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Loxoprofen | CAS No: 68767-14-6 | GMP-certified suppliers
A medication that relieves pain, inflammation, and fever associated with musculoskeletal and joint disorders, supporting reliable therapeutic development needs for API sourcing teams.
Therapeutic categories
Primary indications
- Loxoprofen is non-steroidal anti-inflammatory medication (NSAID) indicated for pain and inflammation related to musculoskeletal and joint disorders
- In addition to its effects on pain, it is an antipyretic and anti-inflammatory medication
Product Snapshot
- Loxoprofen is an oral and topical small‑molecule NSAID available in tablet, gel, and transdermal patch formulations
- It is used for pain, inflammation, and fever associated with musculoskeletal and joint conditions
- It is an approved product in multiple regulated markets
Clinical Overview
The compound is a phenylpropanoic acid that functions primarily as a prodrug. After administration, it is rapidly converted to its trans‑alcohol metabolite, which provides pharmacological activity. This metabolite is a potent, non‑selective inhibitor of cyclooxygenase isoforms COX‑1 and COX‑2. Inhibition reduces synthesis of prostaglandins, prostacyclin, and thromboxanes involved in nociception, inflammation, and febrile responses.
Pharmacodynamically, non‑selective COX inhibition decreases peripheral and central sensitization to pain while suppressing inflammatory mediator production at sites of tissue injury. Because COX‑1 also regulates gastric mucosal integrity, renal blood flow, and platelet aggregation, non‑selective blockade contributes to the expected class‑based risk profile.
Following oral dosing, loxoprofen is absorbed and undergoes rapid metabolic activation. The active metabolite is further conjugated, with UGT2B7 identified as a metabolic pathway. Elimination occurs primarily via renal excretion. Specific bioavailability, half‑life, and protein binding values are not provided in the source data and are therefore not included.
Safety considerations align with other non‑selective NSAIDs. Clinically relevant risks include gastrointestinal irritation or ulceration, renal function impairment, fluid retention, hypertension, and potential exacerbation of hyperkalemia. Use in patients with compromised renal function, cardiovascular disease, or gastrointestinal ulcer history requires caution. Known nephrotoxic potential and effects on platelet function are consistent with its COX‑1 activity.
Loxoprofen is available in systemic and topical formulations, with transdermal preparations used to achieve localized exposure while limiting systemic effects.
For API procurement, suppliers should provide evidence of identity and purity, validated control of stereochemistry and impurity profiles, and compliance with regional regulatory standards. Batch‑specific data on residual solvents, particle properties, and stability support reliable formulation development and quality assurance.
Identification & chemistry
| Generic name | Loxoprofen |
|---|---|
| Molecule type | Small molecule |
| CAS | 68767-14-6 |
| UNII | 3583H0GZAP |
| DrugBank ID | DB09212 |
Pharmacology
| Summary | Loxoprofen is a prodrug converted to an active trans‑alcohol metabolite that non‑selectively inhibits the COX‑1 and COX‑2 enzymes. This inhibition decreases synthesis of prostaglandins and related mediators involved in pain, inflammation, and fever. Its pharmacologic activity aligns with therapeutic use in musculoskeletal and joint inflammatory conditions. |
|---|---|
| Mechanism of action | Loxoprofen itself is a prodrug and carries little-to-no pharmacological activity - it is rapidly metabolized to its trans-alcohol form, which is a potent and non-selective inhibitor of cyclooxygenase.Cyclooxygenase (COX) is present in 2 forms, COX-1 and COX-2, with each serving different functions. COX-1 is present in human cells and is constitutively released, performing cellular housekeeping functions such as mucus production and platelet aggregation.COX-2 is induced in human cells post-injury or due to other stimuli, is triggered to appear in large quantities at the sites of injury/stimuli, and is ultimately responsible for the mediation of inflammation and pain. Loxoprofen's active metabolite inhibits both COX isoforms, resulting in reduced expression of several mediators of pain, inflammation, and fever (e.g. prostaglandins, prostacyclin, thromboxane, etc). |
| Pharmacodynamics | Loxoprofen is a non-selective inhibitor of cyclooxygenase enzymes, which are responsible for the formation of various biologically active pain, fever, and inflammatory mediators. These include prostaglandins, prostacyclin, thromboxane, and arachidonic acid. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Prostaglandin G/H synthase 2 | Humans | antagonist |
| Prostaglandin G/H synthase 1 | Humans | antagonist |
ADME / PK
| Absorption | Loxoprofen is rapidly and completely absorbed from the GI tract with a bioavailability of 95%.The absorption phase of the medication occurs in the first 4-6 hours after ingestion. Food ingestion with the medication causes a slight decrease in the rate of loxoprofen absorption. |
|---|---|
| Half-life | The elimination half-life of Loxoprofen is approximately 15 hours.Steady concentration is achieved after 2-3 doses. |
| Protein binding | 99% albumin-bound.At doses of loxoprofen greater than 500 mg/day, clearance of the drug increases as saturation of plasma protein binding occurs at higher doses. |
| Metabolism | Loxoprofen is a prodrug that is rapidly converted to its active trans-alcohol metabolite by carbonyl reductase in the liver.This same process also results in a cis-alcohol metabolite, though this isomer carries little pharmacological activity.The parent drug has also been observed to undergo oxidation via CYP3A4/5 to two hydroxylated metabolites (M3 and M4) and glucuronidation by UGT2B7 to two glucuronide metabolites (M5 and M6).The alcohol metabolites of loxoprofen also undergo glucuronide conjugation via UGT2B7 to two glucuronide metabolites (M7 and M8) prior to excretion. When applied in topical formulations, loxoprofen is metabolized to its active trans-alcohol form by carbonyl reductase in the skin. |
| Route of elimination | 50% renal excretion.This drug is 20% - 30% excreted in the stool. |
| Volume of distribution | Loxoprofen has a volume of distribution of 0.16 L/kg. |
| Clearance | Most of the drug as unchanged loxoprofen, 6-0-desmethyl loxoprofen (less than 1%) and glucuronide or other conjugates (66-92%). In patients with renal failure, metabolites may accumulate. |
Formulation & handling
- Low aqueous solubility and moderate lipophilicity support solid oral tablet formulations and favor topical or transdermal delivery for local effect.
