Request Demo

Last update 15 Apr 2025

Leflunomide

Last update 15 Apr 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

5-Methyl-N-(4-(trifluoromethyl)phenyl)-4-isoxazolecarboxamide, 5-Methylisoxazole-4-carboxylic acid (4-trifluoromethyl)anilide, alpha,alpha,alpha-Trifluoro-5-methyl-4-isoxazolecarboxy-p-toluidide

+ [16]

Target

DHODH

Action

inhibitors

Mechanism

DHODH inhibitors(Dihydroorotate dehydrogenase inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesSkin and Musculoskeletal Diseases

Active Indication

Arthritis, PsoriaticRheumatoid Arthritis

Inactive Indication

Renal transplant rejectionSystemic Lupus ErythematosusViremia

Originator Organization

Sanofi

Active Organization

Zentiva ks

Suzhou Changzheng Cinkate Pharmaceutical Co., Ltd.

Sanofi-Aventis Deutschland GmbH

+ [7]

Inactive Organization

Teva Pharmaceuticals Europe BVTeva Pharmaceuticals USA, Inc.

Sanofi

Drug Highest PhaseApproved

First Approval Date

United States (10 Sep 1998),

Rheumatoid Arthritis

Regulation-

Structure/Sequence

Molecular FormulaC12H9F3N2O2

InChIKeyVHOGYURTWQBHIL-UHFFFAOYSA-N

CAS Registry75706-12-6

130

Clinical Trials associated with Leflunomide

NCT06923488

/ Not yet recruitingPhase 1/2IIT

Phase I/II Study of Leflunomide in Combination With Decitabine for Treatment of Relapsed or Refractory (R/R) Myelodysplastic Syndromes (MDS)

The goal of this interventional clinical trial is to evaluate the safety and tolerability of leflunomide in combination with decitabine as treatment for patients with relapsed or refractory myelodysplastic syndromes (R/R MDS).
The main question this study aims to answer are to evaluate and estimate the maximum tolerated doses and/or biologically active doses of the combination of leflunomide-decitabine in participants.
Decitabine will be administered at a dose of 20 mg/m2 by continuous intravenous infusion over one hour repeated daily for 5 days with repeating cycle every 4 weeks. Leflunomide is administered orally at 10 to 20 mg once daily (without a loading dose) for 14 to 21 days, as part of a 28-day treatment cycle in adult subjects with R/R MDS. After 12 cycles (study duration) responding patients can continue progression with the assigned doses.

Start Date01 May 2025

Sponsor / Collaborator

West Virginia University

NCT06714461

/ Not yet recruitingNot Applicable

Post Authorization Safety Study on Assessment of Effectiveness of Additional Risk Minimization Measures Related to ARAVA® (Leflunomide) in Saudi Arabia

The main objective of this post-authorization safety study is to assess healthcare professionals' awareness, knowledge, and behavior related to receipt and reading of the Direct Healthcare Professional Communication and educational materials for ARAVA® (leflunomide) and of the additional risk minimization measures.

Start Date15 Apr 2025

Sponsor / Collaborator

Sanofi

EUCTR2017-001079-22-NL

/ Unknown statusPhase 3

A multicenter randomized placebo controlled treatment study of leflunomide in polymyalgia rheumatica - Leflunomide in PMR

Start Date22 Jul 2024

Sponsor / Collaborator

University Medical Center Groningen

100 Clinical Results associated with Leflunomide

100 Translational Medicine associated with Leflunomide

100 Patents (Medical) associated with Leflunomide

5,042

Literatures (Medical) associated with Leflunomide

01 Jun 2025·INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

A new perspective on the antimicrobial mechanism of linezolid against Staphylococcus aureus revealed by proteomics and metabolomics analysis

Article

Author: Wang, Longlong ; Zhu, Jianguo ; Ma, Shiwei ; Xie, Weile ; Luo, Dan ; Wang, Zhe

Understanding bacterial responses to antimicrobials is crucial for identifying tolerance mechanisms and for developing new therapies. Using mass spectrometry-based metabolomics and proteomics, this study examines the response of Staphylococcus aureus to linezolid (LZD) treatment. Under LZD stress, significant fluctuations were observed in key metabolic pathways such as amino acid biosynthesis and the TCA cycle, alongside a general increase in ribosomal protein complexes. Additionally, LZD disrupted nucleotide metabolism, particularly affecting pyrimidine pathways. Combining LZD with the pyrimidine synthesis inhibitor leflunomide enhanced bactericidal effects both in vitro and in vivo, highlighting the importance of targeting pyrimidine biosynthesis to amplify the antimicrobial efficacy of protein inhibitors. These results underscore downstream metabolic processes as viable targets for synergistic drug combinations, suggesting a strategy to potentially improve the clinical effectiveness of LZD.

