Drugs / Leflunomide
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Leflunomide

also known as LEF · SU101 · Arava · Arthfree · HWA-486 · L04AA13 · Leflunomid · Leflunomida · +9 more

Small molecule targets DHODH via inhibition

Developed for
rheumatoid arthritis · autoimmune disease · psoriatic arthritis · smoldering plasma cell myeloma · central nervous system neoplasm · chronic graft versus host disease · COVID-19 · immunoglobulin A vasculitis
+40 more · melanoma · plasma cell myeloma · acute graft versus host disease · anti-neutrophil cytoplasmic antibody-associated vasculitis · bullous pemphigoid · chronic kidney disease · colorectal cancer · glioma · Her2-receptor negative breast cancer · HIV infectious disease · IgA glomerulonephritis · immunoglobulin G4-related sclerosing disease · lung cancer · lupus erythematosus · lupus nephritis · lymphoproliferative syndrome · malignant pancreatic neoplasm · multiple endocrine neoplasia type 1 · musculoskeletal system disorder · myelodysplastic syndrome · nephritis · neuroendocrine neoplasm · pancreatic ductal adenocarcinoma · polyarticular juvenile idiopathic arthritis · polyomavirus infectious disease · prostate cancer · pulmonary hemosiderosis · reactive arthritis · refractory malignant neoplasm · sarcoma · Sjogren syndrome · systemic lupus erythematosus · triple-negative breast carcinoma · uveitis · adult-onset Still disease · disease related to solid organ transplantation · juvenile idiopathic arthritis · myasthenia gravis · polymyalgia rheumatica · Takayasu arteritis
Investigated by
National Cancer Institute (NCI) · City of Hope Medical Center · Sanofi · Peking Union Medical College Hospital · Pfizer · Chinese PLA General Hospital
+59 more · Novum Pharmaceutical Research Services · Par Pharmaceutical, Inc. · Qilu Hospital of Shandong University · Second Affiliated Hospital, School of Medicine, Zhejiang University · Shanghai Zhongshan Hospital · Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University · Tata Memorial Centre · Teva Pharmaceuticals USA · The First Affiliated Hospital of Anhui Medical University · University of Erlangen-Nürnberg Medical School · Affiliated Hospital of Jilin University, Changchun,China · Agentschap voor Innovatie door Wetenschap en Technologie · AnHui ShengLi Hospital · Assistance Publique - Hôpitaux de Paris · Bangladesh Medical University · Beijing Shijitan Hospital, Capital Medical University · Cancer Institute and Hospital, Chinese Academy of Medical Sciences · Changhai Hospital · Changzheng-Cinkate · Charite University, Berlin, Germany · Chinese SLE Treatment And Research Group · Deborah Doroshow · First Affiliated Hospital of Kunming Medical University · First Affiliated Hospital of Wenzhou Medical University · Indian Council of Medical Research · Joseph Sparano · Karolinska University Hospital · Massachusetts General Hospital · N.N. Petrov National Medical Research Center of Oncology · NYU Langone Health · Nanjing Children's Hospital · National Eye Institute (NEI) · National Institute of Allergy and Infectious Diseases (NIAID) · P. Verschueren · Peking University · Peking University People's Hospital · RenJi Hospital · Sandoz · Second Affiliated Hospital of Nanchang University · Shanghai 10th People's Hospital · Shanxi Medical University · Shengjing Hospital · Shenzhen Second People's Hospital · Sichuan Province People's Hospital · The Affiliated Hospital of Inner Mongolia Medical University · The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School · The First Affiliated Hospital of Bengbu Medical University · The First Affiliated Hospital of Soochow University · The First Affiliated Hospital with Nanjing Medical University · The People's Hospital of Hebei Province · Tongji Hospital · University Hospital, Basel, Switzerland · University Hospital, Limoges · University of Chicago · University of Oxford · Uppsala University Hospital · West Virginia University · Zhejiang University · dfg

