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| Other names | SDX |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Bioavailability | < 3% (absolute oral)[2] |
| Metabolites | Dexmethylphenidate,ritalinic acid[2] |
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| Chemical and physical data | |
| Formula | C25H29N3O8 |
| Molar mass | 499.520 g·mol−1 |
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Serdexmethylphenidate (SDX) is aprodrug ofdexmethylphenidate created by the pharmaceutical company Zevra Therapeutics. The compound was first approved by the FDA as one of the active ingredients inAzstarys for the treatment ofattention deficit hyperactivity disorder (ADHD) in children, adolescents, and adults in March 2021.[2][3] Serdexmethylphenidate is a prodrug which has a delayedonset of action and a prolonged duration of effects compared to dexmethylphenidate, its parent compound.
The combinationserdexmethylphenidate/dexmethylphenidate (Azstarys) was approved by theFood and Drug Administration (FDA) in March 2021, for the treatment of ADHD in people six years of age and older.[2] Co-formulation of serdexmethylphenidate with dexmethylphenidate allows for a more rapid onset of action while still retaining up to 13 hours of therapeutic efficacy.[4][5]
Serdexmethylphenidate has mean terminal plasma elimination half-life of 5.7 hours.[6] Less than 3% of the drug is measurable in circulation intact following oral administration.[3] When administered alone, serdexmethylphenidate produces a dexmethylphenidate tmax of 8 hours.[7] It is believed that serdexmethylphenidate is metabolized to dexmethylphenidate primarily in the lower gastrointestinal tract. Enzymes involved in this conversion have yet to be elucidated.[6]
The abuse potential of serdexmethylphenidate has been evaluated in clinical studies.[8] Administration of serdexmethylphenidate via common routes of administration used during the abuse of psychostimulants such asinsufflation and intravenous injection resulted in significantly reduced systemic exposure to active dexmethylphenidate and thus markedly decreased pharmacodynamic effects when compared to unmodified dexmethylphenidate.[9]
Following an Eight Factor Analysis by the FDA Controlled Substance Staff (CSS), theU.S. Department of Health and Human Services (HHS) provided a scheduling recommendation to theDrug Enforcement Administration (DEA) to control serdexmethylphenidate and its salts inschedule IV of theControlled Substances Act (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.[8][10]
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-actingpsychostimulant in the treatment of variousCNS disorders,substance use disorder (SUD), andsleep disorders.[11] 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.[11]
In January 2021, the FDA granted approval for clinical trials investigating serdexmethylphenidate (as KP879) for the treatment forstimulant use disorder.[12]
