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7-Hydroxygranisetron is a chemical substance that belongs to the metabolic products or related derivatives of Granisetron. It is usually in the form of a gray white solid and may have limited solubility in water, but is easily soluble in certain organic solvents. As a metabolite or related derivative of granisetron, it may be used in drug development to study the metabolic pathways, pharmacological or toxicological properties of granisetron. In addition, it may also serve as a potential drug candidate for further research and development. In the field of chemical synthesis, it may also serve as an intermediate or starting material for the synthesis of other complex organic compounds. It should be stored in a dry, cool, well ventilated place, away from sources of fire and heat.
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Chemical Formula |
C18H24N4O2 |
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Exact Mass |
328 |
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Molecular Weight |
328 |
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m/z |
328 (100.0%), 329 (19.5%), 330 (1.8%), 329 (1.5%) |
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Elemental Analysis |
C, 65.83; H, 7.37; N, 17.06; O, 9.74 |
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7-Hydroxygranisetron, as an important chemical substance, has shown broad application prospects in drug development, chemical synthesis, and biomedical research. The following will elaborate on its specific uses and potential value from multiple dimensions:
Application in the field of drug development
7-Hydroxygranisetron is a key metabolite of Granisetron, a highly selective 5-hydroxytryptamine 3 (5-HT3) receptor antagonist widely used in clinical practice for the prevention and treatment of nausea and vomiting caused by radiation therapy and cytotoxic chemotherapy. For example, by studying the enzymatic reactions and intermediate products involved in its metabolism, it is possible to clarify how granisetron is metabolized into 7-Hydroxygranisetron in organs such as the liver.
This provides important theoretical basis for optimizing drug dosage and administration regimens. Understanding metabolic pathways can also help predict metabolic differences of drugs in different populations. Due to genetic factors, age, gender, disease status, and other factors, individuals may have differences in their ability to metabolize drugs. Studying its metabolic pathways can identify key factors that affect metabolism, providing guidance for personalized medication and avoiding adverse reactions or poor efficacy caused by abnormal drug metabolism.
Research on drug metabolites
Pharmacodynamics is the discipline that studies the absorption, distribution, metabolism, and excretion processes of drugs in the body. Studying its pharmacokinetic properties, such as absorption rate, distribution volume, metabolic rate, and excretion pathways, can provide a deeper understanding of its dynamic changes in vivo. For example, by measuring its concentration time curve in plasma, parameters such as half-life and clearance rate of the drug can be calculated, which are of great significance for determining the dosing interval and dose adjustment of the drug.
When granisetron is used in combination with other drugs, its metabolism may be affected by other drugs, or it may itself affect the metabolism of other drugs. By studying its pharmacokinetic properties, the risk of drug interactions can be predicted and evaluated, ensuring the safety and effectiveness of combination therapy.
Its molecular structure contains functional groups such as indazole rings and carboxylic acid groups, which have high reactivity in organic synthesis and provide the possibility for structural modification. A series of its derivatives can be synthesized by introducing or changing substituents on the indazole ring, or by esterifying or amidating carboxylic acid groups. The synthesized derivatives need to undergo activity screening to evaluate their antagonistic effects on 5-HT3 receptors or other potential pharmacological activities.
In vitro cell experiments can be used, such as measuring the effect of derivatives on the intracellular calcium ion concentration changes mediated by 5-HT3 receptors, to preliminarily screen for active compounds. Then, further in vivo animal experiments were conducted to verify the efficacy of the compound, such as observing its inhibitory effect on chemotherapy-induced animal vomiting models. By combining structural modification with activity screening, it is possible to develop novel antiemetic drugs or candidate drugs in other therapeutic fields.
Development of potential drug candidates
Further drug optimization is needed for the screened derivatives with potential activity. This includes improving its pharmacokinetic properties, such as increasing oral bioavailability, prolonging half-life, etc; Reduce its toxicity, such as minimizing damage to organs such as the liver and kidneys; And improve its selectivity, making it more specific to target receptors and reducing non-specific effects on other receptors. On the basis of drug optimization, comprehensive preclinical studies are needed. This includes pharmacological studies to further determine the effective dose range and maximum tolerated dose of compounds; Toxicological research, evaluating the acute toxicity, chronic toxicity, genetic toxicity, etc. of compounds to animals; And pharmacokinetic studies, studying its absorption, distribution, metabolism, and excretion processes in animal models closer to the human body.
Only through rigorous preclinical studies can compounds be demonstrated to have good safety, efficacy, and pharmacokinetic properties before entering the clinical trial phase.
