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Palonosetron | CAS No: 135729-56-5 | GMP-certified suppliers
A medication that helps prevent acute and delayed nausea and vomiting associated with cancer chemotherapy and provides short‑term prevention of postoperative nausea and vomiting.
Therapeutic categories
Primary indications
- For the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy, as well as prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy
- Also used for the prevention of postoperative nausea and vomiting for up to 24 hours post operation
Product Snapshot
- Palonosetron is an oral and intravenous small‑molecule antiemetic supplied in capsules and injectable solutions
- It is used for prevention of acute and delayed chemotherapy-induced nausea and vomiting and for postoperative nausea and vomiting
- It is approved in the US, Canada, and EU, with some investigational status in additional indications
Clinical Overview
Its pharmacology is defined by high‑affinity, selective blockade of 5‑HT3 receptors located in the gastrointestinal tract and central nervous system. By inhibiting receptor activation on vagal afferent nerves and within the area postrema and chemoreceptor trigger zone, palonosetron disrupts signaling pathways that initiate the emetic response following serotonin release from enterochromaffin cells during chemotherapy‑related mucosal injury. Its prolonged plasma half‑life and receptor interactions are considered contributory to activity observed in delayed phases of chemotherapy‑induced nausea and vomiting.
Palonosetron displays linear pharmacokinetics over therapeutic ranges. After intravenous administration, it distributes extensively with a large apparent volume of distribution and exhibits moderate plasma protein binding. Elimination occurs through both renal excretion and hepatic metabolism, involving CYP2D6, CYP3A, and CYP1A2 pathways, with a significant fraction excreted unchanged in urine. A terminal elimination half‑life of approximately 40 hours supports once‑per‑cycle dosing in chemotherapy settings.
Safety considerations include typical class‑related adverse effects such as headache and constipation. As a serotonergic agent, it may contribute to serotonin syndrome when combined with other serotonergic drugs. No pronounced QT‑prolonging effect has been consistently observed at approved doses, but caution is advised in patients with underlying risk factors or when coadministered with QT‑prolonging agents.
For API procurement, sourcing should emphasize control of stereochemistry, impurity profiling consistent with regulatory expectations, and verification of compliance with regional pharmacopeial or dossier requirements to support formulation development and global regulatory submissions.
Identification & chemistry
| Generic name | Palonosetron |
|---|---|
| Molecule type | Small molecule |
| CAS | 135729-56-5 |
| UNII | 5D06587D6R |
| DrugBank ID | DB00377 |
Pharmacology
| Summary | Palonosetron is a selective 5‑HT3 receptor antagonist that blocks serotonin-mediated activation of vagal and central pathways involved in the emetic response. By inhibiting 5‑HT3 receptors in the gastrointestinal tract and area postrema, it reduces afferent signaling to the vomiting center during chemotherapy‑ or surgery‑related serotonin release. Its high receptor affinity and prolonged activity contribute to effects observed in both acute and delayed emesis. |
|---|---|
| Mechanism of action | Palonosetron is a selective serotonin 5-HT<sub>3</sub> receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT<sub>3</sub> receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT<sub>3</sub> receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. Alternative mechanisms appear to be primarily responsible for delayed nausea and vomiting induced by emetogenic chemotherapy, since similar temporal relationships between between serotonin and emesis beyond the first day after a dose have not been established, and 5-HT<sub>3</sub> receptor antagonists generally have not appeared to be effective alone in preventing or ameliorating delayed effects. It has been hypothesized that palonosetron's potency and long plasma half-life may contribute to its observed efficacy in preventing delayed nausea and vomiting caused by moderately emetogenic cancer chemotherapy. |
| Pharmacodynamics | Palonosetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Palonosetron is a highly specific and selective serotonin 5-HT<sub>3</sub> receptor antagonist that is pharmacologically related to other 5-HT<sub>3</sub> receptor antagonists, but differs structurally. Palonosetron has a high affinity for 5-HT<sub>3</sub> receptors, but has little to no affinity for other receptors. The serontonin 5-HT<sub>3</sub> receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. It is suggested that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 3A | Humans | antagonist |
ADME / PK
| Absorption | Low oral bioavailability. |
|---|---|
| Half-life | Approximately 40 hours |
| Protein binding | 62% |
| Metabolism | Hepatic (50%), primarily CYP2D6-mediated, although CYP3A4 and CYP1A2 are also involved. |
| Route of elimination | After a single intravenous dose of 10 mcg/kg [14C]-palonosetron, approximately 80% of the dose was recovered within 144 hours in the urine |
| Volume of distribution | * 8.3 ± 2.5 L/kg |
| Clearance | * 160 +/- 35 mL/h/kg |
Formulation & handling
- Suitable for both oral capsules and sterile IV solutions; moderate water solubility and small‑molecule properties support conventional excipient systems for each route.
- For IV formulations, solution stability and control of pH and oxidative degradation are typical considerations for maintaining clarity and potency.
- Oral products are not food‑sensitive, allowing flexible administration and straightforward capsule or liquid‑filled capsule design.
Regulatory status
| Lifecycle | With key U.S. patents expiring in July 2024, the API is transitioning from protected to post‑exclusivity status. Given its presence in the US, Canada, and EU, the product is moving toward a mature, potentially more competitive market phase across major regions. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Palonosetron appears to have a single originator manufacturer, with multiple contract packagers supporting commercial distribution. Branded products are established across the US, Canada, and the EU, indicating broad international market presence. With key US patents expiring in mid‑2024, the product is entering a period in which generic competition may emerge or expand. |
|---|
Safety
| Toxicity | A single intravenous dose of palonosetron at 30 mg/kg (947 and 474 times the human dose for rats and mice, respectively, based on body surface area) was lethal to rats and mice. The major signs of toxicity were convulsions, gasping, pallor, cyanosis and collapse. |
|---|
- High-dose exposure has demonstrated acute lethality in rodents, with prominent neuro‑respiratory toxicity including convulsions, gasping, pallor, cyanosis, and collapse
- Handle and formulate to minimize risk of concentrated or accidental intravenous exposure, as toxicity escalates sharply at supratherapeutic levels
- Monitoring for signs of CNS excitation may be warranted in high‑intensity manufacturing or research settings where aerosolization or accidental injection could occur
Palonosetron 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.
Palonosetron (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.
Palonosetron API manufacturers & distributors
Compare qualified Palonosetron API suppliers worldwide. We currently have 10 companies offering Palonosetron API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| ALP PHARM | Producer | China | China | CoA, USDMF | 33 products |
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, KDMF, MSDS, USDMF, WC | 170 products |
| Emcure Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 80 products |
| Helsinn Advanced Synthesi... | Producer | Switzerland | Switzerland | CoA, JDMF | 3 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Rolabo Outsourcing | Producer | Spain | Spain | CoA, USDMF | 11 products |
| Tianjin Pharmacn Medical ... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 66 products |
| USV | Producer | India | India | CoA, USDMF | 35 products |
| Yangtze River Pharmaceuti... | Producer | China | China | CoA, GMP, ISO14001 | 34 products |
When sending a request, specify which Palonosetron 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 Palonosetron 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.
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