Leflunomide is a low-molecular weight, synthetic, oral agent specifically developed for immunosuppression. Leflunomide reduces the clinical symptoms and signs of RA(rheumatoid arthritis), improves health related quality of life, and retards structural damage. Leflunomide has been evaluated in RA patients as monotherapy and in combination with methotrexate[3]. Leflunomide itself induces AHR-ARNT interaction to inhibit hepatic CRP production and attenuate bone erosion in CRPL (CRPLower, CRPL) arthritic rats[4]. A significant elevation of liver enzymes in leflunomide-treated mice (10 mg/kg) and histopathological examination revealed higher necro-inflammatory scores in leflunomide-treated mice. Furthermore, leflunomide-treated mice (5 or 10 mg/kg) showed greater staining for NFκB compared to vehicle control[5]. Compared with cyclophosphamide, low-dose leflunomide in combination with prednisone showed both effectiveness and safety in the induction therapy of proliferative lupus nephritis in Chinese patients[6].
Leflunomide/来氟米特 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HeLa cells
4 µM
Validated leflunomide's inhibition of caspase 3/7 activity
Gastroenterology. 2020 Mar;158(4):1000-1015.
C17.2 cells
50 µM
16 hours
To evaluate whether Leflunomide could promote cell survival following OGD, and it was found that Leflunomide was unable to promote cell survival.
Cells. 2024 Apr 4;13(7):631.
WRJ388 cells
36 µM (Day 2), 15 µM (Day 4)
2-4 days
Suppressed the growth of WRJ388 cells, primarily through S-phase cell cycle arrest
Mol Cancer Ther. 2021 Feb;20(2):274-283.
4T1 cells
10 µM
3 days
Leflunomide induced mitochondrial elongation by promoting Mfn2 expression and reducing Drp1 levels, and restricted the proliferative capacity of 4T1 cells.
Sci Adv. 2024 Nov 8;10(45):eadm8212.
HOAT1-HEK293 cells
5 µM
30 minutes
To investigate the effect of teriflunomide on the uptake of acyclovir in hOAT1-HEK293 cells, results showed that teriflunomide significantly inhibited the uptake of acyclovir.
Acta Pharmacol Sin. 2020 Jan;41(1):129-137.
HOAT3-HEK293 cells
5 µM
30 minutes
To investigate the effect of teriflunomide on the uptake of acyclovir in hOAT3-HEK293 cells, results showed that teriflunomide significantly inhibited the uptake of acyclovir.
Acta Pharmacol Sin. 2020 Jan;41(1):129-137.
HeLa cells
20-51 µM
3-6 days
Induced apoptosis in HeLa cells, resulting in the regression of HeLa xenografts
Mol Cancer Ther. 2021 Feb;20(2):274-283.
HAP1 cells
4 µM
48 hours
Reduced caspase 3 and 7 activity, increased cell viability
Gastroenterology. 2020 Mar;158(4):1000-1015.
H460 cells
80.5 µM (48 hours), 27 µM (72 hours)
48-72 hours
Induced G1 cell cycle arrest but not apoptosis in H460 cells, attenuated the growth of H460-derived xenografts
Mol Cancer Ther. 2021 Feb;20(2):274-283.
MRP2-MDCK cells
0.5 - 100 µM
60 minutes
To investigate the effect of leflunomide/teriflunomide on the accumulation of acyclovir in MRP2-MDCK cells, results showed that teriflunomide dose-dependently increased the accumulation of acyclovir with an IC50 value of 4.91 μmol/L.
Acta Pharmacol Sin. 2020 Jan;41(1):129-137.
MM cell lines
30-150 µM
72 hours
To validate the anti-MM activity of Leflunomide, results showed inhibition of MM cell growth.
Blood Adv. 2019 Apr 9;3(7):1027-1032.
Leflunomide/来氟米特 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Breast cancer model
Oral
25 or 50 mg/kg
5 days on, 2 days off, throughout the duration of the experiment
Leflunomide significantly reduced the number of visible metastatic lesions and total metastatic area in the lungs of the 4T1 breast cancer model.
To evaluate the effect of Leflunomide combined with Lenalidomide on survival in an MM model, results showed significantly prolonged survival with the combination treatment.
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