Other potential applications
Application in biomarker research
Nausea and vomiting are common adverse reactions during chemotherapy. As a metabolite of granisetron, its level in the patient's body may be related to the severity of chemotherapy-induced nausea and vomiting. By detecting its concentration in biological samples such as blood and urine of patients, it can be used as an auxiliary diagnostic tool to assess the risk of nausea and vomiting in patients. For example, if a patient's concentration of granisetron is low before or during chemotherapy, it may indicate a weaker metabolic capacity for granisetron and a higher likelihood of nausea and vomiting, requiring adjustments to the dosage or regimen of prophylactic medication.
In addition to chemotherapy related adverse reactions, the potential diagnostic value of 7-Hydroxygranisetron in other diseases is also worth exploring. For example, in some neurological or gastrointestinal diseases, the function of 5-HT3 receptors may be altered, and 7-Hydroxygranisetron is associated with 5-HT3 receptors, so its levels in patients with these diseases may also change. Through large-scale clinical studies, the feasibility and accuracy of using it as a diagnostic biomarker for these diseases can be further validated.
Application in biomarker research
The correlation between chemotherapy efficacy and prognosis: During chemotherapy treatment, the prognosis of patients is related to multiple factors, among which the control of chemotherapy related adverse reactions is an important aspect. Its level can reflect the control effect of granisetron on chemotherapy-induced nausea and vomiting. If the patient's level of granisetron can be maintained within an effective range after use, it may indicate that chemotherapy related adverse reactions have been well controlled, and the patient's prognosis may be relatively good. On the contrary, if its level is abnormal, it may indicate poor control of chemotherapy related adverse reactions and require further adjustment of treatment plans, which may have adverse effects on the patient's prognosis.
Long term follow-up studies can further explore the relationship between 7-Hydroxygranisetron and long-term survival rates of patients. If certain characteristics of 7-Hydroxygranisetron (such as concentration trends, combined detection results with other biomarkers, etc.) are found to be associated with long-term survival rates in patients, it can serve as a prognostic biomarker to help doctors develop more personalized treatment and follow-up plans.
In the production process of granisetron, 7-Hydroxygranisetron may exist as an impurity. In order to ensure the quality and safety of granisetron drugs, it is necessary to strictly control the impurities of 7-Hydroxygranisetron. By establishing effective detection methods such as high-performance liquid chromatography (HPLC), the content of 7-Hydroxygranisetron impurity in granisetron preparations can be accurately determined. At the same time, establish reasonable impurity limit standards to ensure that the impurity content in drugs is within a safe range.
In depth research on the sources and mechanisms of impurities in 7-Hydroxygranisetron can help optimize the production process of granisetron. For example, by analyzing various links in the production process, identifying factors that may lead to the production of 7-Hydroxygranisetron impurities, such as reaction conditions, raw material purity, etc., and then taking corresponding measures to improve, reduce the production of impurities, and improve the quality of drugs.
Drug stability research
During the storage and use of drugs, degradation reactions may occur, producing various degradation products. 7-Hydroxygranisetron may be one of the degradation products of granisetron under certain conditions. By studying the stability of granisetron under different storage conditions such as temperature, humidity, and light, and analyzing the production of degradation products such as 7-Hydroxygranisetron, the shelf life of the drug and appropriate storage conditions can be determined.
In order to accurately monitor the quality changes of drugs during storage, it is necessary to develop stability indicator methods. These methods should be able to specifically detect drugs and their degradation products, including 7-Hydroxygranisetron. By establishing appropriate analytical methods, quality issues of drugs can be identified in a timely manner, ensuring the safety and effectiveness of the drugs used by patients.
Due to the existence of genetic polymorphism, there may be differences in drug metabolism ability among different individuals. Its metabolic process may be influenced by certain genes. Studying the relationship between gene polymorphism and 7-Hydroxygranisetron metabolism can provide a basis for personalized medication. For example, if a mutation in a certain gene locus is found to slow down the metabolic rate of 7-Hydroxygranisetron, patients carrying the mutation gene may need to adjust the dosage of granisetron to avoid adverse reactions caused by drug accumulation in the body.
Optimization of drug formulation
Granisetron has different dosage forms, such as injections, oral preparations, etc. There may be differences in the absorption, distribution, metabolism, and excretion processes of different dosage forms in the body. By studying the metabolism of 7-Hydroxygranisetron in different formulations, the advantages and disadvantages of different formulations can be compared, providing a basis for optimizing drug formulations. For example, if it is found that the production rate of 7-Hydroxygranisetron in a certain oral formulation is slow, it may indicate that there are some problems with the absorption or metabolism process of the formulation and further improvement is needed.
adverse reaction
Hydroxygranisetron (usually referring to granisetron and its active metabolites or similar structural drugs) is a highly selective 5-HT ∝ receptor antagonist mainly used for the prevention and treatment of nausea and vomiting caused by radiotherapy, chemotherapy, and surgery. Although it has high selectivity and no adverse reactions such as extrapyramidal reactions or excessive sedation, it may still cause a series of adverse reactions in clinical applications.