- Oral formulations may require consideration of food-related GI tolerability and CYP3A4‑modulating excipients due to metabolism characteristics.
- As a small‑molecule solid, standard handling applies, with attention to stability in semi-solid topical bases for gels and patches.
Regulatory status
Safety
| Toxicity | Adverse effects include anorexia, nausea, vomiting, bleeding, anemia, diarrhea, and constipation.Loxoprofen toxicity may lead to gastrointestinal disturbance (including flatulence, dyspepsia and gastritis) and renal failure. |
|---|
- Handle with controls that minimize exposure to agents associated with gastrointestinal irritation (e
- G
- , nausea, vomiting, dyspepsia, bleeding) and renal burden observed in toxicity profiles
Loxoprofen is a type of NSAIDs
NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) are a widely used subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs). These medications are commonly prescribed for their analgesic (pain-relieving), anti-inflammatory, and antipyretic (fever-reducing) properties. NSAIDs work by inhibiting the production of certain enzymes called cyclooxygenases (COX), which play a crucial role in the synthesis of prostaglandins, substances that contribute to pain, inflammation, and fever.
These pharmaceutical APIs are available in various formulations, including tablets, capsules, creams, and gels, making them convenient for different administration routes. Some popular examples of NSAIDs include aspirin, ibuprofen, naproxen, and diclofenac.
NSAIDs are commonly used to treat a wide range of conditions such as arthritis, musculoskeletal injuries, dental pain, menstrual pain, and headaches. They are also effective in managing inflammatory conditions like rheumatoid arthritis and ankylosing spondylitis.
While NSAIDs are generally safe and effective when used as directed, they may have side effects. These can include gastrointestinal issues such as stomach ulcers or bleeding, cardiovascular risks, and kidney problems. Therefore, it is essential to follow the recommended dosage and consult with healthcare professionals to ensure proper and safe usage.
In conclusion, NSAIDs are a subcategory of pharmaceutical APIs that offer analgesic, anti-inflammatory, and antipyretic properties. Their versatility and effectiveness in treating various conditions make them widely prescribed medications. However, it is crucial to be aware of potential side effects and consult healthcare providers for appropriate usage.
Loxoprofen (NSAIDs), 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.
Loxoprofen API manufacturers & distributors
Compare qualified Loxoprofen API suppliers worldwide. We currently have 15 companies offering Loxoprofen 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 |
|---|---|---|---|---|---|
| Daiichi Sankyo | Producer | Japan | Japan | CoA, JDMF | 9 products |
| Dongbang FTL | Producer | South Korea | South Korea | CoA, JDMF, KDMF | 13 products |
| Fujian Huitian Bio-pharma | Producer | China | China | CoA, JDMF | 1 products |
| Hamari Chemicals | Producer | Japan | Japan | CoA, JDMF | 12 products |
| Hanseo Chem | Producer | South Korea | South Korea | CoA, JDMF | 2 products |
| Hubei Xunda Pharmaceutica... | Producer | China | China | CoA, JDMF | 2 products |
| Kolon Life Science | Producer | South Korea | South Korea | CoA, JDMF | 32 products |
| Kukjeon Pharm | Producer | Japan | Japan | CoA, JDMF | 3 products |
| Pen Tsao Chemical Industr... | Producer | Germany | China | CoA, KDMF | 18 products |
| SAMOH Pharm | Producer | South Korea | South Korea | CoA, JDMF | 2 products |
| Shin Poong Pharm | Producer | South Korea | South Korea | CoA, JDMF | 11 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, MSDS, USDMF | 757 products |
| Yungjin Pharmaceutical | Producer | South Korea | South Korea | CoA, JDMF | 10 products |
| ZCL Chemicals | Producer | India | India | CoA, Other, FDA, ISO9001 | 30 products |
| Zhejiang Apeloa Tospo-Jia... | Producer | China | China | CoA, JDMF | 15 products |
When sending a request, specify which Loxoprofen 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 Loxoprofen 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 Loxoprofen API
Sourcing
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Technical
What is Loxoprofen (CAS 68767-14-6) used for?
Which therapeutic class does Loxoprofen fall into?
What conditions is Loxoprofen mainly prescribed for?
How does Loxoprofen work?
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Is Loxoprofen a small molecule?
Are there special stability concerns for oral Loxoprofen?
Pharmaoffer
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