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The objective of this Open Label Study is to evaluate effects of Rolapitant IV solution, and its metabolite, on the pharmacokinetics (PK) of the P-gp substrate (digoxin), the BCRP substrate (sulfasalazine), and multiple cytochrome P450 (CYP) probe substrates in a healthy adult population.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Part A | Experimental | Rolapitant IV and Digoxin |
|
| Part B | Experimental | Rolapitant IV and Sulfasalazine |
|
| Part C | Experimental | Rolapitant IV and Cooperstown Cocktail |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Rolapitant | Drug |
| ||
| Digoxin |
| Measure | Description | Time Frame |
|---|---|---|
| AUC: area under the plasma concentration-time curve | To evaluate the effect of Rolapitant on the PK of probe substrates | Predose - up to 120 hours postdose |
| Cmax = observed maximum plasma concentration | To evaluate the effect of Rolapitant on the PK of probe substrates | Predose - up to 120 hours postdose |
| Measure | Description | Time Frame |
|---|---|---|
| Number of participants with adverse events | To evaluate the safety and tolerability of combination administration of the P-gp substrate (digoxin), the BCRP substrate (sulfasalazine), and CYP probe substrates (midazolam, omeprazole, warfarin, caffeine, and dextromethorphan [Cooperstown Cocktail]) with a single dose of rolapitant IV in a healthy adult population, as assessed by incidence and severity of AEs. |
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Main Inclusion Criteria:
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 Early Phase Unit | Baltimore | Maryland | 21225 | United States |
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| Drug |
P-gp substrate |
|
| Sulfasalazine | Drug | BCRP substrate |
|
| Cooperstown Cocktail | Drug | Midazolam, omeprazole, warfarin, caffeine, and dextromethorphan |
|
| 0 - 38 days |
| 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 |
| D004077 | Digoxin |
| D012460 | Sulfasalazine |
| ID | Term |
|---|---|
| D004071 | Digitalis Glycosides |
| D002298 | Cardenolides |
| D002301 | Cardiac Glycosides |
| D002297 | Cardanolides |
| D013256 | Steroids |
| D000072473 | Fused-Ring Compounds |
| D011083 | Polycyclic Compounds |
| D006027 | Glycosides |
| D002241 | Carbohydrates |
| D013449 | Sulfonamides |
| D000577 | Amides |
| D009930 | Organic Chemicals |
| D013450 | Sulfones |
| D013457 | Sulfur Compounds |
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