General Information
Granisetron Impurities and Granisetron

Daicel Pharma offers worldwide delivery options for a custom synthesis of Granisetron impurities, including the impurity standard, 7-Methoxy Granisetron. The impurity plays a vital role in evaluating the purity and safety of Granisetron, an active pharmaceutical ingredient.

An indazole derivative, Granisetron [CAS: 109889-09-0], serves as a selective antagonist of the 5-HT3 receptor, effectively managing nausea and vomiting caused by cancer chemotherapy and radiotherapy. Acting as an antiemetic, Granisetron functions as a serotonin receptor antagonist. Its effectiveness in alleviating these symptoms has made it a widely prescribed medication in clinical practice.

Granisetron: Use and Commercial Availability  

Granisetron, available under brand names like Granisol, Kytril, Sancuso, and Sustol, is a medication to prevent nausea and vomiting. It is for individuals undergoing emetogenic cancer therapy, including high-dose cisplatin, post-operation, and radiation treatments. Additionally, Granisetron prevents nausea and vomiting during moderately or highly emetogenic chemotherapy, whether with or without cisplatin, for up to five consecutive days.

Granisetron Structure and Mechanism of Action

The chemical name of Granisetron is 1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide. Its chemical formula is C₁₈H₂₄N₄O, and its molecular weight is approximately 312.4 g/mol.

Granisetron is a 5-hydroxytryptamine3 (5-HT3) receptor antagonist which binds with serotonin receptors located on the vagal nerve terminals peripherally and centrally in the chemoreceptor zone.

Granisetron Impurities and Synthesis

Granisetron impurities can form during the synthesis¹, storage, or usage of the drug due to side reactions, incomplete reactions, or interactions with other compounds. Analytical methods such as HPLC, LC-MS, NMR, and IR spectroscopy help analyze and quantify these impurities. The control measures involve optimizing the synthetic process and purification steps and ensuring appropriate storage conditions to minimize impurity formation. Stability studies assess impurity profiles over time and establish expiration dates and storage recommendations. Compliance with regulatory guidelines, such as those set by ICH, is crucial for ensuring the quality and safety of Granisetron formulations. Effective impurity control measures contribute to maintaining the integrity of Granisetron as a pharmaceutical product.

Daicel Pharma strictly adheres to cGMP standards and operates an analytical facility synthesizing Granisetron impurity standard, 7-Methoxy Granisetron. We offer deuterium-labeled Granisetron standards, including 7-Hydroxy Granisetron-D3 and Granisetron-D3, essential for bioanalytical research and BA/BE studies. Our impurities include a detailed Certificate of Analysis (CoA) that provides a comprehensive characterization report. This report has data obtained through techniques, 1H NMR, 13C NMR, IR, MASS, and HPLC purity analysis². Upon request, we give additional data like 13C-DEPT. We can synthesize unknown Granisetron impurities or degradation products and labeled compounds. Each delivery has a comprehensive characterization report.