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Lubiprostone | CAS No: 136790-76-6 | GMP-certified suppliers
A medication that helps manage chronic idiopathic and opioid‑induced constipation and alleviates constipation symptoms in IBS‑C, supporting more regular and predictable bowel movements for adults.
Therapeutic categories
Alimentary Tract and MetabolismChloride Channel AgonistsDrugs for ConstipationDrugs that are Mainly Renally ExcretedFatty AcidsFatty Acids, Monounsaturated
Generic name
Lubiprostone
Molecule type
small molecule
CAS number
136790-76-6
DrugBank ID
DB01046
Approval status
Approved drug, Investigational drug
ATC code
A06AX03
Primary indications
- Lubiprostone is indicated for the treatment of adult patients with chronic idiopathic constipation, or opioid-induced constipation in patients with chronic non-cancer pain
- It is also indicated for the treatment of irritable bowel syndrome with constipation (IBS-C) in female patients ≥18 years old
Product Snapshot
- Lubiprostone is an oral small‑molecule API supplied in capsule formulations
- It is used for chronic idiopathic constipation, opioid‑induced constipation, and IBS‑C
- It is approved in the US and Canada, with additional investigational status in some markets
Clinical Overview
Lubiprostone (CAS 136790-76-6) is a prostaglandin E1 derivative indicated for chronic idiopathic constipation in adults, opioid‑induced constipation in adults with chronic non‑cancer pain, and irritable bowel syndrome with constipation in women aged 18 years and older. It is structurally characterized as a bicyclic fatty acid related to endogenous prostaglandins.
Its pharmacological activity is localized to the gastrointestinal tract. Lubiprostone selectively activates apical ClC‑2 chloride channels on intestinal epithelial cells, promoting chloride efflux into the lumen. This drives a paracellular movement of sodium to maintain electrical neutrality, followed by water influx to preserve isotonic conditions. The resulting increase in intestinal fluid facilitates improved motility, softer stool consistency, and more predictable spontaneous bowel movements. Restoration of epithelial tight‑junction integrity has also been observed in experimental systems, suggesting a potential contribution to barrier function.
Systemic exposure after oral administration is minimal, consistent with its local mechanism. Available evidence indicates rapid metabolism to inactive derivatives. Absorption, distribution, and elimination parameters are characterized by low bioavailability and predominant excretion of metabolites without prolonged systemic retention.
The safety profile typically reflects gastrointestinal pharmacology. Nausea is the most frequently reported adverse effect and may be dose related. Diarrhea, abdominal discomfort, and transient dyspnea have been observed. Clinically meaningful electrolyte disturbances are not expected because chloride secretion occurs without measurable serum sodium or potassium changes. Use requires caution in patients with suspected mechanical gastrointestinal obstruction.
Lubiprostone is marketed in several regions, with Amitiza being a widely recognized brand in the United States and other territories.
For API procurement, sourcing should prioritize suppliers with demonstrated control of stereochemistry, impurity profiles, and stability of the highly oxygenated fatty acid structure. Compliance with ICH quality expectations and confirmation of consistent polymorphic form are essential for formulation reproducibility and regulatory submissions.
Its pharmacological activity is localized to the gastrointestinal tract. Lubiprostone selectively activates apical ClC‑2 chloride channels on intestinal epithelial cells, promoting chloride efflux into the lumen. This drives a paracellular movement of sodium to maintain electrical neutrality, followed by water influx to preserve isotonic conditions. The resulting increase in intestinal fluid facilitates improved motility, softer stool consistency, and more predictable spontaneous bowel movements. Restoration of epithelial tight‑junction integrity has also been observed in experimental systems, suggesting a potential contribution to barrier function.
Systemic exposure after oral administration is minimal, consistent with its local mechanism. Available evidence indicates rapid metabolism to inactive derivatives. Absorption, distribution, and elimination parameters are characterized by low bioavailability and predominant excretion of metabolites without prolonged systemic retention.
The safety profile typically reflects gastrointestinal pharmacology. Nausea is the most frequently reported adverse effect and may be dose related. Diarrhea, abdominal discomfort, and transient dyspnea have been observed. Clinically meaningful electrolyte disturbances are not expected because chloride secretion occurs without measurable serum sodium or potassium changes. Use requires caution in patients with suspected mechanical gastrointestinal obstruction.
Lubiprostone is marketed in several regions, with Amitiza being a widely recognized brand in the United States and other territories.