01 May 2025·EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS

Intradermal delivery of teriflunomide loaded emulsomes using hollow microneedles for effective minimally invasive psoriasis management

Article

Author: Abbas, Haidy ; Zewail, Mariam ; Abd-El-Azim, Heba ; Sayed, Nesrine El

Conventional topical psoriasis treatments suffer from limited delivery to affected areas along with skin irritation due to high local drug concentration. Herein an attempt to improve the delivery of leflunomide's active metabolite (teriflunomide (TER)) by improving its solubility through nanoencapsulation in emulsomes (EMLs) besides ensuring effective intradermal delivery using hollow microneedles. Evaluation of colloidal characteristics of EMLs, encapsulation efficiency and drug release were performed. Additionally, the antipsoriatic activity in an imiquimod-induced psoriatic mouse model was evaluated by the measurement of inflammatory mediators' levels and histopathological assessment of anatomized skin. The particle size of the chosen EMLs formulation was 147.9 nm and the zeta potential value was -21.7. Entrapment efficiency was 97.23 % and EMLs provided sustained drug release for 48 h. No statistically significant differences in the in vivo levels of NF-KB, IL 8, MMP1, GSH, SOD and catalase between the animals treated by TER-EMLs and the negative control cohort were observed. Also, histopathological inspection of dissected skin samples reflected the superiority of TER-EMLs over TER suspension. Collectively, combining nanoencapsulation and hollow microneedles application improved TER properties and ensured effective TER delivery to the affected psoriatic areas.

01 Apr 2025·INTERNATIONAL JOURNAL OF DERMATOLOGY

Acneiform lesions in a 57‐year‐old woman

Article

Author: Sulejmani, Pranvera ; Amber, Kyle ; Medhus, Emily J. ; Bittar, Julie ; Baczynski, Alexandra

Abstract:

A 57‐year‐old woman on leflunomide with a history of chronic obstructive pulmonary disease and rheumatoid arthritis presented with multiple flesh‐colored to hyperpigmented dome‐shaped papules, scattered comedones, and underlying scarring on bilateral cheeks and chin. These dermatologic manifestations, laboratory evaluation, and punch biopsy led to a final diagnosis of acneiform or comedonal discoid lupus erythematosus (ACDLE). For patients with acneiform or comedonal lesions, ACDLE should be considered if the lesions do not improve with conventional treatment for acne vulgaris.

News (Medical) associated with Leflunomide

12 Mar 2025

·www.prnewswire.com

Psoriatic Arthritis Market Sees Major Shift with Growing Biosimilar Adoption | DelveInsight

