Literature DB >> 25712857

Leflunomide and teriflunomide: altering the metabolism of pyrimidines for the treatment of autoimmune diseases.

Yara Dadalti Fragoso1, Joseph Bruno Bidin Brooks.   

Abstract

Leflunomide modulates T-cell responses and induces a shift from the Th1 to Th2 subpopulation. This process results in a beneficial effect in diseases in which there is good evidence that T cells play a major role in both initiation and perpetuation of the inflammatory condition. Leflunomide has been successfully used for treating rheumatoid arthritis and psoriatic arthritis for many years. The active metabolite of leflunomide is teriflunomide, which has been approved for treating multiple sclerosis. Teriflunomide, just like the mother drug, inhibits dihydro-orotate dehydrogenase and synthesis of pyrimidine. The present review presents and discusses the safety profiles of leflunomide and teriflunomide, two drugs that are indeed the same, considering that much can be learned from the reported side effects of both.

Entities:  

Keywords:  leflunomide; multiple sclerosis; pyrimidine; rheumatoid arthritis; teriflunomide

Mesh:

Substances:

Year:  2015        PMID: 25712857     DOI: 10.1586/17512433.2015.1019343

Source DB:  PubMed          Journal:  Expert Rev Clin Pharmacol        ISSN: 1751-2433            Impact factor:   5.045


  29 in total

1.  Leflunomide: an unlikely trigger and mechanistically a beneficial drug for alopecia areata.

Authors:  Kabir Sardana; Aastha Gupta; Pulin Kumar Gupta
Journal:  Clin Rheumatol       Date:  2019-07-23       Impact factor: 2.980

2.  The Dihydroorotate Dehydrogenase Inhibitor Brequinar Is Synergistic with ENT1/2 Inhibitors.

Authors:  Christine R Cuthbertson; Hui Guo; Armita Kyani; Joseph T Madak; Zahra Arabzada; Nouri Neamati
Journal:  ACS Pharmacol Transl Sci       Date:  2020-11-23

3.  Adaptive Reprogramming of De Novo Pyrimidine Synthesis Is a Metabolic Vulnerability in Triple-Negative Breast Cancer.

Authors:  Kristin K Brown; Jessica B Spinelli; John M Asara; Alex Toker
Journal:  Cancer Discov       Date:  2017-03-02       Impact factor: 39.397

4.  Encapsulation of Leflunomide (LFD) in a novel niosomal formulation facilitated its delivery to THP-1 monocytic cells and enhanced Aryl hydrocarbon receptor (AhR) nuclear translocation and activation.

Authors:  Mahsa Hasani; Neda Abbaspour Sani; Behnaz Khodabakhshi; Mehdi Sheikh Arabi; Saeed Mohammadi; Yaghoub Yazdani
Journal:  Daru       Date:  2019-08-20       Impact factor: 3.117

Review 5.  Infectious Complications of Novel Multiple Sclerosis Therapies.

Authors:  S N Levin; T B Kaplan
Journal:  Curr Infect Dis Rep       Date:  2017-02       Impact factor: 3.725

Review 6.  Nitrile-containing pharmaceuticals: target, mechanism of action, and their SAR studies.

Authors:  Xi Wang; Yuanxun Wang; Xuemin Li; Zhenyang Yu; Chun Song; Yunfei Du
Journal:  RSC Med Chem       Date:  2021-08-10

Review 7.  Pharmacotherapy Pearls in Rheumatology for the Care of Older Adult Patients: Focus on Oral Disease-Modifying Antirheumatic Drugs and the Newest Small Molecule Inhibitors.

Authors:  Blas Y Betancourt; Ann Biehl; James D Katz; Ananta Subedi
Journal:  Rheum Dis Clin North Am       Date:  2018-06-12       Impact factor: 2.670

8.  Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase.

Authors:  Joseph T Madak; Christine R Cuthbertson; Yoshinari Miyata; Shuzo Tamura; Elyse M Petrunak; Jeanne A Stuckey; Yanyan Han; Miao He; Duxin Sun; Hollis D Showalter; Nouri Neamati
Journal:  J Med Chem       Date:  2018-05-14       Impact factor: 7.446

Review 9.  Recent advances in developing small-molecule inhibitors against SARS-CoV-2.

Authors:  Rong Xiang; Zhengsen Yu; Yang Wang; Lili Wang; Shanshan Huo; Yanbai Li; Ruiying Liang; Qinghong Hao; Tianlei Ying; Yaning Gao; Fei Yu; Shibo Jiang
Journal:  Acta Pharm Sin B       Date:  2021-07-02       Impact factor: 14.903

10.  Inhibition of de novo pyrimidine synthesis augments Gemcitabine induced growth inhibition in an immunocompetent model of pancreatic cancer.

Authors:  Thuy Phan; Vu H Nguyen; Ralf Buettner; Corey Morales; Lifeng Yang; Paul Wong; Weiman Tsai; Marcela d'Alincourt Salazar; Ziv Gil; Don J Diamond; Joshua D Rabinowitz; Steven Rosen; Laleh G Melstrom
Journal:  Int J Biol Sci       Date:  2021-06-01       Impact factor: 6.580

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