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Alosetron | CAS No: 122852-42-0 | GMP-certified suppliers
A medication that treats severe diarrhea-predominant irritable bowel syndrome in women with chronic symptoms unresponsive to conventional therapies by modulating gastrointestinal function and visceral sensitivity.
Therapeutic categories
Primary indications
- Only for the treatment of symptoms of severe diarrhea-predominant irritable bowel syndrome (IBS) in women with chronic symptoms (generally lasting greater than 6 months) who does not present with anatomic or biochemical GI abnormalities and have not responded to conventional therapy
Product Snapshot
- Alosetron is an oral small molecule formulated as film-coated tablets
- It is indicated for the treatment of severe diarrhea-predominant irritable bowel syndrome in women with chronic symptoms unresponsive to conventional therapy
- The product has been approved and subsequently withdrawn in the US market
Clinical Overview
Pharmacologically, alosetron exerts its effect by blocking 5-HT3 receptors, which are ligand-gated nonselective cation channels predominantly located on enteric neurons within the gastrointestinal tract. Activation of these receptors modulates visceral pain, colonic motility, and gastrointestinal secretions—key processes implicated in the pathophysiology of IBS. By antagonizing 5-HT3 receptors, alosetron reduces neuronal depolarization related to serotonin signaling, thereby regulating bowel function and visceral sensitivity.
The compound belongs to the chemical class of n-alkylindoles, characterized by an indole core with an alkyl substituent at the 1-position. Alosetron undergoes metabolism primarily via cytochrome P450 enzymes, including CYP1A2, CYP2C9, CYP2E1, and CYP3A4 isoforms, both as a substrate and moderate inhibitor, which necessitates consideration of potential drug-drug interactions during co-administration with other CYP-metabolized agents.
Safety concerns are significant for alosetron due to risks of serious adverse events, including ischemic colitis, severely obstructed or ruptured bowel, and fatal outcomes. These risks led to a voluntary market withdrawal in 2000. After extensive evaluation, regulatory agencies such as the FDA allowed its reintroduction under restricted use programs with stringent prescribing guidelines to mitigate these safety issues.
Alosetron is marketed under limited access frameworks, reflecting a balance of clinical benefit against potential risks. For API procurement, sourcing must ensure compliance with established quality standards, considering the compound’s specialized indication and the critical nature of its safety profile. Rigorous batch validation, impurity profiling, and regulatory conformity are essential to support formulation development and subsequent regulatory submissions.
Identification & chemistry
| Generic name | Alosetron |
|---|---|
| Molecule type | Small molecule |
| CAS | 122852-42-0 |
| UNII | 13Z9HTH115 |
| DrugBank ID | DB00969 |
Pharmacology
| Summary | Alosetron is a selective antagonist of the 5-HT3 receptor, a nonselective cation channel located on enteric neurons involved in gastrointestinal function. By inhibiting 5-HT3 receptor activation, alosetron modulates visceral pain perception, colonic transit, and gastrointestinal secretions. This pharmacodynamic action targets dysregulated serotonin-sensitive pathways implicated in diarrhea-predominant irritable bowel syndrome (IBS). |
|---|---|
| Mechanism of action | Alosetron is a potent and selective 5-HT<sub>3</sub> receptor antagonist. 5-HT<sub>3</sub> receptors are nonselective cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit and gastrointestinal secretions, processes that relate to the pathophysiology of irritable bowel syndrome (IBS). 5-HT<sub>3</sub> receptor antagonists such as alosetron inhibit activation of non-selective cation channels which results in the modulation of serotonin-sensitive GI motor and sensory processes. |
| Pharmacodynamics | Alosetron is a potent and selective antagonist of the serotonin 5-HT<sub>3</sub> receptor type. Activation of these receptors and the resulting neuronal depolarization affects the regulation of visceral pain, colonic transit, and GI secretions processes that are related to IBS. By blocking these receptors, alosetron is able to effectively control IBS. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 3A | Humans | antagonist |
ADME / PK
| Absorption | 50-60 % |
|---|---|
| Half-life | 1.5 hours |
| Protein binding | 82% |
| Metabolism | Hepatic, via microsomal cytochrome P450 (CYP) |
| Route of elimination | Renal elimination of unchanged alosetron accounts for only 6% of the dose. Alosetron is extensively metabolized in humans. |
| Volume of distribution | * 65 to 95 L |
| Clearance | * 600 mL/min |
Formulation & handling
- Alosetron is a small molecule API formulated exclusively for oral administration typically as film-coated tablets.
