Drug intelligence / Profile preview

TRPM8 agonist + TRPV4 agonist + TRPV1 agonist

Development stage
Unknown
Lead developer
Alcon
Modality
Small Molecules
Administration
Topical, Oral
01

Overview

This is a combination drug consisting of three distinct pharmacological agents, each acting as an agonist at a different member of the transient receptor potential (TRP) channel family: - A TRPM8 agonist, which activates the transient receptor potential melastatin 8 channel, known for its role in cold sensation and implicated in pain and itch modulation. - A TRPV4 agonist, which activates the transient receptor potential vanilloid 4 channel, involved in mechanosensation and osmosensation. - A TRPV1 agonist, which activates the transient receptor potential vanilloid 1 channel—a well-studied target for pain and heat sensation. Agonists at this site include capsaicin and endogenous lipids such as anandamide and N-arachidonoyldopamine[1][3][5][6]. The combination would theoretically modulate multiple sensory pathways simultaneously. While individual modulators of these channels are under investigation or clinical use (e.g., capsaicin for pain), there is no evidence that a fixed-dose pharmaceutical product combining all three types of agonists currently exists or has been clinically developed.

02

Targets

TRPV4 (Transient receptor potential cation channel subfamily V member 4)TRPV1 (Transient receptor potential cation channel subfamily V member 1)

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