Regulatory milestones approvals, filings & regulatory actions · 4 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Label expansions (2) US (FDA) ARAVA — 2003-06-13 – 2004-03-05 fda.gov ↗
Approved EU (EMA) Arava — 1999-09-02 europa.eu ↗
Approved US (FDA) ARAVA — 1998-09-10 fda.gov ↗

Trials 61 · started per year

today
US approved 1998
EU approved 1999
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1997199819992000200120022003200420052006200720082009201020112012201320142015201620172018201920202021202220232024202520262027
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 01 trial
Phase 0 NCT04370483 Oct 2020 → Nov 2026 expected smoldering plasma cell myeloma City of Hope Medical Center Active not recruiting No outcome recorded
Phase 113 trials · 1 met primary
Phase 1 NCT06454383 May 2024 → Nov 2026 expected pancreatic ductal adenocarcinoma City of Hope Medical Center Recruiting No outcome recorded
Phase 1 NCT04997993 Dec 2023 → Jul 2027 expected Her2-receptor negative breast cancer Deborah Doroshow Recruiting No outcome recorded
Phase 1 NCT05443425 Jun 2023 → Jan 2027 expected acute graft versus host disease, hematopoietic and lymphoid system neoplasm City of Hope Medical Center Recruiting No outcome recorded
Phase 1 NCT04212416 May 2020 → Jun 2027 expected chronic graft versus host disease City of Hope Medical Center Active not recruiting No outcome recorded
Phase 1 NCT04361214 May 2020 → Jan 2022 COVID-19 University of Chicago Terminated No outcome recorded
Phase 1 NCT01611675 Jul 2012 → Jan 2014 melanoma Massachusetts General Hospital Terminated No outcome recorded
Phase 1 NCT00101374 Jan 2005 → May 2008 HIV infectious disease National Institute of Allergy and Infectious Diseases (NIAID) Completed No outcome recorded
Phase 1 NCT00653003 Dec 2003 → Jan 2004 — Par Pharmaceutical, Inc. Completed No outcome recorded
Phase 1 NCT00652665 Jun → Jul 2003 — Par Pharmaceutical, Inc. Completed No outcome recorded
Phase 1 NCT00946686 Sep 2002 psoriatic arthritis Sandoz Completed No outcome recorded
Phase 1/25 trials
Phase 1/2 NCT06923488 Jul 2025 → Oct 2027 expected myelodysplastic syndrome West Virginia University Recruiting No outcome recorded
Phase 1/2 NCT05937191 Jun 2023 → Dec 2026 expected pulmonary hemosiderosis Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University Recruiting No outcome recorded
Phase 1/2 NCT04532372 Jan → Aug 2021 COVID-19, cancer, hematopoietic and lymphoid cell neoplasm City of Hope Medical Center Completed No outcome recorded
Phase 1/2 NCT03709446 Apr 2019 → Nov 2025 triple-negative breast carcinoma Joseph Sparano Completed No outcome recorded
Phase 1/2 NCT02509052 Dec 2015 → Sep 2018 plasma cell myeloma City of Hope Medical Center Completed No outcome recorded
Phase 217 trials
Phase 2 NCT07138898 Dec 2025 → Jan 2028 expected rheumatic disorder NYU Langone Health Recruiting No outcome recorded
Phase 2 NCT07709013 Oct 2024 → Apr 2029 expected hematopoietic and lymphoid cell neoplasm Tata Memorial Centre Recruiting No outcome recorded
Phase 2 NCT06229340 Oct 2023 → Oct 2026 expected colorectal cancer, lung cancer, malignant pancreatic neoplasm, melanoma +1 N.N. Petrov National Medical Research Center of Oncology Recruiting No outcome recorded
Phase 2 NCT04932564 Sep 2023 → Jun 2024 chronic graft versus host disease, musculoskeletal system disorder Tata Memorial Centre Terminated No outcome recorded Stop: Enrollment
Phase 2 NCT05014646 Mar 2022 → Jan 2027 expected smoldering plasma cell myeloma City of Hope Medical Center Active not recruiting No outcome recorded
Phase 2 NCT05113004 Jan 2022 → Apr 2025 overdue Sjogren syndrome Assistance Publique - Hôpitaux de Paris Recruiting No outcome recorded
Phase 2 NCT04463615 May → Jul 2021 lymphoproliferative syndrome City of Hope Medical Center Completed No outcome recorded
Phase 2 NCT04508790 Nov 2020 → Feb 2027 expected plasma cell myeloma City of Hope Medical Center Recruiting No outcome recorded
Phase 2 NCT06540937 Jul 2020 → Dec 2024 overdue neuroendocrine neoplasm Cancer Institute and Hospital, Chinese Academy of Medical Sciences Recruiting No outcome recorded
