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Caffeine Pill

Rothman Institute Orthopaedics · Phase 3 active Small molecule

Caffeine blocks adenosine receptors in the central nervous system, reducing drowsiness and increasing alertness and mental focus.

Caffeine blocks adenosine receptors in the central nervous system, reducing drowsiness and increasing alertness and mental focus. Used for Fatigue and drowsiness, Cognitive enhancement and mental alertness.

At a glance

Generic nameCaffeine Pill
SponsorRothman Institute Orthopaedics
Drug classAdenosine receptor antagonist
TargetAdenosine receptors (A1, A2A)
ModalitySmall molecule
Therapeutic areaNeurology / Stimulant
PhasePhase 3

Mechanism of action

Caffeine is a non-selective adenosine receptor antagonist that crosses the blood-brain barrier and competitively inhibits adenosine binding at A1 and A2A receptors. By blocking adenosine—a neurotransmitter that promotes sleep and relaxation—caffeine increases neuronal firing and the release of excitatory neurotransmitters like dopamine and norepinephrine, resulting in increased wakefulness, improved concentration, and enhanced cognitive performance.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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