Drug intelligence / Profile preview

capsaicin + phenylephrine + caffeine

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Implantable Devices → Device-based Delivery → Drug Delivery Systems, Small Molecules, Transdermal Patches → Device-based Delivery → Drug Delivery Systems, Inhalation Devices → Device-based Delivery → Drug Delivery Systems
Administration
Sublingual, Oral
01

Overview

This is a combination drug consisting of capsaicin, phenylephrine, and caffeine. It has been studied as a sublingual/oral gel formulation for its safety, tolerability, and pharmacokinetics in healthy adult volunteers. The primary investigational use is for the acute management of vasovagal syncope (VVS) or impending syncopal attacks. Capsaicin acts as a TRPV1 receptor agonist leading to sensory nerve activation and subsequent desensitization; phenylephrine is an alpha-1 adrenergic receptor agonist that induces vasoconstriction and increases blood pressure; caffeine is a central nervous system stimulant that antagonizes adenosine receptors and can increase alertness and blood pressure. In phase I studies, this combination was well tolerated with no serious adverse effects reported[1][2]. The main side effect observed was temporary oral/gastric discomfort due to capsaicin.

Other names
CPC
02

Targets

ADRA1A (α1A)ADOR (Adenosine receptors)

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