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Alvimopan | CAS No: 156053-89-3 | GMP-certified suppliers
A medication that accelerates gastrointestinal recovery after bowel resection surgery and reduces postoperative ileus duration, supporting improved patient outcomes in gastrointestinal care.
Therapeutic categories
Primary indications
- Used to accelerate the time to upper and lower gastrointestinal recovery following partial large or small bowel resection surgery with primary anastomosis
- Also investigated for use in the treatment of pain (acute or chronic)
Product Snapshot
- Alvimopan is an oral small molecule formulated as capsules
- It is primarily used to accelerate gastrointestinal recovery following bowel resection surgery and has investigational use in pain management
- The product is approved for use in the US market and remains investigational for additional indications
Clinical Overview
Pharmacologically, alvimopan belongs to the class of hybrid peptides, compounds composed of two or more different amino acid types linked via peptide bonds. Its mechanism of action involves competitive binding to peripheral μ-opioid receptors predominantly within the gastrointestinal tract. Unlike other peripheral opioid antagonists such as methylnaltrexone, whose peripheral selectivity arises from ionic charge, alvimopan’s selective action is attributed to its unique pharmacokinetic profile. It exhibits a high binding affinity to μ-opioid receptors with a Ki of 0.2 ng/mL, enabling it to effectively counteract opioid-induced gastrointestinal motility inhibition without significant central nervous system penetration.
Key absorption, distribution, metabolism, and excretion (ADME) characteristics of alvimopan include minimal systemic availability within the central nervous system, supporting its peripheral selectivity. Detailed pharmacokinetic parameters such as bioavailability, half-life, metabolic pathways, and elimination routes are proprietary or limited in published literature but are critical for dosing regimen considerations in clinical use.
Safety and toxicity profiles indicate that alvimopan is generally well tolerated in approved indications; however, its use is contraindicated in patients who have taken therapeutic doses of opioids for more than seven consecutive days prior to initiation due to risk of precipitating withdrawal. Cardiovascular safety signals observed in long-term use have restricted its indication to short-term inpatient use.
Notable branded products containing alvimopan include Entereg, primarily marketed for postoperative ileus prevention in the United States. Regulatory approval status varies globally, with approvals focused on postoperative gastrointestinal function recovery.
For API procurement, it is essential to ensure rigorous quality control given the compound’s peptide nature, including assessment of purity, peptide sequence integrity, and potential impurities. Sourcing from manufacturers compliant with current Good Manufacturing Practices (cGMP) and supported by comprehensive analytical documentation is crucial to meet regulatory requirements and ensure batch-to-batch consistency.
Identification & chemistry
| Generic name | Alvimopan |
|---|---|
| Molecule type | Small molecule |
| CAS | 156053-89-3 |
| UNII | Q153V49P3Z |
| DrugBank ID | DB06274 |
Pharmacology
| Summary | Alvimopan is a peripherally acting opioid receptor antagonist that selectively binds mu-opioid receptors in the gastrointestinal tract, with additional affinity for kappa- and delta-opioid receptors. Its pharmacokinetic properties limit central nervous system penetration, enabling modulation of opioid-induced gastrointestinal effects without impacting central analgesia. The drug is primarily utilized to accelerate gastrointestinal recovery after bowel resection surgery. |
|---|---|
| Mechanism of action | Alvimopan competitively binds to mu-opioid receptor in the gastrointestinal tract but, unlike methylnaltrexone which relies upon it ionic charge, alvimopan owes its selectivity for peripheral receptors to its pharmacokinetics. Alvimopan binds to peripheral mu-receptors with a Ki of 0.2 ng/mL. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Mu-type opioid receptor | Humans | antagonist |
| Kappa-type opioid receptor | Humans | antagonist |
| Delta-type opioid receptor | Humans | antagonist |
ADME / PK
| Absorption | Alvimopan's high affinity for the peripheral mu-receptor leads to slower absorption dependent on dissociation from the receptor and subsequently low oral bioavailability of less than 7%. |
|---|---|
| Half-life | 10 to 17 hours (gut metabolite: 10 to 18 hours) |
| Protein binding | 80% to 90% bound in after entering systemic circulation. |
| Metabolism | Alvimopan is primarily metabolized by intestinal flora to an active metabolite although it has no clinically significant contribution to the effects of the drug. |
| Route of elimination | Biliary secretion was considered the primary pathway for alvimopan elimination. Unabsorbed drug and unchanged alvimopan resulting from biliary excretion were then hydrolyzed to its ‘metabolite’ by gut microflora. Feces (via biliary excretion) & urine (35%) |
| Volume of distribution | * 30±10 L |
| Clearance | * 402 ± 89 mL/min |
Formulation & handling
- Alvimopan is formulated for oral administration as capsules due to its solid state and stability profile.
- As a hybrid peptide small molecule, it may require consideration of peptide bond stability during formulation and processing.
- Food intake, especially high-fat meals, can reduce systemic exposure, although clinical impact remains uncertain.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has several patents expiring between 2016 and 2020, with additional patents protecting it until 2029-2030 in the United States. As a result, the US market exhibits varying levels of market maturity, with some generic entry possible following earlier patent expirations and ongoing protection from later patents. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Alvimopan is primarily supplied by a limited number of originator companies involved in packaging and distribution within the US market. The branded product presence is predominantly US-focused, with no indication of significant activity in EU or other regions. Patent protections extend through 2030, indicating ongoing market exclusivity and limited generic competition at present. |
|---|
Alvimopan is a type of Motility inhibitors
Motility inhibitors are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are used to regulate and control the movement of the gastrointestinal tract. These inhibitors play a crucial role in treating conditions such as irritable bowel syndrome (IBS), gastroesophageal reflux disease (GERD), and other gastrointestinal disorders.
Motility inhibitors work by blocking the action of certain neurotransmitters and receptors in the gastrointestinal tract, thereby reducing the frequency and intensity of contractions in the smooth muscles. This leads to a decrease in the speed of food passage through the digestive system, providing relief from symptoms like abdominal pain, bloating, and diarrhea.
One commonly used motility inhibitor is metoclopramide, which acts by inhibiting dopamine receptors in the gastrointestinal tract. It enhances the contractions of the stomach and small intestine while relaxing the muscles of the pyloric sphincter, thus improving gastric emptying and reducing reflux.
Another important motility inhibitor is loperamide, which works by slowing down the muscular contractions of the intestines. It is commonly used to treat diarrhea by increasing the time it takes for stool to move through the digestive system.
Motility inhibitors are available in various forms, including tablets, capsules, and oral suspensions. They are generally well-tolerated, but like any medication, they can have side effects such as drowsiness, dizziness, and constipation.
In summary, motility inhibitors are an essential subcategory of pharmaceutical APIs used to manage gastrointestinal disorders by regulating the movement of the digestive tract. They provide relief from symptoms and improve overall digestive function, enhancing the quality of life for individuals suffering from these conditions.
Alvimopan (Motility inhibitors), classified under 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.
Alvimopan API manufacturers & distributors
Compare qualified Alvimopan API suppliers worldwide. We currently have 2 companies offering Alvimopan 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, ISO9001, MSDS, USDMF | 229 products |
| MSN Life Sciences | Producer | India | India | CoA, USDMF, WC | 46 products |
When sending a request, specify which Alvimopan 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.).
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