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- Antiemetics
- 5HT3 antagonists
- Cilansetron
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Cilansetron | CAS No: 120635-74-7 | GMP-certified suppliers
A medication that targets irritable bowel syndrome symptoms by modulating gastrointestinal function and visceral pain through serotonin receptor antagonism.
Therapeutic categories
Primary indications
- For the treatment of symptoms associated with irritable bowel syndrome
Product Snapshot
- Cilansetron is an oral small molecule formulation
- It is primarily indicated for the treatment of symptoms associated with irritable bowel syndrome
- Cilansetron is currently in the investigational stage and has not received regulatory approval
Clinical Overview
Pharmacodynamically, cilansetron acts by selectively and potently blocking 5-HT3 receptors, which are nonselective cation channels localized extensively on enteric neurons of the gastrointestinal tract, as well as in certain peripheral and central nervous system sites. The activation of these receptors modulates key physiological processes such as visceral pain sensation, colonic motility, and gastrointestinal secretions. By antagonizing 5-HT3 receptor activity, cilansetron modulates the enteric nervous system function, potentially alleviating IBS-related symptoms.
Cilansetron is administered orally. While comprehensive absorption, distribution, metabolism, and excretion (ADME) parameters have not been fully disclosed, the oral route aligns with targeting the gastrointestinal tract. The compound’s metabolism and clearance profiles remain under investigation within ongoing clinical trials.
Safety assessments have been central to cilansetron's clinical development due to historical concerns with alosetron, another 5-HT3 antagonist withdrawn from the market over safety issues. Phase III studies of cilansetron were temporarily suspended to reassess its safety profile in this context but have since recommenced. As of mid-2000s, the sponsoring company was reviewing the development priority for this molecule.
Cilansetron remains investigational, without current regulatory approvals or marketed formulations. It is of interest within categories encompassing drugs for functional gastrointestinal disorders, serotonin receptor antagonists, and agents impacting alimentary tract and metabolism.
For API sourcing, ensuring pharmaceutical-grade purity and consistent quality is essential, particularly given the structural complexity characteristic of carbazole derivatives. Reliable suppliers with validated synthetic routes and stringent quality control measures are critical for supporting clinical development and potential regulatory submission.
Identification & chemistry
| Generic name | Cilansetron |
|---|---|
| Molecule type | Small molecule |
| CAS | 120635-74-7 |
| UNII | 2J6DQ1U5B5 |
| DrugBank ID | DB04885 |
Pharmacology
| Summary | Cilansetron is a selective antagonist of the 5-HT3 receptor, primarily targeting 5-hydroxytryptamine receptor 3A subunits located on enteric neurons. By inhibiting 5-HT3 receptor-mediated cation channel activation, it modulates enteric nervous system activity involved in visceral pain, colonic transit, and gastrointestinal secretions. This pharmacological profile supports its therapeutic intent in managing symptoms associated with irritable bowel syndrome. |
|---|---|
| Mechanism of action | Cilansetron 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 cilansetron inhibit activation of non-selective cation channels which results in the modulation of the enteric nervous system. |
| Pharmacodynamics | Cilansetron is an orally formulated medication that blocks the action of 5-hydroxy-tryptamine 3 (5-HT3) receptors. Phase III studies of cilansetron had been suspended by Solvay in order to assess whether the drug possesses safety concerns similar to alosetron. Alosetron, also a 5-HT3 antagonist, was withdrawn from the market due to questions regarding its safety. Phase III testing with cilansetron has since resumed. In June 2005 the company announced that they were reviewing the priority of the cilansetron program. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 3A | Humans |
ADME / PK
| Absorption | Rapidly absorbed orally with a bioavailability of greater than 80% in rats. |
|---|---|
| Half-life | The elimination half-life after 4- and 8-mg oral doses administered 3 times daily for 6 days was reported to be 1.6 to 1.9 hours. |
Formulation & handling
- Cilansetron is a small molecule suitable for oral formulations due to its moderate water solubility and LogP profile.
- The compound's carbazole structure suggests potential photostability concerns; handling and storage in light-protected conditions are recommended.
- Low aqueous solubility may require solubilization strategies to optimize bioavailability in formulation development.
Regulatory status
Cilansetron 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.
Cilansetron (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.
