Drug intelligence / Profile preview

LU302146

Development stage
Preclinical
Lead developer
Knoll
Modality
Small Molecules
Administration
Intravenous, Intravesical
01

Overview

LU302146 is a **selective Endothelin-A receptor antagonist** developed for experimental modulation of smooth muscle contraction, particularly in bladder function. In preclinical animal studies, LU302146 was shown to **substantially decrease neurostimulation-induced bladder contraction**, suggesting its action involves inhibition of endothelin-1 at the endothelin-A receptor. Its selectivity for the Endothelin-A receptor indicates potential utility in disorders marked by excessive smooth muscle activation, such as **neurogenic bladder dysfunction** or bladder outlet obstruction. The compound works on the atropine-resistant part of efferent detrusor activation, thereby offering a mechanism distinct from anticholinergics. LU302146 has been evaluated in vivo in animal models but as of now there is no evidence of clinical development in humans[1][4].

Brand names
LU302146LU-302146LU 302146
Other names
LU302146LU-302146LU 302146
02

Targets

EDNRA (Endothelin receptor type A)

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