Drug intelligence / Profile preview

methimazole + methylprednisolone

Development stage
Phase 3
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Methimazole + methylprednisolone is a combination of two pharmaceutical agents used together primarily in the management of patients with Graves' disease and associated Graves ophthalmopathy (GO), especially when there is concern for optic nerve damage. Methimazole is a thionamide antithyroid agent that inhibits thyroid peroxidase, thereby reducing thyroid hormone synthesis and controlling hyperthyroidism. Methylprednisolone is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive properties, commonly administered intravenously as pulse therapy to reduce inflammation in GO. The combination may be considered when both control of thyrotoxicosis and suppression of autoimmune orbital inflammation are required. However, co-administration can increase the risk of drug-induced liver injury (DILI), particularly if either agent induces hepatotoxicity or if cumulative doses are high[1][2][4]. Careful monitoring of liver function is recommended during combined use.

02

Targets

GR (Glucocorticoid receptor)TPO (Thyroid peroxidase)

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