Common adverse reactions
Digestive system response
Constipation is one of the most common digestive system adverse reactions to granisetron drugs. This may be related to the inhibition of intestinal 5-HT receptors by drugs, reducing intestinal peristalsis. The incidence of constipation varies in different studies, but is generally higher. For example, in controlled clinical trials, the incidence of constipation in patients treated with granisetron tablets can reach 18% -14%, while in patients treated with granisetron injection, the incidence of constipation is about 3%.
Digestive system response
Diarrhea is also one of the possible adverse reactions caused by granisetron drugs. Its incidence is relatively low, but it may still occur in some patients. For example, in patients receiving treatment with granisetron tablets, the incidence of diarrhea is approximately 8% -9%. Some patients may experience symptoms of abdominal pain or indigestion after using granisetron drugs. These symptoms are usually mild and can mostly resolve on their own.
Neurological response
Headache: Headache is a common neurological adverse reaction of granisetron drugs. Its incidence varies in different studies, but it is generally higher. For example, in patients treated with granisetron tablets, the incidence of headaches can reach 21% -20%, while in patients treated with granisetron injection, the incidence of headaches is about 14%. Headaches are usually mild to moderate, and most can be relieved on their own.
Weakness and drowsiness: Some patients may experience symptoms of weakness or drowsiness after using granisetron drugs. These symptoms are usually mild and do not affect the patient's daily life. However, caution should be exercised when using such medications for patients who need to drive or operate machinery.
Other reactions
Fever: A small number of patients may experience fever symptoms after using granisetron drugs. This may be related to the immune or inflammatory response caused by the medication. Fever is usually low-grade and can mostly alleviate on its own.
Injection site reaction: For patients receiving treatment with granisetron injection, there may be pain, redness, swelling, or hardening at the injection site. These reactions are usually mild and most of them can alleviate on their own.
Origin: Based on the R&D Background of Granisetron
7‑Hydroxygranisetron is not a newly synthesized lead compound, but a key Phase I metabolite of granisetron, a 5‑hydroxytryptamine 3 (5‑HT₃) receptor antagonist. Granisetron was developed by SmithKline Beecham in the 1980s and approved by the FDA in 1991 for chemotherapy‑induced nausea and vomiting. Its molecular structure contains an indole ring and an azabicyclic moiety, which provide the structural basis for hydroxylation metabolism.
Discovery: First Identification in Metabolic Studies
In the early 1990s, during the preclinical and early clinical pharmacokinetic studies of granisetron, researchers detected this hydroxylated metabolite for the first time in human liver microsome incubation systems, as well as in urine and plasma from healthy volunteers, using high‑performance liquid chromatography–mass spectrometry (HPLC‑MS).Studies confirmed that granisetron is oxidized and hydroxylated at the 7‑position of the indole ring by hepatic cytochrome P450 3A4 (CYP3A4) to form 7‑hydroxygranisetron, which represents one of its major metabolic pathways in vivo.
Positioning: From Metabolite to Research Target
In the mid‑1990s, with deeper research into the relationship between drug metabolism and pharmacological activity, the therapeutic value of 7‑hydroxygranisetron was gradually established.In vitro receptor binding assays demonstrated that it still exhibits antagonistic activity at the 5‑HT₃ receptor. Although its binding affinity is slightly lower than that of the parent drug, it contributes synergistically to the antiemetic effect in vivo.Since then, this metabolite has become a key biomarker in studies of granisetron bioequivalence, drug–drug interactions, and pharmacokinetics in special populations. It also provides an important model for metabolism‑guided optimization of 5‑HT₃ receptor antagonists.
FAQ
What is the drug granisetron used for?
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Description. Granisetron injection is used to prevent nausea and vomiting that may occur after treatment with cancer medicines (chemotherapy or radiation), including high-dose cisplatin. This medicine is also used to prevent and treat nausea and vomiting that may happen after surgery.
What is the generic name for granisetron?
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What Is Kytril? Kytril (granisetron hydrochloride) is an antinauseant and antiemetic drug used to prevent nausea and vomiting caused by cancer chemotherapy or radiation therapy, and anesthesia used during surgery.
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