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Olsalazine | CAS No: 15722-48-2 | GMP-certified suppliers
A medication that supports maintenance of remission and treatment of mild to moderate ulcerative colitis with targeted colonic anti-inflammatory effects for patients intolerant to sulfasalazine.
Therapeutic categories
Primary indications
- In the US, olsalazine is indicated for the maintenance of remission of ulcerative colitis in adult patients who are intolerant to [sulfasalazine]
- In Canada, it is used in the treatment of acute ulcerative colitis of mild to moderate severity, with or without the concomitant use of steroids
- It is also indicated for the long-term maintenance of patients with ulcerative colitis in remission
Product Snapshot
- Olsalazine is an oral small molecule available in capsule and tablet formulations
- It is primarily used for the treatment and maintenance of remission in ulcerative colitis
- Olsalazine is approved for use in the US and Canadian markets
Clinical Overview
Clinically, olsalazine is indicated primarily for the maintenance of remission in adult patients with ulcerative colitis who are intolerant to sulfasalazine. Additionally, in Canada, it is approved for the treatment of mild to moderate acute ulcerative colitis, either as monotherapy or in combination with corticosteroids, as well as for long-term maintenance therapy.
Pharmacodynamically, olsalazine acts as an anti-inflammatory agent by inhibiting cyclooxygenase (COX) and lipoxygenase enzymes, thereby reducing the synthesis of pro-inflammatory eicosanoids, including prostaglandins and leukotrienes, which contribute to colonic inflammation. It also exhibits inhibition of xanthine oxidase, potentially reducing oxidative stress via decreased oxygen-derived free radical production. Furthermore, olsalazine may limit macrophage migration to inflamed intestinal mucosa and act as a free radical scavenger, attenuating tissue damage mediated by inflammatory processes.
Upon oral administration, olsalazine is minimally absorbed in the upper gastrointestinal tract. The azo bond remains intact until reaching the colon, where bacterial cleavage releases mesalamine. This targeted delivery limits systemic exposure of the active moiety, potentially reducing systemic adverse effects. At therapeutic doses, olsalazine has been observed to reduce water and sodium absorption in the gut, with some influence on gastrointestinal transit time noted in a subset of patients.
Safety considerations include the potential for dose-dependent gastrointestinal effects such as diarrhea, as well as hypersensitivity reactions typical of aminosalicylates. Nephrotoxicity, although rare, requires monitoring in long-term use, and renal function assessment is recommended during therapy.
Olsalazine is classified chemically as an azobenzene, a compound featuring a central azo group (-N=N-) linking aromatic benzene rings. It falls under several pharmacological categories, including intestinal anti-inflammatory agents and non-selective nonsteroidal anti-inflammatory drugs (NSAIDs).
For pharmaceutical API procurement, it is important to source olsalazine from manufacturers compliant with Good Manufacturing Practices (GMP) to ensure purity, azo bond integrity, and consistent prodrug performance. Analytical characterization should confirm the absence of residual solvents, azo bond cleavage products, and impurities that could affect safety or therapeutic efficacy. Due to its targeted colonic activation, stability under gastrointestinal conditions and reproducible azo cleavage by colonic microflora are critical quality attributes.
Identification & chemistry
| Generic name | Olsalazine |
|---|---|
| Molecule type | Small molecule |
| CAS | 15722-48-2 |
| UNII | ULS5I8J03O |
| DrugBank ID | DB01250 |
Pharmacology
| Summary | Olsalazine is a prodrug that is metabolized in the colon to release mesalamine, which exerts anti-inflammatory effects primarily by inhibiting cyclooxygenase (COX)-mediated prostaglandin production. It also inhibits xanthine oxidase activity, reducing oxidative stress, and may limit macrophage migration to inflamed intestinal mucosa. The compound modulates arachidonic acid metabolism to alleviate inflammation associated with ulcerative colitis. |
|---|---|