For API procurement, sourcing should prioritize suppliers with demonstrated control of stereochemistry, impurity profiles, and stability of the highly oxygenated fatty acid structure. Compliance with ICH quality expectations and confirmation of consistent polymorphic form are essential for formulation reproducibility and regulatory submissions.
Identification & chemistry
| Generic name | Lubiprostone |
|---|---|
| Molecule type | Small molecule |
| CAS | 136790-76-6 |
| UNII | 7662KG2R6K |
| DrugBank ID | DB01046 |
Pharmacology
| Summary | Lubiprostone is a locally acting chloride channel activator that targets ClC‑2 channels on the apical intestinal epithelium. Channel activation increases chloride-driven fluid secretion into the lumen, which enhances intestinal motility and facilitates stool passage. Its activity remains localized to the gastrointestinal tract and may support mucosal barrier function through effects on tight‑junction integrity. |
|---|---|
| Mechanism of action | Lubiprostone acts by specifically activating ClC-2 chloride channels, which is a normal constituent of the apical membrane of the human intestine, in a protein kinase A action independent fashion. Activation of ClC-2 chloride channels causes an efflux of chloride ions into the lumen, which in turn leads to an efflux of sodium ions through a paracellular pathway to maintain isoelectric neutrality. As a result, water follows sodium into the lumen in order to maintain isotonic equilibrium, thereby increasing intestinal fluid secretion. By increasing intestinal fluid secretion, lubiprostone increases motility in the intestine, thereby increasing the passage of stool and alleviating symptoms associated with chronic idiopathic constipation. Activation of ClC-2 chloride channels may also stimulate the recovery of muscosal barrier function by restoring tight junction protein complexes in the intestine. Patch clamp cell studies in human cell lines have indicated that the majority of the beneficial biological activity of lubiprostone and its metabolites is observed only on the apical (luminal) portion of the gastrointestinal epithelium. |
| Pharmacodynamics | Chronic idiopathic constipation is generally defined by infrequent or difficult passage of stool. The signs and symptoms associated with chronic idiopathic constipation (i.e., abdominal pain or discomfort, bloating, straining, and hard or lumpy stools) may be the result of abnormal colonic motility that can delay the transit of intestinal contents and impede the evacuation of rectal contents. One approach to the treatment of chronic idiopathic constipation is the secretion of fluid into the abdominal lumen through the activation of chloride channels in the apical membrane of the gastrointestinal epithelium. Lubiprostone is a locally acting chloride channel activator that increases intestinal chloride and fluid secretion without altering sodium and potassium concentrations in the serum. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Chloride channel protein 2 | Humans | inducer |
ADME / PK
| Absorption | Lubiprostone has low systemic availability following oral administration and concentrations of lubiprostone in plasma are below the level of quantitation (10 pg/mL). |
|---|---|
| Half-life | 0.9 to 1.4 hours |
| Protein binding | 94% |
| Metabolism | The results of both human and animal studies indicate that lubiprostone is rapidly and extensively metabolized by 15-position reduction, α-chain β-oxidation, and ω-chain ω-oxidation. These biotransformations are not mediated by the hepatic cytochrome P450 system but rather appear to be mediated by the ubiquitously expressed carbonyl reductase. M3, a metabolite of lubiprostone in both humans and animals is formed by the reduction of the carbonyl group at the 15-hydroxy moiety that consists of both α-hydroxy and β-hydroxy epimers. M3 makes up less than 10% of the dose of radiolabeled lubiprostone. |
| Route of elimination | Peak plasma concentration was shown to be around 1.14 hours, with a majority of the drug excreted in the urine within 48 hours. Lubiprostone and M3 are only detected in trace amounts in human feces. |
Formulation & handling
- Oral small‑molecule prostaglandin analogue formulated primarily as soft‑gel or liquid‑filled capsules to accommodate low aqueous solubility and lipophilic character (LogP ~4.6).
- Low water solubility may require solubilizing excipients and protection from hydrolysis in aqueous environments during manufacturing and storage.
- Typically administered with food to mitigate GI intolerance, but no critical food‑dependent bioavailability constraints relevant to formulation design.