The arrival of biosimilars like Celltrion's STEQEYMA and Biocon's YESINTEK is shaking up the psoriatic arthritis market, challenging blockbuster biologics with cost-effective alternatives. As competition intensifies, these biosimilars are reshaping treatment choices and driving a shift in the market landscape. LAS VEGAS, March 12, 2025 /PRNewswire/ -- Psoriatic arthritis (PsA) is a chronic inflammatory condition that affects approximately 112 per 100,000 adults worldwide. It is more prevalent in Europe and North America than in Asia and South America. In patients with psoriasis, the prevalence of psoriatic arthritis can range from 6% to 34% in Western populations. Despite its impact, many individuals with psoriatic arthritis remain undiagnosed or receive inadequate treatment, highlighting the need for increased awareness and access to specialized care. As per DelveInsight analysis, among the 7MM, the United States accounted for the highest number of prevalent cases of psoriatic arthritis in 2023, and these cases are expected to increase by the end of 2034 due to several key factors such as an increase in awareness and diagnosis, as well as the rapid prevalence of PsA. Psoriatic arthritis, occurring in approximately 20% of individuals with psoriasis, is a chronic inflammatory arthritis intricately linked to psoriatic arthritis. This aggressive condition is characterized by potential significant morbidity and compromised quality of life. Treatment approaches for psoriatic arthritis encompass a variety of strategies aimed at managing symptoms, slowing disease progression, and improving the overall quality of life. These approaches typically involve a combination of pharmacological therapies, lifestyle modifications, and, in severe cases, surgical interventions. Psoriatic arthritis treatment is highly individualized based on disease severity, response to therapy, and patient preferences, with multidisciplinary care from rheumatologists, dermatologists, and physical therapists playing a key role. Pharmacological treatment for psoriatic arthritis primarily targets inflammation and pain relief. Nonsteroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen and naproxen, are often the first line of defense, helping to reduce pain and inflammation. Disease-modifying antirheumatic drugs (DMARDs) like methotrexate, sulfasalazine, and leflunomide are commonly prescribed to prevent joint damage and suppress the inflammatory process. For individuals with mild-to-moderate psoriatic arthritis, oral small molecules (OSMs) like OTEZLA (apremilast) offer a convenient, non-injectable option by modulating inflammatory pathways. Biologic agents have revolutionized the treatment landscape for psoriatic arthritis. These medications specifically inhibit key molecules in the inflammatory cascade. TNF inhibitors like HUMIRA (adalimumab), ENBREL (etanercept), and REMICADE (infliximab) are frontline biologics that target tumor necrosis factor, a crucial driver of inflammation. Patients who do not respond to TNF inhibitors may benefit from IL-17 inhibitors like COSENTYX (secukinumab) and TALTZ (ixekizumab) or IL-12/23 inhibitors such as STELARA (ustekinumab). Learn more about the FDA-approved psoriatic arthritis drugs @ Drugs for Psoriatic Arthritis Treatment SKYRIZI (risankizumab), developed by AbbVie, is a humanized IgG1 monoclonal antibody that acts as an interleukin-23 (IL-23) antagonist. It can be used on its own or in conjunction with non-biologic DMARDs. In June 2022, the FDA approved SKYRIZI as the first and only targeted IL-23 inhibitor for adults with active psoriatic arthritis. Another biologic, TREMFYA (guselkumab by Janssen), was approved by the FDA in July 2020 as the first monoclonal antibody that selectively binds to the p19 subunit of IL-23, further expanding treatment options for psoriatic arthritis patients. BIMZELX (bimekizumab), developed by UCB Biopharma, is a humanized monoclonal antibody that targets IL-17A and IL-17F. It received European Commission approval in June 2023 for adults with active psoriatic arthritis and axial spondyloarthritis. On September 23, 2024, the FDA approved BIMZELX for treating adults with active psoriatic arthritis, non-radiographic axial spondyloarthritis (nr-axSpA) with objective inflammation, and active ankylosing spondylitis. In Phase III studies, BIMZELX showed meaningful responses in patients with inadequate TNF inhibitor responses and those new to biologics, indicating its potential as an important treatment option for psoriatic arthritis. In cases where joint damage becomes severe and unresponsive to medical