Phase 2 NCT03952832 Dec 2019 → Jun 2021 smoldering plasma cell myeloma City of Hope Medical Center Withdrawn No outcome recorded
Phase 2/32 trials
Phase 2/3 NCT00268567 Oct 2002 → ? lupus nephritis Peking University Completed No outcome recorded
Phase 2/3 NCT00004071 Aug 1999 → Sep 2007 prostate cancer Pfizer Completed No outcome recorded
Phase 34 trials
Phase 3 NCT04610476 Oct 2020 → Oct 2024 psoriatic arthritis, substance withdrawal syndrome University of Erlangen-Nürnberg Medical School Unknown No outcome recorded
Phase 3 NCT02779114 Jan 2009 → Dec 2017 rheumatoid arthritis University of Erlangen-Nürnberg Medical School Unknown No outcome recorded
Phase 3 NCT00596206 Dec 2007 → Oct 2009 rheumatoid arthritis Sanofi Completed No outcome recorded
Phase 3 NCT00003293 Feb 1998 → May 2001 central nervous system neoplasm Pfizer Completed No outcome recorded
Phase 49 trials · 1 met primary · 1 missed
Phase 4 NCT07428551 Mar 2024 → Dec 2025 polyarticular juvenile idiopathic arthritis Bangladesh Medical University Completed No outcome recorded
Phase 4 NCT05626348 Dec 2021 → Jun 2025 overdue rheumatoid arthritis Qilu Hospital of Shandong University Recruiting No outcome recorded
Phase 4 NCT04020328 Sep 2019 → Mar 2022 IgA glomerulonephritis, chronic kidney disease Shenzhen Second People's Hospital Unknown No outcome recorded
Phase 4 NCT03739853 May 2019 → Oct 2024 psoriatic arthritis University of Oxford Completed No outcome recorded
Phase 4 NCT02703194 Mar 2016 → Jan 2019 immunoglobulin G4-related sclerosing disease Chinese PLA General Hospital Completed Met primary
Phase 4 NCT01172639 Feb 2009 → Jun 2015 rheumatoid arthritis P. Verschueren Completed Missed primary
Phase 4 NCT00280644 Apr 2004 → ? rheumatoid arthritis Sanofi Completed No outcome recorded
Phase 4 NCT00563849 May 2003 → Aug 2004 rheumatoid arthritis Sanofi Completed No outcome recorded
Phase 4 NCT00451971 Mar 2002 → ? rheumatoid arthritis Sanofi Completed No outcome recorded
Phase not applicable10 trials
— NCT05605587 May 2023 → Jan 2026 multiple endocrine neoplasia type 1 University Hospital, Basel, Switzerland Terminated No outcome recorded Stop: Enrollment
— NCT05937880 Jan 2023 → Jun 2027 expected immunoglobulin A vasculitis Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University Recruiting No outcome recorded
— NCT05789017 Jul 2022 → Dec 2024 autoimmune disease Peking Union Medical College Hospital Unknown No outcome recorded
— NCT05789030 Jul 2022 → Apr 2026 overdue autoimmune disease Peking Union Medical College Hospital Recruiting No outcome recorded
— NCT04737343 Jun 2021 → Nov 2024 anti-neutrophil cytoplasmic antibody-associated vasculitis Chinese SLE Treatment And Research Group Unknown No outcome recorded
— NCT04124861 Jun 2020 → Dec 2022 autoimmune disease Peking Union Medical College Hospital Unknown No outcome recorded
— NCT03715699 Jul 2018 → Dec 2020 autoimmune disease Peking Union Medical College Hospital Unknown No outcome recorded
— NCT01617590 May 2012 → Dec 2013 rheumatoid arthritis Shanxi Medical University Unknown No outcome recorded
— NCT01172002 Mar 2010 → Jun 2018 lupus erythematosus, nephritis RenJi Hospital Unknown No outcome recorded
— NCT00684372 May 2007 → May 2009 end stage renal failure, polyomavirus infectious disease Karolinska University Hospital Unknown No outcome recorded
Comparator or background therapy49 trials
Phase 1 NCT05247203 Background May 2022 → Oct 2023 systemic lupus erythematosus RemeGen Co., Ltd. Completed No outcome recorded
Phase 2 NCT06753565 Background Dec 2024 → Jun 2025 overdue rheumatoid arthritis German University in Cairo Recruiting No outcome recorded
Phase 2 NCT06640309 Background Dec 2023 → Jun 2025 overdue rheumatoid arthritis Ain Shams University Recruiting No outcome recorded
Phase 2 NCT05447520 Background Dec 2021 → Dec 2022 rheumatoid arthritis Noha Mansour Completed No outcome recorded
Phase 2 NCT03863405 Background Jan 2019 → Jan 2020 rheumatoid arthritis Ain Shams University Unknown No outcome recorded