- The compound exhibits moderate water solubility and a logP value of 1.21, indicating balanced lipophilicity for oral absorption.
- Its absorption profile is stable regardless of food intake, allowing flexible dosing with or without meals.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has patents that expired in the United States in 2013 and 2018, indicating a mature market with potential for generic competition. Its presence is primarily established in the US market. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Alosetron is primarily manufactured by Prometheus Laboratories Inc. and packaged by both Prometheus Laboratories Inc. and GlaxoSmithKline Inc., with its marketed products concentrated in the US. Patent data indicates exclusivity was maintained until at least 2018, suggesting that generic competition may now be present or emerging in the US market. There is no indication of branded products marketed in the EU or other regions. |
|---|
Alosetron is a type of 5HT3 antagonists
5HT3 antagonists are a subcategory of pharmaceutical APIs that play a crucial role in managing various conditions related to the serotonin neurotransmitter system. Serotonin, also known as 5-hydroxytryptamine (5HT), is a neurotransmitter that regulates various physiological functions, including mood, appetite, and gastrointestinal motility.
The 5HT3 antagonists work by selectively blocking the serotonin type 3 receptors in the central and peripheral nervous systems. By doing so, they inhibit the binding of serotonin to these receptors, thereby reducing its effects. This mechanism of action makes them effective in treating conditions such as chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome.
One of the commonly used 5HT3 antagonists is ondansetron, which is available in oral and injectable forms. It is widely prescribed to cancer patients undergoing chemotherapy to alleviate the distressing side effects of nausea and vomiting. Other notable 5HT3 antagonists include granisetron, palonosetron, and dolasetron.
These pharmaceutical APIs offer several advantages, including high selectivity for the 5HT3 receptors, rapid onset of action, and a favorable safety profile. They are typically well-tolerated by patients, with minimal adverse effects. However, healthcare professionals must consider individual patient factors and potential drug interactions when prescribing these medications.
In summary, 5HT3 antagonists are an important subcategory of pharmaceutical APIs that provide effective relief from nausea and vomiting associated with various medical conditions. Their targeted mechanism of action and favorable safety profile make them valuable tools in the management of these symptoms, benefiting patients and improving their overall quality of life.
Alosetron (5HT3 antagonists), classified under Antiemetics
Antiemetics are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) used to alleviate and prevent nausea and vomiting, also known as emesis. They play a vital role in managing these distressing symptoms, which can be caused by various factors such as chemotherapy, postoperative recovery, motion sickness, or gastrointestinal disorders.
Antiemetics work by targeting specific pathways in the body that trigger emesis. One common mechanism involves blocking dopamine receptors in the brain, as dopamine plays a significant role in triggering the vomiting reflex. This class of antiemetics is known as dopamine antagonists. Another mechanism involves inhibiting serotonin receptors, which are associated with nausea and vomiting. These agents, called serotonin antagonists, effectively reduce these symptoms.
In addition to dopamine and serotonin antagonists, other types of antiemetics include neurokinin-1 receptor antagonists, antihistamines, and anticholinergics. Each of these classes acts on different pathways in the body to provide relief from nausea and vomiting.
Pharmaceutical companies manufacture antiemetic APIs in accordance with strict quality control guidelines and regulations. These APIs serve as the active ingredients in various formulations, such as tablets, capsules, injections, or suppositories, designed to deliver the desired therapeutic effects.
Overall, antiemetic APIs form an essential category in the pharmaceutical industry, addressing the significant need for effective management of nausea and vomiting. Their development and availability greatly contribute to enhancing patient comfort and quality of life during various medical treatments and conditions.
Alosetron API manufacturers & distributors
Compare qualified Alosetron API suppliers worldwide. We currently have 4 companies offering Alosetron API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Biophore India | Producer | India | India | CoA, USDMF | 46 products |
| ChemCon GmbH | Producer | Germany | Germany | CoA, GMP, MSDS | 36 products |
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
When sending a request, specify which Alosetron API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Alosetron API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