therapies, surgical interventions like joint replacement surgery may be necessary to restore function and alleviate pain. Lifestyle changes, such as regular exercise, joint protection techniques, and weight management, are also critical in managing psoriatic arthritis, as excess weight can worsen symptoms and increase disease severity. The treatment landscape for psoriatic arthritis continues to evolve, offering hope to patients with more targeted therapies and improved outcomes. As companies like UCB Biopharma, AbbVie, and Janssen advance their biologic portfolios, the future looks promising for psoriatic arthritis management. The competition in the biosimilar market is intensifying as companies introduce cost-effective alternatives to blockbuster biologics. In December 2024, Celltrion announced FDA approval for STEQEYMA (ustekinumab-stba), a biosimilar to STELARA, for subcutaneous injection or intravenous infusion in adult and pediatric patients with plaque psoriasis and psoriatic arthritis, as well as adult patients with Crohn's disease and ulcerative colitis. Simultaneously, Biocon Biologics Ltd. is strengthening its position with positive Phase III results for YESINTEK, its biosimilar to ustekinumab, in adult patients with moderate to severe chronic plaque psoriasis. The pivotal randomized, double-blind, parallel-group study demonstrated comparable efficacy and safety to the reference biologic, STELARA, and the findings are being presented at the 2025 American Academy of Dermatology (AAD) Annual Meeting in Orlando, Florida. With the approval of STEQEYMA and the promising clinical outcomes for YESINTEK, these biosimilars are poised to challenge STELARA by offering cost-effective alternatives in key immunology indications. As pricing pressures and healthcare sustainability concerns drive the demand for biosimilars, these developments mark a significant shift in the treatment landscape, providing greater accessibility and affordability for patients while increasing competition in the immunology market. To know more about psoriatic arthritis treatment options, visit @ New Treatment for Psoriatic Arthritis The psoriatic arthritis market is buzzing with numerous companies advancing treatments to cater to the growing patient base. Several therapies are expected to enter the market during the forecast period, providing new hope for patients. Some of these potential therapies include ACELYRIN Inc.'s Izokibep, Novartis Pharmaceuticals' Secukinumab, UCB Biopharma SRL's Bimekizumab, and Bristol-Myers Squibb's Deucravacitinib. Additionally, AbbVie's Upadacitinib and Risankizumab, as well as Eli Lilly and Company's Ixekizumab, are also part of the promising pipeline. Other noteworthy therapies include Sun Pharma's ILUMYA/ILUMETRI, Bristol-Myers Squibb's SOTYKTU, and Affibody's Izokibep in collaboration with Acelyrin and Inmagene. With these advancements, the psoriatic arthritis treatment landscape is set for a major shift, offering patients more tailored and effective options. The companies involved in developing biosimilars include Alvotech, Teva, Biocon Biologics, Celltrion, Fresenius Kabi, and others. Discover which therapies are expected to grab major psoriatic arthritis market share @ Psoriatic Arthritis Market Report ILUMYA/ILUMETRI by Sun Pharma is an interleukin-23 (IL-23) inhibitor classified as a humanized, anti-IL-23p19 monoclonal antibody. It works by blocking inflammatory proteins (cytokines and chemokines) in the body. By inhibiting the effects of IL-23, ILUMYA helps control the release of other inflammatory proteins, including IL-17 and TNF-α. This mechanism reduces inflammation, decreases the number of inflammatory cells in psoriatic lesions, helps prevent plaque formation, and resolves tissue damage. The drug is currently undergoing evaluation in Phase III clinical development, actively recruiting subjects with active psoriatic arthritis who have prior exposure to anti-TNF agents, as well as those who are anti-TNF naïve. SOTYKTU, developed by Bristol-Myers Squibb, is the first and only novel oral selective tyrosine kinase 2 (TYK2) inhibitor being studied across multiple immune-mediated diseases. Deucravacitinib binds to the regulatory domain of the TYK2 enzyme, inhibiting its activation. This selective inhibition reduces the release of proinflammatory cytokines and chemokines, helping to control the inflammation associated with psoriatic arthritis and alleviating its signs and symptoms. Currently, the drug is being investigated for the treatment of psoriatic arthritis in a Phase III clinical trial. Izokibep, developed by Affibody in