Drug intelligence / Profile preview

paraxanthine + aspirin + acetaminophen

Development stage
Preclinical
Lead developer
Plopii
Modality
Small Molecules
Administration
Oral
01

Overview

paraxanthine + aspirin + acetaminophen is a patent-pending, fixed-dose combination oral formulation developed by Plopii for the acute treatment of migraine and tension headaches. Designed as a next-generation alternative to traditional caffeine-containing analgesics (such as Excedrin), this combination replaces caffeine with its primary active metabolite, paraxanthine. Paraxanthine acts as a selective adenosine receptor antagonist to provide vasoconstriction and enhance the pain-relieving effects of the co-formulated analgesics with a significantly reduced risk of jitters, anxiety, sleep disruption, and rebound headaches. Aspirin acts as an irreversible inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) to reduce inflammatory prostaglandins, while acetaminophen provides central analgesic and antipyretic effects. The drug is being developed under the FDA 505(b)(2) regulatory pathway.

Brand names
Plopii Migraine MedicationPlopii Migraine PillPlopii Headache Pill
Other names
paraxanthine + aspirin + paracetamolparaxanthine + acetylsalicylic acid + acetaminophenparaxanthine + acetylsalicylic acid + paracetamol
02

Targets

ADORA1 (Adenosine receptor A1 subtype)ADORA2A (Adenosine A₂A Receptor)ADORA2B (Adenosine A2B receptor)ADORA3 (Adenosine A3 receptor)CNR1 (Cannabinoid receptor 1)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PDE (Phosphodiesterase family)TRPV1 (Transient receptor potential cation channel subfamily V member 1)

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