Drug intelligence / Profile preview

rolapitant + granisetron + dexamethasone

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**rolapitant + granisetron + dexamethasone** is a three-drug combination regimen used for the prevention of chemotherapy-induced nausea and vomiting (CINV), particularly in patients receiving highly or moderately emetogenic chemotherapy such as cisplatin-based regimens. - **Rolapitant** is a selective and competitive antagonist of the neurokinin-1 (NK-1) receptor, which blocks the action of substance P, a key mediator of emesis in the central and peripheral nervous systems[4][6]. - **Granisetron** is a selective antagonist of the serotonin 5-HT3 receptor, which blocks serotonin-mediated vomiting pathways in the gastrointestinal tract and central nervous system[3][4]. - **Dexamethasone** is a synthetic glucocorticoid corticosteroid that reduces inflammatory responses and contributes to antiemetic efficacy, though its precise antiemetic mechanisms are multifactorial and still not completely understood[3][4]. The combination (one-time oral rolapitant, intravenous or oral granisetron, and oral dexamethasone) has demonstrated superior efficacy versus granisetron plus dexamethasone alone in randomized phase III trials, with higher rates of complete response (no emesis and no need for rescue medication), especially in the delayed phase (24–120 hours after chemotherapy)[1][4][6][7]. The regimen is typically administered prior to chemotherapy, with continuing dexamethasone dosing for several days post-chemotherapy. This combination is mainly developed and studied for improving CINV prevention in cancer patients undergoing highly emetogenic chemotherapy[2][4][6][7].

02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)GR (Glucocorticoid receptor)TACR1 (Neurokinin‑1 Receptor)

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