partnership with Acelyrin and Inmagene, is a unique antibody mimetic and a novel bispecific agent that potentially targets both subunits of the IL-17A homo-dimer and serum albumin. Affibody has entered into a partnership agreement with Acelyrin for the development and commercialization of izokibep and has completed a Phase II trial. As part of this agreement, Acelyrin obtained worldwide rights to izokibep, excluding selected Asian countries, where rights have been granted to Inmagene Biopharmaceuticals. In March 2024, Acelyrin announced the release of positive top-line results from the Phase IIb/III trial, indicating that izokibep was well-tolerated with a favorable safety profile. This drug is currently in Phase III clinical trial. Discover more about drugs for psoriatic arthritis in development @ Psoriatic Arthritis Clinical Trials The anticipated launch of these emerging therapies for psoriatic arthritis is poised to transform the market landscape in the coming years. As these cutting-edge treatments continue to mature and gain regulatory approval, they are expected to reshape the psoriatic arthritis market landscape, offering new standards of care and unlocking opportunities for medical innovation and economic growth. DelveInsight estimates that the psoriatic arthritis market size was USD 9 billion in 2021 and is expected to grow significantly in the coming years. This growth can be attributed to the introduction of upcoming therapies and the rising prevalence of the condition. The anticipated launch of these therapies is also expected to attract new entrants to the psoriatic arthritis market, resulting in increased competition and innovation. DelveInsight's latest published market report titled " Psoriatic Arthritis Market Insight, Epidemiology, and Market Forecast – 2034" will help you discover which market leader is set to capture the largest market share. The report provides comprehensive insights into country-specific treatment guidelines, patient pool analysis, and epidemiology forecasts to help understand key opportunities and assess the market's underlying potential. The psoriatic arthritis market report offers epidemiological analysis for the study period 2020–2034 in the 7MM, segmented into: Total Prevalent Cases of Psoriatic Arthritis Total Diagnosed Prevalent Cases of Psoriatic Arthritis Gender-specific Diagnosed Prevalent Cases of Psoriatic Arthritis Severity-specific Diagnosed Prevalent Cases of Psoriatic Arthritis The report provides an edge while developing business strategies by understanding trends shaping and driving the 7MM Psoriatic Arthritis market. Highlights include: 10-year Forecast 7MM Analysis Epidemiology-based Market Forecasting Historical and Forecasted Market Analysis upto 2034 Emerging Drug Market Uptake Peak Sales Analysis Key Cross Competition Analysis Industry Expert's Opinion Access and Reimbursement Download this psoriatic arthritis market report to assess the epidemiology forecasts, understand patient journeys, gain insights into KOLs' opinions about upcoming treatment paradigms, and identify the factors contributing to changes in the psoriatic arthritis market. Additionally, stay informed about the mitigating factors that can enhance your market position in the psoriatic arthritis therapeutic space. Related Reports Psoriatic Arthritis Pipeline Psoriatic Arthritis Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key schizophrenia companies, including Affibody, Kymera, Selection Therapeutics GmbH, Jiangsu HengRui Medicine Co., Ltd., Nimbus Lakshmi, Inc., Hansoh BioMedical R&D Company, Bio-Thera Solutions, ACELYRIN Inc., among others. Psoriatic Arthritis Epidemiology Forecast Psoriatic Arthritis Epidemiology Forecast – 2034 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, and Psoriatic Arthritis epidemiology trends. Ankylosing Spondylitis Market Ankylosing Spondylitis Market Insights, Epidemiology, and Market Forecast – 2034 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key Ankylosing Spondylitis companies, including UCB, AbbVie, Pfizer, Astella, Amgen, Janssen Biotech, Pozen, Novartis, Iroko Pharmaceuticals, Syntex Pharmaceuticals, Horizon Pharma, Eli Lilly and Company, among others. Psoriasis Market Psoriasis Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key Psoriasis companies, including Amgen, Janssen, Abbvie, Novartis, AstraZeneca, Bausch Health, Eli Lilly, Sun Pharmaceutical, Janssen Biotech, UCB Inc., LEO Pharma, Promius Pharma, Mayne Pharma, Bausch Health Companies, MC2 Therapeutics, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Phase 3Drug ApprovalClinical ResultPhase 2

