In short
Granisetron hydrochloride is an antinauseant and antiemetic medicine used to prevent nausea and vomiting caused by chemotherapy. It is a selective 5-HT3 receptor antagonist available as tablets and solution for injection. One clinical trial in the EU registry is currently studying granisetron as a comparison treatment in adults with cancer, alongside other antiemetics, in a Phase 2 trial with 205 participants.
Granisetron hydrochloride is an antinauseant and antiemetic agent. It is a selective 5-hydroxytryptamine (5-HT3) receptor antagonist with little or no affinity for other serotonin receptors, adrenoreceptors, dopamine, histamine, benzodiazepine, or opioid receptors. It is available as film-coated tablets containing 1 mg or 2 mg granisetron, an oral solution, and a solution for injection.
Key points
- Granisetron hydrochloride is an antiemetic used to prevent chemotherapy-induced nausea and vomiting.
- It works by blocking 5-HT3 serotonin receptors in the gut and brain.
- One EU clinical trial lists granisetron as a comparator in a Phase 2 study of 205 adults with cancer.
- The trial measures complete response (no vomiting and no rescue medication) in the delayed phase of chemotherapy-induced nausea and vomiting.
- Granisetron is available as 1 mg and 2 mg tablets, oral solution, and solution for injection.
What is granisetron hydrochloride?
Granisetron hydrochloride is a medicine used to prevent nausea and vomiting, particularly that caused by chemotherapy. It belongs to a class of drugs called 5-HT3 receptor antagonists, also known as serotonin antagonists. The NHS dm+d browser lists granisetron hydrochloride as an active ingredient in five virtual medicinal products: 1 mg tablets, 2 mg tablets, a 200 micrograms/ml oral solution, and 1 mg/1 ml and 3 mg/3 ml solutions for injection. In the EU clinical trial registry, granisetron is used as a comparator treatment in a study of chemotherapy-induced nausea and vomiting.
How does granisetron hydrochloride work?
Serotonin receptors of the 5-HT3 type are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema in the brain. During chemotherapy that induces vomiting, mucosal enterochromaffin cells release serotonin, which stimulates these 5-HT3 receptors. This evokes vagal afferent discharge, inducing vomiting. Granisetron binds to 5-HT3 receptors and blocks serotonin stimulation, thereby preventing vomiting after emetogenic stimuli such as cisplatin. In animal studies, a single granisetron injection prevented vomiting due to high-dose cisplatin or arrested vomiting within 5 to 30 seconds. In most human studies, granisetron has had little effect on blood pressure, heart rate, or ECG.
Which conditions is it used or studied for?
- Chemotherapy-induced nausea and vomiting (CINV) — granisetron is used to prevent nausea and vomiting caused by chemotherapy. The EU trial studies this condition in adults with cancer.
- Nausea — listed as a condition in the EU trial, where granisetron serves as a comparator.
- Vomiting — also listed as a condition in the EU trial.
- Neoplasms — the trial population consists of adults with cancer.
How is granisetron hydrochloride given?
Granisetron hydrochloride is available in several pharmaceutical forms. Film-coated tablets contain 1 mg or 2 mg of granisetron and are taken by mouth. An oral solution is available at a concentration of 200 micrograms/ml. Solutions for injection are available in 1 mg/1 ml and 3 mg/3 ml ampoules for intravenous use. In the EU clinical trial, granisetron is given as a 2 mg oral dose.
What do the clinical trials show?
One trial in the EU Clinical Trials Information System involves granisetron hydrochloride. The Phase 2 trial (NCT07169851) is authorised and plans to enrol 205 adults with cancer. It compares LY3537021 in combination with other antiemetic treatments to placebo in combination with other antiemetic treatments. Granisetron is one of several antiemetics used in the trial, alongside palonosetron, aprepitant, dexamethasone, and ondansetron.
What is measured?
The primary outcome is the proportion of participants with a complete response (CR) in the delayed phase of chemotherapy-induced nausea and vomiting. Complete response is defined as no vomiting and no rescue medication.
Who can take part?
The trial enrols adults with cancer who are experiencing nausea and vomiting caused by chemotherapy. The study type is interventional.