Regulatory status
| Lifecycle | Key U.S. patents for the API expired by September 2024, indicating the product is entering a late‑lifecycle phase. With commercialization limited to the United States and Canada, the market is expected to reflect a mature competitive environment. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Lubiprostone is supplied primarily by a single originator product supported by several packagers that handle distribution in regulated markets. Branded formulations are established mainly in the United States and Canada, with no listed presence in the EU. Most listed U.S. patents have expired or are nearing expiry, indicating that generic competition is likely already present or poised to expand. |
|---|
Safety
| Toxicity | In a definitive Phase 1 cardiac repolarization study, 51 patients were administered a single oral dose of 144 mcg of lubiprostone, which is 6 times the normal single administration dose. Thirty-nine (39) of the 51 patients experienced an adverse event. The adverse events reported in >1% of this group included the following: nausea (45.1%), vomiting (27.5%), diarrhea (25.5%), dizziness (17.6%), loose or watery stools (13.7%), headache (11.8%), retching (7.8%), abdominal pain (5.9%), flushing or hot flush (5.9%), dyspnea (3.9%), pallor (3.9%), stomach discomfort (3.9%), syncope (3.9%), upper abdominal pain (2.0%), anorexia (2.0%), asthenia (2.0%), chest discomfort (2.0%), dry mouth (2.0%), hyperhidrosis (2.0%), skin irritation (2.0%) and vasovagal episode (2.0%). |
|---|
High Level Warnings:
- High-dose exposure (144 mcg, sixfold typical single dose) was associated with a high incidence of gastrointestinal adverse events, notably nausea, vomiting, and diarrhea, indicating dose‑dependent GI intolerance
- Transient autonomic and neurologic effects such as dizziness, flushing, syncope, and vasovagal episodes occurred at low frequency, suggesting sensitivity to acute hemodynamic shifts under supratherapeutic conditions
- Occasional respiratory and dermal reactions (e
Lubiprostone is a type of Gastrointestinal Agents
Gastrointestinal Agents belong to the pharmaceutical API category that focuses on treating disorders and ailments related to the digestive system. These agents play a crucial role in addressing various gastrointestinal conditions, such as acid reflux, ulcers, irritable bowel syndrome (IBS), and inflammatory bowel disease (IBD).
One of the key types of gastrointestinal agents is proton pump inhibitors (PPIs), which work by reducing the production of stomach acid. PPIs help in treating conditions like gastroesophageal reflux disease (GERD) and peptic ulcers. Another essential class of agents is antacids, which neutralize excessive stomach acid, providing relief from heartburn and indigestion.
Gastrointestinal agents also include antispasmodics that alleviate abdominal cramps and spasms associated with conditions like IBS. These drugs work by relaxing the smooth muscles of the digestive tract. Additionally, there are drugs categorized as laxatives that aid in relieving constipation by promoting bowel movements.
Moreover, certain gastrointestinal agents act as antiemetics, effectively reducing nausea and vomiting. These drugs are particularly useful for patients undergoing chemotherapy or experiencing motion sickness.
Pharmaceutical companies develop and manufacture a wide range of gastrointestinal agents in various forms, including tablets, capsules, suspensions, and injections. These agents are typically formulated using active pharmaceutical ingredients (APIs) and other excipients to ensure their efficacy and safety.
In conclusion, gastrointestinal agents form a vital category of pharmaceutical APIs, providing relief from digestive disorders and improving overall gastrointestinal health. The availability of diverse agents catering to different conditions ensures that patients can receive targeted treatment for their specific gastrointestinal needs.
Lubiprostone API manufacturers & distributors
Compare qualified Lubiprostone API suppliers worldwide. We currently have 6 companies offering Lubiprostone API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF | 229 products |
| Chirogate International | Producer | Taiwan | Taiwan | CoA, FDA, GMP, KDMF, USDMF | 17 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Jiangxi Bioman Pharma Lim... | Producer | China | China | CoA | 15 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, USDMF, WC | 762 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
When sending a request, specify which Lubiprostone 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 Lubiprostone 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.
Frequently asked questions about Lubiprostone API
Sourcing
What matters most when sourcing GMP-grade Lubiprostone?
Key considerations include confirming GMP compliance and verifying that the supplier meets U.S. and Canadian regulatory requirements. Because supply is centered on a single originator with multiple packagers, assessing the reliability and continuity of the distribution chain is important. With most U.S. patents expired or nearing expiry, verifying the regulatory status of available generic sources is also essential.
Which documents are typically required when sourcing Lubiprostone API?
Request the core API documentation set: CoA (6 companies), USDMF (5 companies), GMP (4 companies), WC (2 companies), FDA (2 companies). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Lubiprostone API?
Known or reported manufacturers for Lubiprostone: Apino Pharma Co., Ltd., Sinoway industrial Co.,Ltd. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Lubiprostone API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Lubiprostone manufacturers?
Audit reports may be requested for Lubiprostone: 2 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Lubiprostone API on Pharmaoffer?
Reported supplier count for Lubiprostone: 6 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Lubiprostone API?
