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Tofacitinib | CAS No: 477600-75-2 | GMP-certified suppliers
A medication that supports management of rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, and polyarticular juvenile idiopathic arthritis in patients with inadequate response to prior therapies.
Therapeutic categories
Primary indications
- Tofacitinib is indicated for the treatment of adult patients with moderately-to-severely active rheumatoid arthritis (RA), active psoriatic arthritis, active ankylosing spondylitis, or moderately-to-severely active ulcerative colitis who have had an inadequate response or intolerance to one or more TNF blockers
- It is also indicated as an oral solution in patients ≥2 years of age for the treatment of polyarticular course juvenile idiopathic arthritis who have had an inadequate response or intolerance to one or more TNF blockers
- Tofacitinib is not recommended to be used in combination with other biologic disease-modifying anti-rheumatic drugs (DMARDs) or potent immunosuppressive agents such as azathioprine or cyclosporine
Product Snapshot
- Oral small‑molecule formulation available as tablets, extended‑release tablets, and oral solution
- Primary uses include rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, and polyarticular juvenile idiopathic arthritis
- Approved in the US, EU, and Canada, with additional investigational status in other markets
Clinical Overview
The drug modulates cytokine‑driven inflammatory activity by partially and reversibly inhibiting JAK family enzymes, reducing downstream STAT phosphorylation and transcriptional activation. This dampens signaling of interleukins and interferons implicated in autoimmune pathology. Pharmacodynamic effects include dose‑dependent reductions in C‑reactive protein, decreases in natural killer cells, and increases in B cells. Clinical studies in rheumatoid arthritis demonstrated early improvements in ACR20 responses within approximately two weeks.
Absorption is rapid after oral dosing and metabolism occurs primarily via CYP3A‑mediated pathways, with a lesser contribution from CYP2C19. Pharmacodynamic activity may persist beyond the plasma half‑life, consistent with prolonged suppression of inflammatory markers.
Common adverse effects include headache, diarrhea, nausea, nasopharyngitis, and upper respiratory tract infection. More serious risks relate to immunosuppression and hematologic toxicity, including lymphopenia, neutropenia, anemia, and increased susceptibility to bacterial, viral, fungal, or mycobacterial infections. Screening and monitoring for tuberculosis are required before and during therapy. Long‑term use has been associated with increased rates of lymphomas and other malignancies, and routine monitoring of lymphocytes, neutrophils, hemoglobin, liver enzymes, and lipid parameters is recommended.
Tofacitinib is marketed under the brand name Xeljanz in several regions. For API procurement, manufacturers should verify compliance with regional GMP standards, control for polymorphic form and impurity profile, and ensure suitability for both immediate‑release solid oral formulations and oral solution manufacturing where applicable.
Identification & chemistry
| Generic name | Tofacitinib |
|---|---|
| Molecule type | Small molecule |
| CAS | 477600-75-2 |
| UNII | 87LA6FU830 |
| DrugBank ID | DB08895 |
Pharmacology
| Summary | Tofacitinib is a reversible inhibitor of JAK1, JAK2, JAK3, and TYK2 that suppresses cytokine‑driven signaling in autoimmune and inflammatory pathways. By blocking JAK‑mediated phosphorylation of STAT proteins, it reduces transcription of genes involved in immune‑cell activation and inflammatory mediator production. Its pharmacodynamic profile reflects broad attenuation of cytokine activity, including reductions in inflammatory markers such as C‑reactive protein. |
|---|---|
| Mechanism of action | Rheumatoid arthritis is an autoimmune disease characterized by a dysregulation of pro-inflammatory cytokines including IL7, IL15, IL21, IL6, IFN-alpha, and IFN-beta. (3) Cytokines signalling results in tissue inflammation and joint damage by stimulating the recruitment and activation of immune cells via the janus kinase signalling pathway. Tofacitinib is a partial and reversible janus kinase (JAK) inihibitor that will prevent the body from responding to cytokine signals. By inhibiting JAKs, tofacitinib prevents the phosphorylation and activation of STATs. The JAK-STAT signalling pathway is involved in the transcription of cells involved in hematopoiesis, and immune cell function. Tofacitinib works therapeutically by inhibiting the JAK-STAT pathway to decrease the inflammatory response. However, there is evidence to suggest that it may also achieve efficacy via other pathways as well. |
| Pharmacodynamics | Tofacitinib targets inflammation present in rheumatoid arthritis by inhibiting the janus kinases involved in the inflammatory response pathway. In placebo controlled trials of rheumatoid arthritis patients receiving 5mg or 10mg of tofacitinib twice daily, higher ACR20 responses were observed within 2 weeks in some patients (with ACR20 being defined as a minimum 20% reduction in joint pain or tenderness and 20% reduction in arthritis pain, patient disability, inflammatory markers, or global assessments of arthritis by patients or by doctors, according to the American College of Rheumatology (ACR) response criteria list), and improvements in physical functioning greater than placebo were also noted. Common known adverse effects of tofacitinib include headaches, diarrhea, nausea, nasopharyngitis and upper respiratory tract infection. More serious immunologic and hematological adverse effects have also been noted resulting in lymphopenia, neutropenia, anemia, and increased risk of cancer and infection. Before initiations of tofacitinib patients should be tested for latent infections of tuberculosis, and should be closely monitored for signs and symptoms of infection (fungal, viral, bacterial, or mycobacterial) during therapy. Therapy is not to be started in the presence of active infection, systemic or localized, and is to be interrupted if a serious infection occurs. Tofacitinib has been associated with an increased risk of lymphomas, such as Epstein-Barr virus associated lymphomas, and other malignancies (including lung, breast, gastric, and colorectal cancers). It is recommended to monitor lymphocytes, neutrophils, hemoglobin, liver enzymes, and lipids. Tofacitinib use is associated with a rapid decrease in C-reactive protein (CRP), dose dependent decreases in natural killer cells, and dose dependent increases in B cells. Depression in C-reactive protein levels continue after 2 weeks of tofacitinib discontinuation and suggest that pharmacodynamic activity last longer than pharmacokinetic half life. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Tyrosine-protein kinase JAK1 | Humans | inhibitor |
