Drug intelligence / Profile preview

16a-methylhydrocortisone

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-117 (16a-methylhydrocortisone) is a synthetic corticosteroid derivative developed by Merck in the late 1950s. It belongs to a class of 16-methylated steroids designed to enhance anti-inflammatory activity while minimizing the mineralocorticoid effects (such as sodium and water retention) typically associated with natural corticosteroids like hydrocortisone. In early clinical evaluations for rheumatoid arthritis, MK-117 demonstrated approximately 70% of the antirheumatic potency of prednisolone. Although it successfully avoided discernible electrolyte disturbances at therapeutic doses, its relatively lower potency compared to other derivatives in the same series, such as dexamethasone (MK-125), led to its discontinuation in favor of more effective analogs.

Other names
16a-methyl hydrocortisone16-alpha-methylhydrocortisone
02

Targets

GR (Glucocorticoid receptor)

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