News releases announcing trial results or a regulatory action · 3

DateIssuerRelease
2020-02-05 Lupin Limited Regulatory Lupin receives approval for Leflunomide Tablets USP lupin.com ↗
2019-04-25 Zydus Lifesciences Limited Regulatory Zydus receives final approval from the USFDA for Leflunomide Tablets USP zyduslife.com ↗
Zydus Cadila has received the final approval from the USFDA to market Leflunomide Tablets USP (US RLD – Arava Tablets ), 10 mg and 20 mg.
2005-09-14 Teva Branded Pharmaceutical Products R&D, Inc. Regulatory Teva Announces Approval of Leflunomide Tablets tevapharm.com ↗
Jerusalem, Israel, September 14, 2005 - Teva Pharmaceutical Industries Ltd. (Nasdaq: TEVA) announced today that the U.S. Food and Drug Administration has granted final approval for the Company's ANDA for Leflunomide Tablets, 10 mg and 20 mg.

All press releases naming this drug 5 releases

DateIssuerRelease

Evidence & citations 22 cited values

Every value below carries the sentence it was read from. 112 sources stand behind the page.

FieldValueCited text
Known as Leflunomide “Standard therapy comprises any of the following (alone or in combination): corticosteroids, antimalarials, non-steroidal anti-inflammatory drugs (NSAIDs), and immunosuppressive...” NCT02885610 ↗
107

“During the study, subjects continued to receive 1 or more background non-biologic DMARDs (e.g. methotrexate, leflunomide) at the dose level(s) and regimen(s) administered at...” NCT00124982 ↗

“Patients on corticosteroids (plus conventional therapy) will be randomized to receive anakinra (Kineret®), or one of the following: methotrexate, azathioprine, leflunomide,...” NCT01033656 ↗

“Patients who receive standard-therapy (Sulphasalazine, Methotrexate, Leflunomide) are treated with common dosages of these drugs that are deduced from the common treatment of...” NCT00244179 ↗

