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Osmotic-release oral system methylphenidate

Eli Lilly and Company · FDA-approved active Small molecule

Methylphenidate is a central nervous system stimulant that increases dopamine and norepinephrine activity in the brain by blocking their reuptake at the synapse.

Methylphenidate is a central nervous system stimulant that increases dopamine and norepinephrine activity in the brain by blocking their reuptake at the synapse. Used for Attention-deficit/hyperactivity disorder (ADHD), Narcolepsy.

At a glance

Generic nameOsmotic-release oral system methylphenidate
SponsorEli Lilly and Company
Drug classCentral nervous system stimulant
TargetDopamine transporter (DAT), Norepinephrine transporter (NET)
ModalitySmall molecule
Therapeutic areaNeurology / Psychiatry
PhaseFDA-approved

Mechanism of action

Methylphenidate inhibits the reuptake of dopamine and norepinephrine by blocking their respective transporters (DAT and NET), leading to increased concentrations of these neurotransmitters in the synaptic cleft. This enhanced dopaminergic and noradrenergic signaling improves attention, focus, and impulse control. The osmotic-release oral system (OROS) formulation provides controlled, extended-release delivery over approximately 12 hours.

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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