| Tyrosine-protein kinase JAK2 | Humans | antagonist, inhibitor |
| Tyrosine-protein kinase JAK3 | Humans | inhibitor |
ADME / PK
| Absorption | 74% oral absorption (absolute bioavailability), with peak plasma concentrations (T <sub> max</sub>) achieved in 0.5-1 hour. Administration with fatty meals does not alter AUC but reduces Cmax by 32%. |
|---|---|
| Half-life | ~3 hours |
| Protein binding | 40%, mostly bound to albumin. |
| Metabolism | Metabolized in the liver by CYP3A4 and CYP2C19. Metabolites produced are inactive. |
| Route of elimination | 70% metabolized in the liver by CYP3A4 (major) and CYP2C19 (minor). Metabolites produced are inactive. 30% renally eliminated as unchanged drug. |
| Volume of distribution | Vd= 87L after intravenous administration. Distribution is equal between red blood cells and plasma. |
Formulation & handling
- Oral small‑molecule API with moderate hydrophilicity (LogP ~1.2) and low aqueous solubility, typically formulated as immediate‑release or extended‑release tablets and oral solutions.
- Chemical stability is compatible with conventional solid‑oral processing; moisture control is advisable due to limited solubility and potential recrystallization risk in solution formats.
- Metabolism is CYP3A4/2C19‑dependent, and grapefruit/St. John’s Wort interactions imply potential need for labeling considerations but do not affect standard oral formulation approaches.
Regulatory status
| Lifecycle | Most U.S. patent protections for the API expired between 2020 and early 2023, indicating that the product has transitioned into a mature market phase. With commercialization across Canada, the US, and the EU, the API is broadly established and likely subject to increased generic competition. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Tofacitinib was introduced by a single originator company, with subsequent supply in Canada, the US, and the EU through multiple branded generic versions, indicating a well‑established global market presence. The numerous brand samples from different manufacturers reflect an active post‑originator supply landscape. US patents expired between 2020 and 2023, supporting the availability of generics and continued expansion of non‑originator manufacturing. |
|---|
Safety
| Toxicity | Minimum lethal dose in rat: 500 mg/kg. Maximum asymptomatic dose in non human primate: 40 mg/kg. Lymphatic, immune system, bone marrow and erythroid cell toxicity was seen in animal studies involving rate and monkeys. Doses used in these studies ranged from 1mg/kg/day to 10mg/kg/day, over a duration of 6 weeks to 6 months. Lymphopenia, neutropenia, and anemia is seen in human subjects and may call for an interruption or discontinuation of therapy if severe. Reduced female fertility in rats was seen at exposures 17 times the maximum recommended human dose. Fertility may be impaired in human females and harm may be caused to unborn child. Carcinogenic potential is seen, however evidence for dose dependency is lacking. Because the janus kinase pathway plays a role in stimulating the production of red blood cells and is involved in immune cell function, inhibition of this pathway leads to increased risk of anemia, neutropenia, lymphopenia, cancer and infection. Lymphopenia, neutropenia, and anemia in human subjects may call for an interruption or discontinuation of therapy if severe. Role of JAK inhibition in the development of gastrointestinal perforation is not known. |
|---|
- Animal studies indicate dose‑dependent hematopoietic and immune toxicity, with lymphopenia, neutropenia, and anemia observed in rats and non‑human primates at 1–10 mg/kg/day
- Human data reflect similar cytopenic profiles
- Reproductive and developmental risks include reduced female fertility in rats at high exposures and potential embryo–fetal toxicity
Tofacitinib 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.
Tofacitinib (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.
Tofacitinib API manufacturers & distributors
Compare qualified Tofacitinib API suppliers worldwide. We currently have 15 companies offering Tofacitinib 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 |
|---|---|---|---|---|---|
| ACE Japan | Producer | Japan | Japan | CoA | 76 products |
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, MSDS, USDMF | 229 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Dr. Sahu's Laboratories | Producer | India | India | BSE/TSE, CoA, GMP | 70 products |
| Hunan Ouya Biological Co.... | Producer | China | China | CoA | 7 products |
| Micro Labs | Producer | India | India | CoA, USDMF | 38 products |
| Minakem | Producer | France | Canada | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF | 31 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Qilu Tianhe | Producer | China | China | CoA, USDMF | 16 products |
| Senova Technology Co., Lt... | Producer | China | China | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, USDMF | 157 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, MSDS, USDMF | 757 products |
| Sintenovo | Producer | Spain | Spain | CoA, USDMF | 7 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
| Unichem Labs. | Producer | India | India | CoA, USDMF | 62 products |
When sending a request, specify which Tofacitinib 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 Tofacitinib 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 Tofacitinib API
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