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capsaicin + phenylephrine + caffeine
- Development stage
- Phase 2
- Lead developer
- Astellas Pharma
- Modality
- Small Molecules, Implantable Devices → Device-based Delivery → Drug Delivery Systems, 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
ADOR (Adenosine receptors)ADRA1A (α1A)
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