| Mechanism of action | Upon administration, the azo bond connecting two molecules of mesalamine (also known as 5-aminosalicylic acid or 5-ASA) is cleaved by azoreductase-containing bacteria in the colon. The two molecules of mesalamine are released to mediate therapeutic effects. The exact mechanism of action of olsalazine and its active moiety mesalamine in ulcerative colitis has not been elucidated; however, it is understood that mesalamine mediates an anti-inflammatory action on epithelial cells of the colon. The COX-derived (i.e., prostanoids such as prostaglandin E2) and lipoxygenase-derived products (i.e., leukotrienes [LTs] and hydroxyeicosatetraenoic acids [HETEs]) of arachidonic acid metabolism have been implicated in the pathogenesis and maintenance of inflammatory disorders, including ulcerative colitis and inflammatory bowel disease. Mesalamine may attenuate inflammation by blocking the COX enzyme and inhibiting prostaglandin production in the colon. Olsalazine was also shown to inhibit xanthine oxidase, an enzyme that generates oxygen-derived free radicals. Olsalazine may attenuate intestinal inflammation by limiting macrophage migration to inflamed intestinal mucosa: it was shown to inhibit _in vitro_ migration of intestinal macrophages in response to leukotriene B<sub>4</sub>. Olsalazine may also act as a free radical scavenger, and mesalazine may suppress fatty acid peroxidation. |
| Pharmacodynamics | Olsalazine is an anti-inflammatory agent that blocks the production of cyclooxygenase (COX)-derived products of arachidonic acid metabolism. It works to alleviate inflammation in ulcerative colitis. Olsalazine was shown to decrease water and sodium absorption. While olsalazine is not expected to affect the motility and transit time of small intestines, it decreased small bowel transit time at high doses ranging from 60 to 120 mg/kg. In about 40% of the patients with ulcerative colitis, administration of olsalazine 1g daily was associated with a decrease in whole gut transit time. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Human Cyclooxygenases | Humans | inhibitor |
| Thiopurine S-methyltransferase | Humans | inhibitor |
| Interferon gamma | Humans |
ADME / PK
| Absorption | After oral administration, olsalazine has limited systemic bioavailability, with less than 5% of the oral dose being absorbed. Based on oral and intravenous dosing studies, approximately 2.4% of a single 1 g oral dose is absorbed. Maximum serum concentrations of olsalazine appear after approximately one hour and, even after a 1 g single dose, are low (e.g., 1.6 to 6.2 µmol/L). Patients on daily doses of 1 g olsalazine for two to four years show a stable plasma concentration of olsalazine-S (3.3 to 12.4 µmol/L). Olsalazine-S accumulates to a steady state within two to three weeks. Serum concentrations of mesalamine are detected after four to eight hours. The peak levels of mesalamine after an oral dose of 1 g olsalazine are low (i.e., 0 to 4.3 µmol/L). |
|---|---|
| Half-life | Olsalazine has a very short serum half-life, approximately 0.9 hours. Olsalazine-S has a half-life of seven days due to slow dissociation from the protein binding site. |
| Protein binding | Olsalazine and its metabolite olsalazine-S, are more than 99% bound to plasma proteins. Less than 1% of both olsalazine and olsalazine-S appears undissociated in plasma. It does not interfere with the protein binding of warfarin. Mesalamine (5-aminosalicylic acid, 5-ASA) and its metabolite, N-acetyl-5-ASA, are 74 and 81%, respectively, bound to plasma proteins. |
| Metabolism | Olsalazine is cleaved by colonic bacteria to release its active ingredient, mesalamine. Mesalamine can undergo acetylation to form N-acetyl-5-aminosalicylic acid (N-acetyl-5-ASA, Ac-5-ASA) by the colonic epithelium; however, the extent of acetylation depends on transit time. Approximately 0.1% of an oral dose of olsalazine is metabolized in the liver to olsalazine-O-sulfate (olsalazine-S). |
| Route of elimination | Olsalazine and its metabolites are excreted in the urine. Total recovery of oral 14C-labeled olsalazine in animals and humans ranges from 90 to 97%. Approximately 20% of the total mesalamine is recovered in the urine. Of the total mesalamine found in the urine, more than 90% is N-acetyl-5-ASA. Only small amounts of mesalamine are detected in the urine. The remaining mesalamine is partially acetylated and excreted in the feces. From fecal dialysis, the concentration of mesalamine in the colon following olsalazine has been calculated to be 18 to 49 mmol/L. The urinary recovery of olsalazine is below 1%. Less than 5% of an oral dose (0.25 to 2g) was recovered unchanged in the feces; however, more than 50% of the oral dose was excreted in feces as unchanged olsalazine when the whole gut transit time was decreased by approximately 50%. |
| Volume of distribution | The steady-state volume of distribution determined in healthy volunteers is approximately 5L. |
Formulation & handling
- Olsalazine is formulated for oral administration primarily as capsules or tablets due to its low water solubility.
- It is a small molecule azobenzene compound and does not have peptide or biologic characteristics.
- Administering with food is recommended to reduce adverse effects, although food does not impact its absorption or systemic exposure.
