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Also known as Rolapitant - Oral, Rolapitant - IV, Varubi
Rolapitant · 6 trials · 1 indication
The primary objective of this study is to determine whether administration of rolapitant with granisetron and dexamethasone improves CINV in the delayed phase (\>24 to 120 hours) of CINV compared with administration of placebo with granisetron and dexamethasone in subjects receiving HEC. The primary outcome will be based on complete response (defined as no emetic episodes and no rescue medication) in the delayed phase (\>24 to 120 hours).
To evaluate the effect of Rolapitant on the PK of probe substrates
To evaluate the effect of Rolapitant on the PK of probe substrates
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
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.
| Arm | Type | Description |
|---|---|---|
| Rolapitant | EXPERIMENTAL | Day 1: Rolapitant (200 mg PO) + Granisetron (10 mcg/kg IV) + dexamethasone (20 mg PO) Days 2-4: Dexamethasone (8 mg PO) will be administered orally BID. |
| Placebo + Granisetron + Dexamethasone | PLACEBO_COMPARATOR | Day 1: Placebo + Granisetron (10 mcg/kg IV)+ dexamethasone (20 mg PO) Days 2-4: Dexamethasone (8 mg PO) will be administered orally BID. |
| Part A | EXPERIMENTAL | Rolapitant IV and Digoxin |
| Part B | EXPERIMENTAL | Rolapitant IV and Sulfasalazine |
| Part C | EXPERIMENTAL | Rolapitant IV and Cooperstown Cocktail |
| 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 | EXPERIMENTAL | Investigational Product: Rolapitant Dose 6 administered IV as a 30-minute infusion Dosage Form: 2 mg/mL solution |
| Rolapitant - Oral | EXPERIMENTAL | Investigational Product: Rolapitant Dose: 200 mg (4 x 50mg) Route of Administration: Oral Dosage Form: Capsule Dosing Condition: Fasted (10 hours overnight) |
| Rolapitant - IV | EXPERIMENTAL | Investigational Product: Rolapitant Dose: 185 mg Route of Administration: IV (30 minutes) Dosage Form: 2 mg/mL solution Dosing Condition: Fasted (10 hours overnight) |
| Name | Type | Description |
|---|---|---|
| Rolapitant | DRUG | (4 X 50 mg capsules) 200 mg PO |
| Granisetron | DRUG | 10 mcg/kg IV |
| dexamethasone | DRUG | 20 mg PO and 8 mg PO |
| Placebo | DRUG | (4 X 0 mg capsules) 0 mg PO |
| Digoxin | DRUG | P-gp substrate |
| Sulfasalazine | DRUG | BCRP substrate |
| Cooperstown Cocktail | DRUG | Midazolam, omeprazole, warfarin, caffeine, and dextromethorphan |
| Rolapitant - Oral | DRUG | Oral Treatment A Investigational Product: Rolapitant Dose: 200 mg (4 x 50 mg) Route of Administration: Oral Dosage Form: Capsule Dosing Condition: Fasted (10 hours overnight) |
| Rolapitant - IV | DRUG | IV Treatment B Investigational Product: Rolapitant Dose: 185 mg Route of Administration: IV (30 minutes) Dosage Form: 2 mg/mL solution Dosing Condition: Fasted (10 hours overnight) |
Inclusion Criteria: * 18 years of age or older, of either gender, and of any race * has never been treated with cisplatin and is to receive the first course of cisplatin-based chemotherapy (≥60 mg/m2) * Karnofsky performance score of ≥60 * Predicted life expectancy of ≥4 months * Adequate bone marr...
Rolapitant is used for the prevention of chemotherapy-induced nausea and vomiting (CINV). It is a small molecule developed for patients receiving emetogenic chemotherapy, including moderately emetogenic regimens. Clinical development has focused on this single indication across Phase 1 and Phase 3 studies.
Rolapitant targets TACR1, also known as the neurokinin-1 (NK1) receptor. It acts as an antagonist at this receptor. By blocking TACR1, rolapitant interferes with substance P signaling, a pathway involved in triggering nausea and vomiting after chemotherapy.
Rolapitant is developed by GSK plc, which trades under the ticker GSK. The company has sponsored the clinical trial program for the asset, including Phase 1 pharmacokinetic and bioequivalence studies and Phase 3 efficacy and safety studies in chemotherapy-induced nausea and vomiting.
Rolapitant has been studied in Phase 3 clinical development. Its Phase 3 program includes a safety and efficacy trial in patients receiving moderately emetogenic chemotherapy. The drug is investigational in this dataset, and the trials listed are completed rather than active.
Rolapitant has been evaluated in six completed trials. These include the Phase 3 study NCT01500226 in patients receiving moderately emetogenic chemotherapy, plus Phase 1 studies NCT02434861, NCT02382666, and NCT02285647 covering drug interaction, single ascending dose, and oral versus intravenous bioequivalence assessments.
Yes. Rolapitant - Oral refers to the oral formulation of rolapitant, the same active drug developed by GSK. The clinical program evaluated both oral and intravenous forms, including a bioequivalence study comparing oral and intravenous rolapitant in healthy volunteers.