Serdexmethylphenidate is a

prodrug A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be ...

dexmethylphenidate Dexmethylphenidate, sold under the brand name Focalin among others, is a central nervous system (CNS) stimulant used in the treatment of attention deficit hyperactivity disorder (ADHD) in those over the age of five years. It is taken by mouth. ...

created by the pharmaceutical company Zevra Therapeutics. The compound was first approved by the FDA as one of the active ingredients in Azstarys for the treatment of

attention deficit hyperactivity disorder Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by symptoms of inattention, hyperactivity, impulsivity, and emotional dysregulation that are excessive and pervasive, impairing in multiple con ...

(ADHD) in children, adolescents, and adults in March 2021. Serdexmethylphenidate is a prodrug which has a delayed

onset of action Onset of action is the duration of time it takes for a drug's effects to come to prominence upon administration. With oral administration, it typically ranges anywhere from 20 minutes to over an hour, depending on the drug in question. Other meth ...

and a prolonged duration of effects compared to dexmethylphenidate, its parent compound.

Medical uses

The combination serdexmethylphenidate/dexmethylphenidate (Azstarys) was approved by the

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respo ...

(FDA) in March 2021, for the treatment of ADHD in people six years of age and older. Co-formulation of serdexmethylphenidate with dexmethylphenidate allows for a more rapid onset of action while still retaining up to 13 hours of therapeutic efficacy.

Society and culture

Abuse potential

The abuse potential of serdexmethylphenidate has been evaluated in clinical studies. Administration of serdexmethylphenidate via common routes of administration used during the abuse of psychostimulants such as

insufflation In religious and magical practice, insufflation and exsufflation are ritual acts of blowing, breathing, hissing, or puffing that signify variously expulsion or renunciation of evil or of the devil (the Evil One), or infilling or blessing with go ...

and intravenous injection resulted in significantly reduced systemic exposure to active dexmethylphenidate and thus markedly decreased pharmacodynamic effects when compared to unmodified dexmethylphenidate. Following an Eight Factor Analysis by the FDA Controlled Substance Staff (CSS), the

U.S. Department of Health and Human Services The United States Department of Health and Human Services (HHS) is a cabinet-level executive branch department of the US federal government created to protect the health of the US people and providing essential human services. Its motto is "Im ...

(HHS) provided a scheduling recommendation to the

Drug Enforcement Administration The Drug Enforcement Administration (DEA) is a Federal law enforcement in the United States, United States federal law enforcement agency under the U.S. Department of Justice tasked with combating illicit Illegal drug trade, drug trafficking a ...

(DEA) to control serdexmethylphenidate and its salts in schedule IV of the

Controlled Substances Act The Controlled Substances Act (CSA) is the statute establishing federal government of the United States, federal drug policy of the United States, U.S. drug policy under which the manufacture, importation, possession, use, and distribution of ...

(CSA). Based on this recommendation and its own review, the DEA concluded that serdexmethylphenidate met the criteria for placement in schedule IV of the CSA.

Research

Due to the delayed onset and prolonged duration of effects following oral administration of serdexmethylphenidate, several dosage forms containing serdexmethylphenidate are under investigation for use as long-acting

psychostimulant Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition ...

in the treatment of various CNS disorders,

substance use disorder Substance use disorder (SUD) is the persistent use of drugs despite substantial harm and adverse consequences to self and others. Related terms include ''substance use problems'' and ''problematic drug or alcohol use''. Along with substance-ind ...

(SUD), and

sleep disorders A sleep disorder, or somnipathy, is a medical disorder affecting an individual's sleep patterns, sometimes impacting physical, mental, social, and emotional functioning. Polysomnography and actigraphy are tests commonly ordered for diagnosing sle ...

. Under the developmental codename KP484, serdexmethylphenidate is being investigated as part of a potential "super-extended duration" psychostimulant, with therapeutic efficacy lasting up to 16 hours following oral administration. In January 2021, the FDA granted approval for clinical trials investigating serdexmethylphenidate (as KP879) for the treatment for

stimulant use disorder Stimulant use disorder is a type of substance use disorder where the use of stimulants caused clinically significant impairment or distress. It is defined in the DSM-5 as "the continued use of amphetamine-type substances, cocaine, or other stimul ...

References

{{Portal bar , Medicine 2-Benzylpiperidines Methylphenidate Nootropics Norepinephrine–dopamine reuptake inhibitors Pyridinium compounds Stimulants