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Apremilast | CAS No: 608141-41-9 | GMP-certified suppliers
A medication that treats adult psoriatic arthritis, plaque psoriasis requiring systemic care, and oral ulcers linked to Behcet’s disease for broad inflammatory disease management.
Therapeutic categories
Primary indications
- Apremilast is indicated for the treatment of adults with active psoriatic arthritis and adults with oral ulcers associated with Behcet's Disease
- In addition, apremilast is indicated for the treatment of plaque psoriasis, of any severity, in adult patients who are candidates for phototherapy or systemic therapy
Product Snapshot
- Apremilast is an oral small-molecule product supplied as film-coated tablets
- It is used for psoriatic arthritis, plaque psoriasis, and oral ulcers associated with Behçet’s disease
- It is approved in the US, EU, and Canada, with additional investigational activity noted
Clinical Overview
Apremilast decreases the production of multiple proinflammatory cytokines, including TNF‑α, IL‑1α, IL‑6, IL‑8, MCP‑1, MIP‑1β, and MMP‑3. Symptom improvement in psoriatic disease and Behcet’s‑related oral ulcers reflects reductions in these mediators rather than full suppression.
Its primary mechanism involves PDE4 inhibition, which elevates intracellular cAMP concentrations. Increased cAMP downregulates the expression of cytokines implicated in epidermal hyperproliferation, synovial inflammation, and mucocutaneous ulceration. Although the exact downstream cascade is not fully defined, attenuation of IL‑17 and IL‑23 activity appears to contribute to clinical efficacy across psoriatic and Behcet’s phenotypes.
Apremilast is orally bioavailable and undergoes extensive metabolism, with CYP3A4 representing a major pathway and minor contributions from CYP1A2 and CYP2A6. Metabolites are eliminated through both renal and fecal routes. It is also a P‑glycoprotein substrate. No specific dose adjustments are typically described for mild organ impairment, but exposure may rise in severe renal dysfunction.
Safety considerations include gastrointestinal intolerance, headache, weight loss, and mood‑related adverse effects. Reports of depression and suicidal ideation necessitate baseline and ongoing monitoring, particularly in patients with pre‑existing psychiatric conditions. Clinically meaningful weight reduction warrants reassessment of therapy.
For API procurement, sourcing should prioritize manufacturers with demonstrated control of stereochemical integrity, impurity profiles aligned with current regulatory expectations, and validated processes for managing PDE4‑inhibitor–specific degradation pathways. Consistent documentation of synthetic route, residual solvents, and stability data supports reliable formulation development and global regulatory submission.
Identification & chemistry
| Generic name | Apremilast |
|---|---|
| Molecule type | Small molecule |
| CAS | 608141-41-9 |
| UNII | UP7QBP99PN |
| DrugBank ID | DB05676 |
Pharmacology
| Summary | Apremilast is a phosphodiesterase‑4 inhibitor that increases intracellular cAMP, leading to downstream suppression of pro‑inflammatory mediators such as TNF‑α, IL‑17, and IL‑23. This modulation of cytokine activity reduces inflammatory signaling relevant to psoriatic disease and Behçet’s disease. Its pharmacodynamic profile reflects partial reduction of multiple cytokines involved in these conditions. |
|---|---|
| Mechanism of action | The full mechanism of action of this drug is not fully established, however, it is known that apremilast is an inhibitor of phosphodiesterase 4 (PDE4), which mediates the activity of cyclic adenosine monophosphate (cAMP), a second messenger.The inhibition of PDE4 by apremilast leads to increased intracellular cAMP levels.An increase in cAMP results in the suppression of inflammation by decreasing the expression of TNF-α, IL-17, IL-23, and other inflammatory mediators. The above inflammatory mediators have been implicated in various psoriatic conditions as well as Behcet's disease, leading to their undesirable inflammatory symptoms such as mouth ulcers, skin lesions, and arthritis.Apremilast administration leads to a cascade which eventually decreases the levels of the above mediators, relieving inflammatory symptoms. |
| Pharmacodynamics | Apremilast reduces but does not completely inhibit various inflammatory cytokines such as IL-1α, IL-6, IL-8, IL-10 MCP-1, MIP-1β, MMP-3, and TNF-α, relieving the symptoms of psoriasis and Behcet's disease, which are caused by an increase in these inflammatory mediators.This drug has also been proven to be effective in relieving the pain associated with oral ulcers in Behcet's disease. Apremilast may cause unwanted weight loss and worsen depression, leading to suicidal thoughts or actions. It is advisable to monitor for symptoms of depression and seek medical attention if they occur, especially in patients with pre-existing depression. The need for apremilast should be carefully assessed along with the risk of worsening depression and suicide. If weight loss occurs, the degree of weight loss should be evaluated, and consideration should be made for the possible discontinuation of apremilast. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Phosphodiesterase isozyme 4 | Humans | antagonist |
