Drug intelligence / Profile preview

methylprednisolone + clemastine

Development stage
Unknown
Lead developer
Technical University of Munich
Modality
Small Molecules
Administration
Intravenous
01

Overview

Methylprednisolone + clemastine is a combination therapy consisting of a synthetic glucocorticoid (methylprednisolone) and a first-generation H1-antihistamine (clemastine). This combination was utilized as the active comparator (standard therapy) in a Phase 2 clinical trial (NCT01154361) sponsored by the Technical University of Munich for the treatment of acute ACE inhibitor-induced angioedema. Methylprednisolone acts as an anti-inflammatory agent by activating the glucocorticoid receptor, while clemastine blocks the effects of histamine at the H1 receptor. Although historically used for angioedema, this combination is considered theoretically ineffective for ACE inhibitor-induced cases, which are primarily mediated by bradykinin rather than histamine or typical inflammatory pathways. The trial results confirmed its inferiority to the bradykinin B2 receptor antagonist icatibant, with significantly longer times to symptom resolution.

Other names
cortisone + clemastin-Technical University of Munich-angioedema (ACE inhibitor-induced)cortisone + clemastinmethylprednisolone + clemastineprednisolone + clemastinestandard therapy (cortisone and clemastine)
02

Targets

mAChR (Muscarinic acetylcholine receptors)GR (Glucocorticoid receptor)HRH1 (Histamine H1 Receptor)

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