Serdexmethylphenidate is a

prodrug A prodrug is a 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 used to improve how the drug ...

dexmethylphenidate Dexmethylphenidate, sold under the brand name Focalin among others, is a strong central nervous system (CNS) stimulant medication used to treat attention deficit hyperactivity disorder (ADHD) in those over the age of five years. If no benefit i ...

created by the pharmaceutical company KemPharm (now 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 (ADHD) in children, adolescents, and adults in March 2021. Serdexmethylphenidate is a prodrug which has a delayed onset of action 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 (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 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 U.S. federal government created to protect the health of all Americans and providing essential human services. Its motto is " ...

(HHS) provided a scheduling recommendation to the Drug Enforcement Administration (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 often referred to as psychostimulants or colloquially as uppers) is an overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and inv ...

in the treatment of various

CNS disorders Central nervous system diseases, also known as central nervous system disorders, are a group of neurological disorders that affect the structure or function of the brain or spinal cord, which collectively form the central nervous system (CNS). T ...

substance use disorder Substance use disorder (SUD) is the persistent use of drugs (including alcohol) despite substantial harm and adverse consequences as a result of their use. Substance use disorders are characterized by an array of mental/emotional, physical, and ...

(SUD), and sleep disorders. 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 that involves the non-medical use of stimulants. It is defined in the DSM-5 as "the continued use of amphetamine-type substances, cocaine, or other stimulants leading to clinically signif ...

References

2-Benzylpiperidines Methylphenidate Nootropics Norepinephrine–dopamine reuptake inhibitors Pyridinium compounds Stimulants {{Nervous-system-drug-stub