ADME / PK
| Absorption | An oral dose of apremilast is well-absorbed and the absolute bioavailability is approximately 73%. Tmax is approximately 2.5 hoursand Cmax has been reported to be approximately 584 ng/mL in one pharmacokinetic study.Food intake does not appear to affect apremilast absorption. |
|---|---|
| Half-life | The average elimination half-life of this drug ranges from 6-9 hours. |
| Protein binding | The plasma protein binding of apremilast is about 68%. |
| Metabolism | Apremilast is heavily metabolized by various pathways, which include oxidation, hydrolysis, in addition to conjugation. About 23 metabolites are produced from its metabolism.The CYP3A4 primarily mediates the oxidative metabolism of this drug, with smaller contributions from CYP1A2 and CYP2A6 enzymes.The main metabolite of apremilast, M12, is an inactive glucuronide conjugate form of the O-demethylated drug.Some other major metabolites, M14 and M16, are significantly less active in the inhibition of PDE4 and inflammatory mediators than their parent drug, apremilast. After an oral dose, unchanged apremilast (45%) and the inactive metabolite, O-desmethyl apremilast glucuronide (39%) are found in the plasma. Minor metabolites M7 and M17 are active, but are only present in about 2% or less of apremilast concentrations, and likely not significant contributors to the actions of apremilast. |
| Route of elimination | Only 3% and 7% of an apremilast dose are detected in the urine and feces as unchanged drug, respectively, indicating extensive metabolism and high absorption. |
| Volume of distribution | The average apparent volume of distribution (Vd) is about 87 L, suggesting that apremilast is distributed in the extravascular compartment. |
| Clearance | In healthy patients, the plasma clearance of apremilast is about 10 L/hour. |
Formulation & handling
- Oral small‑molecule solid with low aqueous solubility, typically formulated as film‑coated tablets to aid manufacturability and consistent dissolution.
- Moderate lipophilicity and poor water solubility may require particle-size control or solubility‑enhancing excipients for uniform oral absorption.
- As a CYP3A substrate, co‑administration with strong enzyme inducers (e.g., St. John’s wort) can reduce exposure, but food has minimal impact on performance.
Regulatory status
| Lifecycle | Most U.S. patents covering this API have expired, with the final group ending in 2023, indicating that the product is now in a post‑exclusivity stage. Across the US, EU, and Canada, the market is expected to reflect a mature competitive environment. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Apremilast was originally developed by a single originator company, with branded products established across the US, EU, and Canada. With multiple key US patents expiring in 2018 and 2023, the product has moved into a period where generic competition is viable. This shift supports broader manufacturer participation beyond the initial originator supply base. |
|---|
Safety
| Toxicity | The oral LD50 in mice was greater than 2000 mg/kg in mice. In rats, oral LD50 was 2000 mg/kg males and 300 mg/kg in females. Overdose information In healthy subjects receiving a maximum dose of 100 mg (given as 50 mg twice daily) for about 5 days, no significant toxicity was observed. In cases of an overdose, supportive and symptomatic treatment should be administered. Contact the local poison control center for the most recent overdose management for apremilast. |
|---|
- Acute oral toxicity shows species- and sex‑dependent variability, with LD50 values ›2000 mg/kg in mice and 2000 mg/kg (males) vs
- 300 mg/kg (females) in rats
- In controlled studies up to 100 mg/day for 5 days, no significant systemic toxicity was detected, indicating a relatively wide acute exposure margin under test conditions
Apremilast is a type of Immunosuppressants
Immunosuppressants are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in medical treatments. These substances are designed to suppress or weaken the immune system's response, making them invaluable in various therapeutic applications.
Immunosuppressants find extensive use in the management of autoimmune diseases, organ transplantation, and the prevention of rejection reactions. By modulating the immune system's activity, these APIs help control excessive immune responses that can lead to tissue damage and chronic inflammation.
