Leflunomide - CAS 75706-12-6
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Not Intended for Therapeutic Use. For research use only.
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Leflunomideinhibits the reproduction of rapidly dividing cells by inhbiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH).
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1.Detection of in Vitro Metabolite Formation of Leflunomide: A Fluorescence Dynamics and Electronic Structure Study.
Sharma P1, Gangopadhyay D1, Mishra PC1, Mishra H2, Singh RK1. J Med Chem. 2016 Apr 14;59(7):3418-26. doi: 10.1021/acs.jmedchem.6b00088. Epub 2016 Apr 1.
The metabolic transformation of antirheumatic fluorescent drug leflunomide into its active metabolite teriflunomide through isoxazole ring opening has been monitored in vitro using steady state and time domain fluorescence spectroscopy and density functional theory. During metabolic reaction, absorption of leflunomide split into two bands resembling absorption spectra of teriflunomide. The fluorescence spectra reveal slow conversion of leflunomide to E and Z forms of teriflunomide in aqueous medium, which becomes faster at basic pH. The E form, which is more potent as a drug, becomes more stable with an increase in the basicity of the medium. Both molecules are associated with charge transfer due to twisting in the lowest singlet excited state. Excited state charge transfer followed by proton transfer was also observed in the Z form during the ring opening of leflunomide. Quantum yield and radiative decay rates have been observed to decrease for the metabolite because of an increase in nonradiative decay channels.
2.Evaluation of leflunomide for the treatment of BK viremia and biopsy proven BK nephropathy; a single center experience.
Nesselhauf N1, Strutt J2, Bastani B3. J Nephropathol. 2016 Jan;5(1):34-7. doi: 10.15171/jnp.2016.06. Epub 2015 Dec 23.
BACKGROUND: BK virus reactivation is a significant complication following renal transplantation that can result in graft failure. Reduction of immunosuppression and substitution of leflunomide for mycophenolate mofetil (MMF) has been used to treat this entity.
3.Management of rheumatoid arthritis: Impact and risks of various therapeutic approaches.
Negrei C1, Bojinca V2, Balanescu A2, Bojinca M3, Baconi D1, Spandidos DA4, Tsatsakis AM5, Stan M1. Exp Ther Med. 2016 Apr;11(4):1177-1183. Epub 2016 Feb 2.
Rheumatic diseases are highly prevalent chronic disorders and the leading cause of physical disability worldwide, with a marked socio-economic impact. Rheumatoid arthritis (RA) is a chronic systemic inflammatory disease of unknown etiology with an autoimmune pathogenesis, characterised by arthropathy with chronic, deforming, destructive evolution and multiple systemic manifestations. The management of RA has undergone significant changes as far as objectives and approaches are concerned, ending in the current strategy known as 'treat to target'. The therapeutic array of RA includes several categories of medicinal products, of varying potential. There are several criteria for the classification of medicinal products used against this disease, one of the most important and modern of which divides such substances according to their effects on the progress of the disease: symptom-modifying antirheumatic drugs (including non-steroidal anti-inflammatory drugs and corticoids), disease-modifying antirheumatic drugs (including various substances, such as gold salts, antimalarials, sulfasalazine, D-penicillamine; non-specific immunosuppressive medication, such as methotrexate, cyclophosphamide, azathioprine and leflunomide) and biological therapy is a recent addition, providing new insight into the treatment of this disease.
4.Second-line therapy with biological drugs in rheumatoid arthritis patients in German rheumatologist practices: a retrospective database analysis.
Gossen N1, Jacob L2, Kostev K3. Rheumatol Int. 2016 Mar 2. [Epub ahead of print]
The aim of the study was to assess the proportion of German patients with rheumatoid arthritis (RA) who received biological disease-modifying antirheumatic drugs (DMARDs) after initiation of conventional DMARD therapy. Patients aged 18 years or over who had initiated therapy with a conventional DMARD in a rheumatic care practice between 2009 and 2013 were included (IMS LRx database). The main outcome was the first prescription of a biological DMARD within 5 years following the index date. A multivariate Cox regression model was adopted to predict the prescription of biological DMARDs on the basis of patient characteristics. The mean age of the 137,673 patients with RA was 57.8 years (SD = 15.0). 68.3 % of the subjects were women. Most patients started their conventional DMARD therapy with methotrexate (62 %), sulfasalazine (13 %), and hydroxychloroquine (12 %). 20.7 % of the RA patients were given a biological DMARD within 5 years following the index date.
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CAS 75706-12-6 Leflunomide

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