Production countries reported for Lubiprostone: China (3 producers), India (2 producers), Taiwan (1 producer). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Lubiprostone usually hold?
Common certifications for Lubiprostone suppliers: CoA (6 companies), USDMF (5 companies), GMP (4 companies), WC (2 companies), FDA (2 companies). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Lubiprostone (CAS 136790-76-6) used for?
Lubiprostone is used to treat chronic idiopathic constipation in adults, opioid‑induced constipation in adults with chronic non‑cancer pain, and irritable bowel syndrome with constipation in women aged 18 years and older. It increases intestinal fluid secretion and motility by activating ClC‑2 chloride channels on the apical surface of intestinal epithelial cells.
Which therapeutic class does Lubiprostone fall into?
Lubiprostone belongs to the following therapeutic categories: Alimentary Tract and Metabolism, Chloride Channel Agonists, Drugs for Constipation, Drugs that are Mainly Renally Excreted, Fatty Acids. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Lubiprostone mainly prescribed for?
The primary indications for Lubiprostone: Lubiprostone is indicated for the treatment of adult patients with chronic idiopathic constipation, or opioid-induced constipation in patients with chronic non-cancer pain, It is also indicated for the treatment of irritable bowel syndrome with constipation (IBS-C) in female patients ≥18 years old. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Lubiprostone work?
Lubiprostone acts by specifically activating ClC-2 chloride channels, which is a normal constituent of the apical membrane of the human intestine, in a protein kinase A action independent fashion. Activation of ClC-2 chloride channels causes an efflux of chloride ions into the lumen, which in turn leads to an efflux of sodium ions through a paracellular pathway to maintain isoelectric neutrality. As a result, water follows sodium into the lumen in order to maintain isotonic equilibrium, thereby increasing intestinal fluid secretion. By increasing intestinal fluid secretion, Lubiprostone increases motility in the intestine, thereby increasing the passage of stool and alleviating symptoms associated with chronic idiopathic constipation. Activation of ClC-2 chloride channels may also stimulate the recovery of muscosal barrier function by restoring tight junction protein complexes in the intestine. Patch clamp cell studies in human cell lines have indicated that the majority of the beneficial biological activity of Lubiprostone and its metabolites is observed only on the apical (luminal) portion of the gastrointestinal epithelium.
What should someone know about the safety or toxicity profile of Lubiprostone?
Lubiprostone’s safety profile is primarily gastrointestinal, with nausea, diarrhea, abdominal discomfort, and transient dyspnea occurring most commonly and often in a dose‑related manner. Supratherapeutic exposure has produced higher rates of nausea, vomiting, and diarrhea, along with infrequent autonomic or neurologic symptoms such as dizziness, flushing, syncope, or vasovagal episodes. Systemic toxicity is limited because absorption is minimal and electrolytes typically remain stable. Use requires caution when mechanical gastrointestinal obstruction is suspected.
What are important formulation and handling considerations for Lubiprostone as an API?
Lubiprostone’s low aqueous solubility and lipophilicity support use of soft‑gel or liquid‑filled capsule formats with appropriate solubilizing excipients. Formulations should minimize exposure to aqueous environments to reduce hydrolysis during manufacturing and storage. The API is rapidly metabolized and has low systemic availability, so handling should focus on maintaining chemical stability rather than controlling systemic exposure. No special food‑dependent formulation adjustments are required.
Is Lubiprostone a small molecule?
Lubiprostone is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Lubiprostone?
Lubiprostone’s low aqueous solubility and lipophilic character make it susceptible to hydrolysis in aqueous environments, so formulations typically use soft‑gel or liquid‑filled capsules to limit water exposure. Protection from moisture during manufacturing and storage is important to maintain stability. No additional food‑related stability concerns are noted for the oral product.
Regulatory
Where is Lubiprostone approved or in use globally?
Lubiprostone is reported as approved in the following major regions: US, Canada. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
What’s the regulatory and patent landscape for Lubiprostone right now?
Lubiprostone is authorized for use in the United States and Canada. In both jurisdictions, marketing and post‑approval activities follow standard regulatory requirements for approved prescription drugs. Patent status varies by jurisdiction and specific filings, and is typically determined through the relevant national patent offices and listed drug patent registries.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Lubiprostone procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Lubiprostone. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Lubiprostone included in the PRO Data Insights coverage?
PRO Data Insights coverage for Lubiprostone: 149 verified transactions across 56 suppliers and 50 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Lubiprostone?
Market report availability for Lubiprostone: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