14 Mar 2024

·www.prnewswire.com

Psoriasis in America - Insights into Psoriasis Patient Demographics, Quality of Life, Information-seeking Behaviors, HCP Engagement and Treatment Experiences

DUBLIN, March 14, 2024 /PRNewswire/ -- The "Psoriasis in America 2023: Understanding the Psoriasis Patient Experience" report has been added to ResearchAndMarkets.com's offering. Approximately 7.5 million people in the United States have psoriasis. This Psoriasis in America report provides a comprehensive look at life for those living with psoriasis. Using detailed quantitative data, it gives a full picture of the psoriasis patient experience - from symptoms to treatment to HCP relationships to quality of life - so you can make informed, strategic decisions, identify opportunities, and understand potential challenges. The report offers an in-depth look at the psoriasis patient experience. This large-scale, patient-reported data leverages vital quantitative insights essential to understanding key touchpoints in the psoriasis patient journey, including condition management, HCP engagement, quality of life, treatment experience and satisfaction, and much more. This report lifts the curtain on life with psoriasis, giving stakeholders an actionable look at the behaviors, attitudes, perceptions, needs, and experiences of people living with the condition. Data can be used to inform strategic decisions, including product communications, competitive assessments, concept development, landscape analyses, patient journey overlays, and forecasting inputs. This report also addresses important questions that stakeholders may not even know to ask while offering valuable insights into must-have patient-reported data points not available anywhere else. Add-on custom data analysis opportunities are also available for an additional cost - please see the report following purchase for more information. The analyst reaches millions of people through its portfolio of 45+ condition-specific online health communities - including PlaquePsoriasis.com - to provide information, connection, and support to patients and caregivers in the U.S. This report includes a deep-dive into: Psoriasis patient demographics Age, gender, ethnicity, marital status, children, employment status, income, location, insurance, and other health conditions Impact of psoriasis on quality of life Severity, impact on quality of life, symptoms experienced, and what patients wish others better understood Information-seeking behaviors Information sources used, plus topics of interest HCP engagement Primary HCP seen for condition, satisfaction with HCP, and discussion about brands aware of/not used Psoriasis treatment awareness and experiences Aided awareness of specific treatments, treatment experience, satisfaction with current treatments, perceived control with current treatment plan, and interest/participation in clinical trials Key questions answered in this report: To what extent do people say psoriasis impacts their overall quality of life? What's the average number of flares in the past year? What do patients wish others understood about psoriasis? What percentage of patients see a specialist for psoriasis treatment? What treatments have the highest aided brand awareness among patients? What percentage of patients use a biologic? How many patients feel their psoriasis is well-controlled on their current treatment plan? What percentage of patients are likely to switch or add new treatments in the next six months? What medications have patients discussed with their HCP? What are the top online resources people with psoriasis use to find information? What kinds of content and information do patients search for? What percentage of patients search for information on treatment options? Methodology Psoriasis in America consists of: A 20-minute online quantitative survey, covering demographics, comorbidities, quality of life/impact, HCP interactions, as well as treatment awareness, experiences, and discussions Qualitative patient insights from open-ended responses Additional details: Fielded: January 16, 2023 to April 14, 2023 Convenience sample of 490 respondents diagnosed with psoriasis Respondents are age 18+, living in the U.S., and are recruited from proprietary online health communities and recruiting partners Key Topics Covered: Respondent Demographics Research Highlights Condition Status and Quality of Life Severity and Exacerbations Symptoms Experienced Impact on Quality of Life Qualitative Patient Insights Information-Seeking Behaviors Resources Used to Manage Health Types of Content/Information Sought Treatment Awareness and Experiences Primary HCP Seen for Psoriasis Care Aided Brand Awareness of Treatments Treatment Usage Condition Control on Current Treatment and Clinical Trial Interest Treatment Discussions with HCP Appendix with All Data Charts and Distributions Brands and treatments mentioned in this report include: Topical corticosteroid (such as hydrocortisone) BRYHALIT (halobetasol propionate) lotion DesOwen (desonide) SERNIVOT (betamethasone dipropionate) SORILUXT Foam (calcipotriene) TACLONEX (calcipotriene and betamethasone) TAZORAC (tazarotene) VECTICAL (calcitriol) VTAMA (tapinarof) ZITHRANOLT-RR (anthralin) ZORYVET (roflumilast) Acitretin (SORIATANE) ARAVA (leflunomide) Azathioprine (such as IMURAN, AZASAN) Cyclosporine (such as Sandimmune, NEORAL, RESTASIS) Methotrexate (eg, Rheumatrex), also sometimes given as an injection OTEZLA (apremilast) PLAQUENIL (hydroxychloroquine) RINVOQ (upadacitinib) SOTYKTUT (deucravacitinib) Sulfasalazine (Azulfidine) XELJANZ/XELJANZ XR (tofacitinib citrate) AMJEVITAT (adalimumab-atto) Hide until launched in US AVSOLA (infliximab-axxq) CIMZIA (certolizumab) COSENTYX (secukinumab) CYLTEZO (adalimumab-adbm) Hide until launched in US ENBREL (etanercept) ERELZIT (etanercept-szzs) Hide until launched in US HULIO (adalimumab-fkjp) Hide until launched in US HUMIRA (adalimumab) HYRIMOZ (adalimumab-adaz) Hide until launched in US ILUMYAT (tildrakizumab-asmn) INFLECTRA (infliximab-dyyb) IXIFIT (infliximab-qbtx) Hide until launched in US ORENCIA (abatacept) REMICADE (infliximab) RENFLEXIST (infliximab-abda) SIMPONI (golimumab) SIMPONI ARIA (golimumab for infusion) SILIQT (brodalumab) SKYRIZI (risankizumab-rzaa) STELARA (ustekinumab) TALTZ (ixekizumab) TREMFYA (guselkumab) For more information about this report visit About ResearchAndMarkets.com ResearchAndMarkets.com is the world's leading source for international market research reports and market data. We provide you with the latest data on international and regional markets, key industries, the top companies, new products and the latest trends. Media Contact: Research and Markets Laura Wood, Senior Manager [email protected] For E.S.T Office Hours Call +1-917-300-0470 For U.S./CAN Toll Free Call +1-800-526-8630 For GMT Office Hours Call +353-1-416-8900 U.S. Fax: 646-607-1907 Fax (outside U.S.): +353-1-481-1716 Logo: SOURCE Research and Markets

