molecules of the month


oral P2X3 ion channel antagonist

Ph. II, multiple settings (50-750 mg BID)

from literature P2X3 antagonists

Scientific Reports

Bayer AG, Berlin, DE

Chemical structure of molecule eliapixant (BAY1817080)
1 min read

The Bayer P2X3 purinoreceptor antagonist, eliapixant (BAY1817080), is intended to treat various disorders associated with hypersensitive nerve fibers, including endometriosis. The hypothesis is that P2X3 receptor antagonism can inhibit cycles of pain causing neurogenic inflammation, causing pain, etc. modifying the underlying disease in endometriotic lesions. Endometriosis is an area of significant unmet medical need but with a high bar for safety.  Eliapixant is highly potent and selective for P2X3 over other P2X subtypes in vitro, including P2X2/3. The molecule completed a phase I safety study and is in several ongoing phase II trials in different conditions including endometriosis (NCT04614246); other hypersensitive nerve fiber-associated disorders, including refractory or unexplained chronic cough (RUCC) (NCT04562155); diabetic neuropathic pain (DNP) (NCT04641273) and overactive bladder (OAB) (NCT04545580).…

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