Regulatory status
| Lifecycle | The API's patent protection has expired in both the US and Canadian markets, allowing for generic competition and indicating a mature product lifecycle in these regions. Ongoing market activity is primarily driven by off-patent formulations. |
|---|
| Markets | US, Canada |
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Supply Chain
| Supply chain summary | Olsalazine is supplied by multiple originator companies, including Alaven Pharmaceutical, Pfizer Inc., Pharmacia Inc., and UCB Pharma, primarily targeting the US and Canadian markets. The branded product Dipentum has a consistent global presence in these regions. Patent expiries have allowed for existing generic competition in these markets. |
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Safety
| Toxicity | There is no information available regarding acute toxicity (LD<sub>50</sub>) of olsalazine. Symptoms of salicylate toxicity include nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe intoxication may lead to electrolyte and blood pH imbalance and potentially to organ damage. There is no antidote for olsalazine overdose; however, conventional therapy for salicylate toxicity, such as gastrointestinal tract decontamination, may be beneficial in acute overdosage. Overdose should be managed with proper medical care and appropriate supportive care, including the possible use of emesis, cathartics, and activated charcoal to prevent further absorption. Fluid and electrolyte imbalance may be managed with appropriate intravenous therapy and maintenance of adequate renal function. |
|---|
- Acute toxicity data (LD50) for olsalazine are not available
- However, salicylate-related toxic effects such as gastrointestinal distress, respiratory symptoms, and neurological impairment have been reported
- Severe overdose may result in electrolyte imbalance, acid-base disturbances, and potential organ damage
Olsalazine is a type of Aminosalicylates
Aminosalicylates are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the treatment of various inflammatory bowel diseases (IBDs), including ulcerative colitis and Crohn's disease. These compounds exhibit anti-inflammatory properties that target the gastrointestinal tract, helping to alleviate symptoms and manage these chronic conditions effectively.
Aminosalicylates function by inhibiting the production of inflammatory mediators, such as prostaglandins and leukotrienes, which play a significant role in triggering inflammation in the gut. By reducing the levels of these compounds, aminosalicylates aid in the suppression of inflammation, leading to symptom relief and promoting mucosal healing.
Commonly prescribed aminosalicylates include mesalazine (also known as mesalamine), olsalazine, and sulfasalazine. These medications are available in various formulations, including oral tablets, capsules, and rectal suppositories or enemas. The choice of formulation depends on the severity and location of the disease within the gastrointestinal tract.
The use of aminosalicylates has been shown to effectively induce and maintain remission in patients with IBDs. They are generally well-tolerated, with few reported side effects. However, as with any medication, individuals may experience mild adverse reactions, such as nausea, abdominal discomfort, or headaches.
In conclusion, aminosalicylates are a crucial class of pharmaceutical APIs utilized in the treatment of inflammatory bowel diseases. Their anti-inflammatory properties and targeted action on the gastrointestinal tract make them valuable therapeutic options for managing these chronic conditions. Proper usage of aminosalicylates, as directed by healthcare professionals, can significantly improve the quality of life for individuals living with IBDs.
Olsalazine (Aminosalicylates), classified under Anti-inflammatory Agents
Anti-inflammatory agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat various inflammatory conditions. These agents play a vital role in alleviating pain, reducing swelling, and controlling inflammation in the body. They are widely employed in the management of diverse medical conditions, including arthritis, autoimmune disorders, asthma, and skin conditions like dermatitis.
Anti-inflammatory APIs primarily function by inhibiting the production of specific enzymes called cyclooxygenases (COX) and lipoxygenases (LOX). These enzymes are responsible for the synthesis of pro-inflammatory molecules known as prostaglandins and leukotrienes, respectively. By suppressing the activity of COX and LOX, anti-inflammatory agents effectively curtail the production of these inflammatory mediators, thereby mitigating inflammation.
Common examples of anti-inflammatory APIs include non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen, aspirin, and naproxen. These agents exhibit analgesic, antipyretic, and anti-inflammatory properties. Another group of anti-inflammatory APIs includes corticosteroids, such as prednisone and dexamethasone, which are synthetic hormones that modulate the body's immune response to control inflammation.
In conclusion, anti-inflammatory agents are a vital category of pharmaceutical APIs widely used to manage inflammation-related disorders. They target enzymes involved in the synthesis of pro-inflammatory molecules, effectively reducing pain and swelling. NSAIDs and corticosteroids are commonly prescribed anti-inflammatory APIs due to their efficacy in controlling inflammation.
Olsalazine API manufacturers & distributors
Compare qualified Olsalazine API suppliers worldwide. We currently have 2 companies offering Olsalazine 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 |
|---|---|---|---|---|---|
| Corden Pharma | Producer | Germany | Italy | CoA, GMP, USDMF | 45 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
When sending a request, specify which Olsalazine 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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