“csDMARDs may include one or two of the following: methotrexate (MTX), hydroxychloroquine or chloroquine, sulfasalazine, and/or leflunomide (combination of leflunomide and MTX...” NCT02873936 ↗

“The following DMARDs were permitted in this study: methotrexate (MTX), chloroquine, hydroxychloroquine, parenteral gold, sulfasalazine, azathioprine, and leflunomide.” NCT00531817 ↗

“Disease-modifying anti-rheumatic drugs included methotrexate, chloroquine, hydroxychloroquine, parenteral gold, sulfasalazine, azathioprine, and leflunomide.” NCT00720798 ↗

“methotrexate 7.5-15 mg once weekly hydroxychloroquine 200 mg twice daily sulfasalazine 500 mg to 3 g once daily leflunomide 20 mg once daily” NCT05671497 ↗

“Methotrexate(MTX) and/or 1 DMARDs(chloroquine, hydroxychloroquine, parenteral gold, sulfasalazine, azathioprine, and leflunomide)” NCT01211834 ↗

“Standard-of-care DMARD therapy, including methotrexate, sulfasalazine, leflunomide, minocycline, and/or hydroxychloroquine” NCT01313208 ↗

“including Leflunomide,Hydroxychloroquine,Sulfasalazine,Azathioprine,Tripterygium glycosides and Total glucosides of paeony” NCT04066803 ↗

Show 97 more sources

Known as Arava “Leflunomide (Arava) is an immunosuppressive drug, approved for the treatment of rheumatoid arthritis, and has been used in more than 300,000 patients worldwide.” NCT00684372 ↗
1

“Leflunomid (e.g. Arava®)” NCT02779114 ↗

Known as Arthfree “leflunomide(Arthfree®)” NCT06753565 ↗
Known as HWA-486 ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as L04AA13 ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as LEF “Leflunomide (LEF) is a derivative of isoxazole and is converted into an active metabolite which blocks de novo synthesis of pyrimidines in activated T lymphocytes, thereby...” NCT05113004 ↗
5

“one group was administered Xinfeng capsule (XFC) plus the placebo of leflunomide and the other given leflunomide (LEF) plus the placebo of XFC for twelve weeks.” PMID 26591677 ↗ Oct 2015

“DMARDs (methotrexate: MTX, leflunomide: LEF) were taken orally for at least 12 months.” NCT01600521 ↗

“ARM 2:Leflunomide(LEF)” NCT01659242 ↗

“Drug: Leflunomide(LEF)” NCT02532777 ↗

“Leflunomide(LEF)” NCT02981979 ↗

Known as Leflunomid “Leflunomid (e.g. Arava®)” NCT02779114 ↗
Known as Leflunomida ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as Leflunomide medac ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as Leflunomide ratiopharm ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as Leflunomide teva ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as Leflunomide winthrop ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as Leflunomide zentiva (previously leflunomide winthrop) ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as NSC-677411 ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as NSC-759864 ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as Repso ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Known as SU101 “patients receive leflunomide (SU101) IV over 4-5 hours weekly for 12 weeks” NCT00004071 ↗
3

“Patients receive leflunomide (SU101) IV over 6 hours daily on days 1-4” NCT00003293 ↗

“Patients receive leflunomide (SU101) IV over 6 hours on days 1-4.” NCT00003775 ↗

NCT00001573 ↗

Known as SULOL ChEMBL registry synonym — accepted as the source's own label CHEMBL960 ↗
Action Inhibit “SU101 is a member of a novel class of antineoplastic agents, platelet-derived growth factor (PDGF) receptor inhibitors.” NCT00001573 ↗
Modality Small molecule “Leflunomide, an isoxazole derivative, has profound immunosuppressive activity.” NCT00001863 ↗
Route Intravenous “Patients receive a 96 hour continuous IV infusion of SU101 on days 1-4.” NCT00001573 ↗
Target DHODH “inhibitor of dihydroorotate dehydrogenase (DHODH)” NCT03709446 ↗