23 Nov 2023

·synapse.patsnap.com

What are DHODH inhibitors and how do you quickly get the latest development progress?

DHODH, or dihydroorotate dehydrogenase, is a kind of iron-containing flavin-dependent mitochondrial enzyme, which is a key enzyme in the catalysis of nucleic acids for pyrimidine synthesis, catalyzing the fourth step in the de novo biosynthetic pathway of pyrimidines. As an enzyme associated with the electron transfer chain, DHODH connects mitochondrial energy, cell proliferation, ROS production, and apoptosis of certain cell types. Depletion of DHODH also leads to an increase in ROS production, reduction in membrane potential, and slow cell growth. Blocking the DHODH synthesis pathway can effectively inhibit the proliferation of activated immune cells and the secretion of cytokines, thereby suppressing cytokine storms caused by diseases. At the same time, inhibiting DHODH activity significantly reduces nucleoside raw materials, hinders viral nucleic acid synthesis, inhibits viral replication, has broad-spectrum antiviral activity, and is not easy to cause drug-resistant mutations. DHODH is a validated therapeutic target that can be used to treat autoimmune diseases, including rheumatoid arthritis and multiple sclerosis. Now the field of drug development for DHODH inhibitors is full of new opportunities. Leflunomide is the first FDA-approved DHODH inhibitor. It is a synthetic isoxazole compound developed by Sanofi. In 1998, the FDA approved the market launch application for leflunomide for the treatment of rheumatoid arthritis, lupus nephritis, and psoriatic arthritis. The listing of leflunomide is based on the Phase III US301 trial. The research results show that leflunomide has comparable clinical efficacy and tolerability with methotrexate and sulfasalazine, and has better efficacy and tolerability compared with placebo. Among 482 patients initially treated, the response rate reached 52%. Teriflunomide is also a DHODH inhibitor developed by Sanofi. In 2012, the FDA approved its market launch. Teriflunomide inhibits the rapid differentiation of T cells, thereby slowing the progression of multiple sclerosis. Based on the global phase III clinical trial TEMSO study with thousands of cases, teriflunomide reduced the annual relapse rate of multiple sclerosis by 31% compared to placebo. In addition, teriflunomide also has antiviral effects on several viruses, including CMV, HSV1, and BK virus. It inhibits viral replication by interfering with the formation of nucleocapsids and virus particle assembly. The analysis of the target DHODH reveals a competitive landscape with multiple companies actively involved in the research and development of drugs. Sanofi, Immunic, Inc., PTC Therapeutics, Inc., and Aslan Pharmaceuticals Ltd. are among the companies with the highest number of drugs in various stages of development. The indications for DHODH-targeting drugs cover a wide range of diseases and conditions, indicating their potential therapeutic applications. Small molecule drugs and unknown drugs are progressing rapidly, suggesting ongoing efforts to develop innovative compounds and identify new drug candidates. The United States, European Union, China, and other countries have made significant progress in the development of DHODH-targeting drugs, indicating a global interest in this target. Overall, the target DHODH presents a promising opportunity for the pharmaceutical industry, with potential for further growth and development in the future. The mechanism of action of DHODH inhibitorsDHODH inhibitors are a type of drugs that target and inhibit the enzyme dihydroorotate dehydrogenase (DHODH). DHODH is an enzyme involved in the de novo pyrimidine biosynthesis pathway, which is essential for the production of DNA and RNA in cells. By inhibiting DHODH, these inhibitors disrupt the synthesis of pyrimidine nucleotides, which are crucial for cell proliferation and growth. From a biomedical perspective, DHODH inhibitors have shown potential in the treatment of various diseases, including cancer, autoimmune disorders, and viral infections. In cancer, these inhibitors can inhibit the growth of tumor cells by blocking their ability to produce DNA and RNA, thereby impeding their proliferation. In autoimmune disorders, DHODH inhibitors can modulate the immune response by suppressing the proliferation of immune cells involved in the disease process. Additionally, DHODH inhibitors have been investigated as antiviral agents, particularly against RNA viruses, by interfering with their replication and propagation. Overall, DHODH inhibitors represent a class of drugs that target an important enzyme involved in nucleotide synthesis, making them potential candidates for therapeutic interventions in various disease conditions. List of DHODH InhibitorsThe currently marketed DHODH inhibitors include: TeriflunomideLeflunomidePTC-299Vidofludimus calciumBrequinar SodiumFarudodstatKIO-101RP-7214Teriflunomide SodiumVidofludimusFor more information, please click on the image below. What are DHODH inhibitors used for?Currently, in clinical practice, DHODH inhibitors are mainly used for autoimmune diseases such as Rheumatoid Arthritis, Lupus Nephritis, and Multiple Sclerosis. Multiple in vitro and clinical studies have shown that drugs that inhibit DHODH have anti-inflammatory, anti-tumor, anti-malaria parasite, and antiviral effects. For more information, please click on the image below to log in and search. How to acquire the most recent advancement in DHODH inhibitors?In the Synapse database, you can keep abreast of the latest research and development advances of DHODH inhibitors anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

100 Deals associated with Leflunomide

External Link

KEGG	Wiki	ATC	Drug Bank
D00749	Leflunomide	L04AA13	DB01097

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Arthritis, Psoriatic	European Union	Sanofi-Aventis Deutschland GmbH	02 Sep 1999
Arthritis, Psoriatic	Iceland	Sanofi-Aventis Deutschland GmbH	02 Sep 1999
Arthritis, Psoriatic	Liechtenstein	Sanofi-Aventis Deutschland GmbH	02 Sep 1999
Arthritis, Psoriatic	Norway	Sanofi-Aventis Deutschland GmbH	02 Sep 1999
Rheumatoid Arthritis	United States	Sanofi-Aventis U.S. LLC	10 Sep 1998

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Renal transplant rejection	Phase 2	United States	Suzhou Changzheng Cinkate Pharmaceutical Co., Ltd.	01 Jul 2012
Viremia	Phase 2	United States	Suzhou Changzheng Cinkate Pharmaceutical Co., Ltd.	01 Jul 2012
Systemic Lupus Erythematosus	Phase 2	Hong Kong	Sanofi	01 Jan 2003

