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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 chemotherapy-induced nausea and vomiting (CINV). It is a small molecule being developed by GSK plc (GSK) and is currently in Phase 3 clinical development as an investigational therapy for this condition.
Rolapitant is a small molecule that targets the neurokinin-1 (NK-1) receptor. By blocking this receptor, it helps prevent nausea and vomiting triggered by chemotherapy. This mechanism is central to its role in managing CINV.
Rolapitant is being developed by GSK plc, a global biopharmaceutical company listed on the stock exchange under the ticker GSK. GSK is advancing Rolapitant through clinical trials for chemotherapy-induced nausea and vomiting.
Rolapitant is in Phase 3 clinical development. It is an investigational drug, not yet approved, and is being studied for the prevention of chemotherapy-induced nausea and vomiting. All six clinical trials listed for Rolapitant have been completed.
Rolapitant has completed six clinical trials, including a Phase 3 study (NCT01499849) with 532 participants evaluating its safety and efficacy for CINV in patients receiving highly emetogenic chemotherapy. Other completed trials include Phase 1 studies on bioequivalence (NCT02285647), safety and pharmacokinetics (NCT02382666), and drug interactions (NCT02434861).
Rolapitant is a distinct drug with no alternative names provided. It is being studied specifically for chemotherapy-induced nausea and vomiting and is not known to be identical to any other marketed medication.