• Tuberculosis and Respiratory Diseases
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• 제66권6호
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• pp.477-481
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• 2009

Leflunomide는 항류마티스 약제로 최근 류마티스 관절염 치료에 효과적으로 사용되고 있다. 최근 본 약제로 인한 간질성 폐렴이 일본과 한국에서 서구에서보다 많이 보고되고 있으며 종종 사망하는 경우도 보고되고 있다. 저자들은 25세 여자에서 Methotrexate와 Leflunomide의 병합요법 중 발생한 간질성 폐렴을 진단하였고 Methylprednisolone과 Cholestyramine을 조기 투여하여 효과적으로 치료하였기에 문헌 고찰과 함께 보고하는 바이다.

• Tuberculosis and Respiratory Diseases
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• 제58권1호
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• pp.83-88
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• 2005

Leflunomide는 최근에 개발된 항류마티스 약물로서 기존의 약물과 작용기전이 다르면서 효과가 우수하여 활동성 류마티스관절염에 널리 사용되고 있다. 알려진 부작용에는 간독성과 피부독성, 조혈기능부전, 위장관계 증상등이 있는데, 시판후 조사에서는 호흡기계 부작용도 드물지만 경한 정도에서 치명적인 경우까지 모두 보고 되었다. 세계 각 처에서의 시판후 조사에 의하면 호흡기계 부작용으로 사망한 경우가 있어서 심각한 폐독성의 가능성을 시사한다. 우리나라에서는 leflunomide로 인한 호흡기계 부작용에 대한 보고가 없었다. 저자들은 leflunomide에 의한 간질성 폐렴 1예를 경험하였기에 문헌고찰과 함께 보고하는 바이다.

• 대한의생명과학회지
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• 제15권1호
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• pp.61-66
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• 2009

Leflunomide is an immunomodulatory agent used for the treatment of rheumatoid arthritis (RA). Leflunomide known as a regulator of iNOS synthesis which largely decreases NO production in diverse cell type. However, the effect of leflunomide on chondrocyte is still poorly understood. In our previous studies, we have shown that direct production of Nitric oxide (NO) by treating chondrocytes with NO donor, sodium nitroprusside (SNP), causes apoptosis via p38 mitogen-activated protein kinase in association with elevation of p53 protein level, caspase-3 activation. In this study, we characterized the molecular mechanism by which A77 1726 inhibit apoptosis. We found that A77 1726 inhibit NO-induced apoptosis as determined by MTT (Thiazolyl Blue Tetrazolium Bromide) assay and DNA fragmentation. The inhibition of apoptosis by A77 1726 was accompanied by increased PI-3 kinase and AKT activities. So, inhibition of phosphatidylinositol (PI)-3kinase with LY294002 rescued apoptosis. Triciribine, the specific inhibitor of AKT, also abolished anti-apoptotic effect. Our results indicate that A77 1726, the active metabolite of leflunomide, mediates NO-induced apoptosis in chondrocytes by modulating up-regulation of PI-3 kinase and AKT.

• Archives of Pharmacal Research
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• 제26권3호
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• pp.197-201
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• 2003

Novel $\beta$-hydroxy propenamides as analogues of the active metabolite of leflunomide (A 771726) were synthesized and evaluated for their inhibitory activity on dihydroorotate dehydrogenase (DHODH) in an investigation into their immunosuppressive activity. Compounds 2a, 3a, and 3h were approximately 4-40 times more potent than leflunomide in their activity while they were-less active than A 771726.

• 약학회지
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• 제50권2호
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• pp.70-77
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• 2006

A cost effective analysis was performed for comparing leflunomide+methotrexate, etanercept monotherapy and etanercept+methotrexate for 6 months. For the patients with methotrexate-resistant RA, ACR20 data were extracted from the published clinical trials searched from Pubmed. The direct medical cost was estimated based on ACR guideline and Korean National Health Insurance reimbursement. Combination therapy of etanercept+methotrexate was found to be more cost-effective than etanercept monotherapy, which meant it was a better therapeutic strategy for methotrexate- resistant RA.

• Tuberculosis and Respiratory Diseases
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• 제77권6호
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• pp.266-270
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• 2014

Recently, the incidence of pulmonary cryptococcosis is gradually increasing in rheumatoid arthritis (RA) patients. Pulmonary rheumatoid nodules (PRN) are rare manifestations of RA. Eighteen months ago, a 65-year old woman was admitted to hospital due to multiple nodules ( $2.5{\times}2.1{\times}2cm$) with cavitations in the right lower lobe. She was diagnosed with RA three year ago. She had been taking methotrexate, leflunomide, and triamcinolone. A video-assisted thoracoscopic surgery biopsy was performed and PRN was diagnosed. However, a newly growing huge opacity with cavitation was detected in the same site. Pulmonary cryptococcal infection was diagnosed through a transthoracic computed tomograpy guided needle biopsy. Cryptococcus antigen was detected in serum but not in cerebrospinal fluid. The patient was treated with oral fluconazole which resulted clinical improvement and regression of the nodule on a series of radiography. Herein, we report the case of pulmonary cryptococcosis occurring in the same location as that of the PRN.

• 한국임상수의학회:학술대회논문집
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• 한국임상수의학회 2006년도 추계학술대회 및 정기총회
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• pp.134-134
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• 2006