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02451748 (CTgov)	Phase 4	Rheumatoid Arthritis	32	Lab Work (DMARD's Responder and Non-Responder)	awoldsupzf(hwtcolgfwj) = iizzraxdfj mmzoiacgqi (wxnnarjfuc, mbdrmqnoja - tjixwcumsv) View more	-	10 Jul 2024
				Naproxen+Medrol+Hydroxychloroquine+humira+Prednisone+Lab Work+Triamcinolone+Sulfasalazine+Certolizumab pegol (CDP870, tradename Cimzia)+Methotrexate+Leflunomide (DMARD's Plus Cimzia (Certolizumab Pegol))	dqwoybfeoy(axallvauhs) = qvojfbqouz dhwkfixxmg (zklidmxvgs, 0.132) View more
EULAR2024	Not Applicable	-	51	Methotrexate	ldxzdpjjex(xnrlfxohst) = There was only one abnormality of low platelet count of 110 x 109/L two weeks after starting sulfasalazine and it was stopped. pyjyubvnxl (gqthdopwly )	-	05 Jun 2024
				Sulfasalazine
ATS2024	Not Applicable	Rheumatoid arthritis with rheumatoid lung disease	-	Leflunomide 20mg/day	fbatqoovqn(ticbgtvfox) = pulmonary nodulosis due to the use of leflunomide was suggested. After discontinuation of the drug, there was a significant improvement in the nodular lesions with remission of the hemoptysis rpozalftrv (nntsmvpnvr ) View more	-	19 May 2024
NCT04212416 (Tandem Meetings ASTCT and CIBMTR2024) Manual	Phase 1	Chronic graft-versus-host disease	18	Leflunomide 20mg	cwrfekdkjt(orjgghlocv) = GI (diarrhea: 27%, nausea/vomiting: 5%, abdominal pain: 5%), cytopenias (anemia: 16%, leukopenia: 11%), hepatic failure (5%), lab abnormalities (AST/ALT increase: 11%, bilirubin increase: 5%), fatigue (11%), and headache (5%). rxfmloanrt (kpxdbogota ) View more	Positive	01 Feb 2024
NCT04463615 (CTgov)	Phase 2	Refractory Lymphoproliferative Disorder	1	Leflunomide	fskqvynmgr = lntemdosgk xwhslgkebd (arncyjbrzg, nvbbwxtjpl - triwskzeym) View more	-	05 Dec 2023
NCT02509052 (CTgov)	Phase 1/2	Recurrent Multiple Myeloma \| Relapse multiple myeloma \| Refractory Multiple Myeloma	12	Pharmacological Study+Leflunomide (Arm 1: 20 mg Leflunomide)	xmhkufwiwr = wadyiievuu stbmovegig (veyfnoljvf, llxzmlituh - rcmxqdetwr) View more	-	10 Oct 2023
				Pharmacological Study+Leflunomide (Arm 2: 40 mg Leflunomide)	xmhkufwiwr = vxapajlous stbmovegig (veyfnoljvf, hbnqvdxgcd - oygxqxyzrq) View more
NCT04508790 (IMS2023)	Phase 2	Relapse multiple myeloma	11	Leflunomide	irdowyujaj(kzsirfbrkf) = zdasrmgqcs leiawuvwcb (ggqiujpkvs ) View more	-	26 Sep 2023
NCT01619176 (CTgov)	Not Applicable	Rheumatoid Arthritis	10	non-steroidal anti-inflammatory drug (NSAID)+methotrexate+leflunomide (Acupuncture)	eotyaodskm = nheigmagxu olmqxbxcgq (isqylmozkp, paozcfkmxp - fvpfeffbur) View more	-	08 Sep 2023
				non-steroidal anti-inflammatory drug (NSAID)+methotrexate+leflunomide (Control)	eotyaodskm = fewlfapcnu olmqxbxcgq (isqylmozkp, spccdlhgnt - tccheuscev) View more
NCT05007678 (DEFEAT-COVID, Pubmed \| BMJ Open)	Phase 3	COVID-19	214	Leflunomide + Standard-of-care treatment	oevtmzphym(vrctbnfuqt) = hpcrmvocsv bzzxnvxpfw (nktdorpbil ) View more	-	13 Apr 2023
				Leflunomide (Standard-of-care treatment)	oevtmzphym(vrctbnfuqt) = utlhtfkamo bzzxnvxpfw (nktdorpbil ) View more
NCT01172002 (Pubmed \| Ann Rheum Dis)	Not Applicable	Lupus Nephritis Maintenance	270	Leflunomide	mqqyrqodhm(dmloepqenu) = vknoukzvwc aelrfowtws (ercdlbfvcg )	Positive	04 Jul 2022
				Azathioprine	mqqyrqodhm(dmloepqenu) = gtqvvnwkix aelrfowtws (ercdlbfvcg )

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis