Drug intelligence / Profile preview

THRX-195518

Development stage
Preclinical
Lead developer
Theravance Biopharma
Modality
Small Molecules
Administration
Not Directly Administered; Occurs Systemically After Inhaled Administration Of Revefenacin
01

Overview

THRX-195518 is the major active **metabolite** of revefenacin, formed through amide hydrolysis of the parent drug. It retains affinity for all five human muscarinic receptor subtypes (hM1 to hM5), but exhibits 3- to 10-fold lower binding affinity than revefenacin itself. Despite reduced potency, it contributes to the systemic antimuscarinic pharmacodynamic activity observed after revefenacin inhalation. THRX-195518 is present at higher systemic exposure than revefenacin following inhaled administration, with exposures exceeding those of revefenacin by approximately 4- to 6-fold in COPD patients (based on AUC). Its elimination is mainly hepatobiliary, with minimal renal excretion. The compound is investigated primarily as a pharmacologically active metabolite in the context of revefenacin therapy for chronic obstructive pulmonary disease (COPD)[1][2][4].

Other names
THRX-195518THRX195518THRX 195518CAS 909800-36-8CAS909800-36-8CAS-909800-36-8
02

Targets

M1 (Muscarinic acetylcholine receptor M1)CHRM3 (M3)CHRM5 (M5)CHRM2 (M2)CHRM4 (M4)

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