There are different classes of immunosuppressants, including corticosteroids, calcineurin inhibitors, antimetabolites, and biologics. Each class targets specific immune pathways to achieve the desired therapeutic effect. Corticosteroids, for instance, are known for their potent anti-inflammatory properties, making them effective in managing conditions such as rheumatoid arthritis and asthma.
Calcineurin inhibitors like cyclosporine and tacrolimus act by inhibiting the activity of calcineurin, a protein involved in immune cell activation. These drugs are commonly used in organ transplantation to prevent the immune system from attacking the transplanted organ.
Antimetabolites interfere with DNA synthesis and cell proliferation, thereby dampening immune responses. They are often prescribed for conditions like psoriasis and rheumatoid arthritis.
Biologic immunosuppressants, such as monoclonal antibodies, target specific immune cells or molecules involved in the disease process. They have revolutionized the treatment of autoimmune diseases like rheumatoid arthritis, Crohn's disease, and psoriasis.
Immunosuppressants require careful administration and monitoring due to their potential side effects and interactions with other medications. Close collaboration between healthcare professionals, pharmacists, and patients is essential to ensure the safe and effective use of these APIs in various therapeutic settings.
Overall, immunosuppressants represent a critical category of pharmaceutical APIs that significantly contribute to improving patients' quality of life by controlling the immune system's activity and managing various autoimmune conditions and transplantation outcomes.
Apremilast (Immunosuppressants), classified under Immunomodulators
Immunomodulators, a category of pharmaceutical active pharmaceutical ingredients (APIs), are substances that help regulate and modify the immune response of an individual. These compounds play a crucial role in treating various immune-related disorders and diseases. Immunomodulators work by either enhancing or suppressing the immune system, depending on the specific condition being treated.
Immunomodulators are used in the treatment of autoimmune disorders, such as rheumatoid arthritis, multiple sclerosis, and psoriasis. By suppressing the immune system, these APIs help reduce the overactive immune response associated with these conditions, thereby alleviating symptoms and preventing further damage to the body's tissues.
On the other hand, immunomodulators are also employed to boost the immune system in cases of immunodeficiency disorders. These APIs stimulate the immune response, enabling the body to better fight off infections and diseases. Additionally, immunomodulators are utilized in the prevention and treatment of organ transplant rejection, where they help modulate the immune system to accept the transplanted organ.
The development and production of immunomodulators require rigorous testing and quality control to ensure their safety and efficacy. Pharmaceutical companies carefully formulate these APIs into various dosage forms, including tablets, capsules, injections, and topical preparations, to cater to different patient needs.
In summary, immunomodulators form a vital category of pharmaceutical APIs that regulate and modify the immune system. With their ability to modulate immune responses, these compounds contribute significantly to the management and treatment of various immune-related disorders and diseases, improving the quality of life for many patients.
Apremilast API manufacturers & distributors
Compare qualified Apremilast API suppliers worldwide. We currently have 24 companies offering Apremilast API, with manufacturing taking place in 5 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 |
|---|---|---|---|---|---|
| Alkem Labs. | Producer | India | India | CoA, USDMF | 22 products |
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, ISO9001, MSDS, USDMF | 229 products |
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Dr. Sahu's Laboratories | Producer | India | India | CoA, GMP | 70 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hetero Drugs | Producer | India | India | CoA, USDMF | 98 products |
| Intas Pharma | Producer | United Kingdom | Unknown | CoA, USDMF | 30 products |
| Jubilant Pharmova | Producer | India | India | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF | 52 products |
| Lek Pharma | Producer | Slovenia | India | CoA, USDMF | 32 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| MSN Life Sciences | Producer | India | India | CoA, USDMF, WC | 46 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Pharma Links India | Distributor | India | India | CoA, GMP | 7 products |
| PLIVA | Producer | Czech Republic | Croatia | CoA, GMP | 31 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CEP, CoA, FDA, GMP, MSDS, USDMF | 64 products |
| Quimica Sintetica | Producer | Spain | Unknown | CoA, GMP, USDMF | 51 products |
| Raks Pharma | Producer | India | India | CoA, USDMF | 58 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, FDA, ISO9001 | 157 products |
| Shandong Boyuan | Producer | China | China | BSE/TSE, CoA, MSDS | 55 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, MSDS | 757 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Unichem Labs. | Producer | India | India | CoA, USDMF | 62 products |
When sending a request, specify which Apremilast 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 Apremilast 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 Apremilast API
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