Drug intelligence / Profile preview

granisetron (Beecham Group)

Development stage
Approved
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous, Transdermal, Subcutaneous
01

Overview

Granisetron is a selective serotonin 5-HT3 receptor antagonist used primarily as an antiemetic to prevent and treat nausea and vomiting associated with cancer chemotherapy (including high-dose cisplatin), radiation therapy, and surgery. It works by blocking serotonin (5-HT) at 5-HT3 receptors in the gut and central nervous system—particularly on vagal nerve terminals—which reduces activation of the vomiting center in the medulla oblongata. Granisetron does not affect dopamine or muscarinic receptors. It is available as oral tablets/solution, intravenous injection/infusion, subcutaneous extended-release injection (Sustol), and a transdermal patch (Sancuso). Developed by Beecham in the mid-1980s and later produced by Roche under Kytril; other manufacturers include Kyowa Kirin for Sancuso. Approved since 1991–1994 globally; it is also available generically[1][2][3][4][5][6][7].

Brand names
KytrilSancusoSustolGranisol
Other names
granisetron hydrochloridegranisétrongranisetróngranisetronum
02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)

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