Abstract
The active metabolite of leflunomide, A77 1726 inhibits the proliferation of a variety of mammalian cell lines in culture. Epidermal growth factor (EGF)-dependent proliferation is inhibited by A77 1726 at an effective dose of 30-40 microM. A77 1726 appears to directly inhibit the EGF receptor tyrosine-specific kinase activity both in intact cells and purified EGF receptors at the same effective dose. These data suggest that leflunomide inhibits cellular proliferation by the inhibition of tyrosine-specific kinase activities.
MeSH terms
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Aniline Compounds / pharmacology*
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Carcinoma, Squamous Cell
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Cell Line
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Cells, Cultured
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Crotonates
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ErbB Receptors / antagonists & inhibitors*
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ErbB Receptors / metabolism*
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Fibroblasts
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Humans
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Hydroxybutyrates / pharmacology*
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Isoxazoles / pharmacology*
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KB Cells
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Leflunomide
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Male
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Nitriles
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Phosphorylation
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Skin / metabolism
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Toluidines
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Tumor Cells, Cultured
Substances
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Aniline Compounds
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Anti-Inflammatory Agents, Non-Steroidal
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Crotonates
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Hydroxybutyrates
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Isoxazoles
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Nitriles
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Toluidines
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teriflunomide
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ErbB Receptors
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Leflunomide