusion Dosage Form: 2 mg/mL solution |
|
| ID | Term |
|---|---|
| D014839 | Vomiting |
| ID | Term |
|---|---|
| D012817 | Signs and Symptoms, Digestive |
| D012816 | Signs and Symptoms |
| D013568 | Pathological Conditions, Signs and Symptoms |
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| ID | Term |
|---|---|
| C578834 | rolapitant |
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