Serdexmethylphenidate

Serdexmethylphenidate is a prodrug of dexmethylphenidate. Dexmethylphenidate HCl is a central nervous system (CNS) stimulant.

• AZSTARYS is indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) in patients 6 years of age and older. Limitations of Use The use of AZSTARYS is not recommended in pediatric patients younger than 6 years of age because they had higher plasma exposure and a higher incidence of adverse reactions (e.g., weight loss) than patients 6 years and older at the same dosage [see Warnings and Precautions ( 5.7 ), Use in Specific Populations ( 8.4 )].ICD-10: F90.9

• AZSTARYS is contraindicated in patients: with known hypersensitivity to serdexmethylphenidate, methylphenidate, or other components of AZSTARYS. Bronchospasm, rash, and pruritus have been reported in patients who received AZSTARYS.contraindicated

Pediatric Patients 6 to 12 years : Recommended starting dosage is 39.2 mg/7.8 mg orally once daily in the morning. Dosage may be increased to 52.3 mg/10.4 mg daily or decreased to 26.1 mg/5.2 mg daily after one week. Maximum recommended dosage is 52.3 mg/10.4 mg once daily. ( 2.2 ) Adults and Pediatric Patients 13 to 17 years: Recommended starting dosage is 39.2 mg/7.8 mg orally once daily in the morning. Increase the dosage after one week to 52.3 mg/10.4 mg once daily depending on response and tolerability. ( 2.2 ) Administer with or without food. ( 2.3 ) Swallow capsules whole or open and sprinkle onto applesauce or add to water. ( 2.3 ) To avoid substitution errors and overdosage, do not substitute for other methylphenidate products on a milligram-per-milligram basis. ( 2.4 ) 2.1 Pretreatment Screening Prior to treating patients with AZSTARYS, assess: for the presence of cardiac disease (i.e., perform a careful history, family history of sudden death or ventricular arrhythmia, and physical exam) [see Warnings and Precautions ( 5.2 )]. the family history and clinically evaluate patients for motor or verbal tics or Tourette’s syndrome before initiating AZSTARYS [see Warnings and Precautions ( 5.10 )]. 2.2 Recommended Dosage Pediatric Patients 6 to 12 years of age The recommended starting dosage of AZSTARYS is 39.2 mg serdexmethylphenidate/7.8 mg dexmethylphenidate once daily in the morning.

Risks to Patients with Serious Cardiac Disease : Avoid use in patients with known structural cardiac abnormalities, cardiomyopathy, serious cardiac arrhythmias, coronary artery disease, or other serious cardiac disease. (5.2) Increased Blood Pressure and Heart Rate : Monitor blood pressure and pulse. (5.3) Psychiatric Adverse Reactions : Prior to initiating AZSTARYS, screen patients for risk factors for developing a manic episode. If new psychotic or manic symptoms occur, consider discontinuing AZSTARYS. (5.4) Priapism : If abnormally sustained or frequent and painful erections occur, patients should seek immediate medical attention. (5.5) Peripheral Vasculopathy, including Raynaud's Phenomenon : Careful observation for digital changes is necessary during AZSTARYS treatment with ADHD stimulants. Further clinical evaluation (e.g., rheumatology referral) may be appropriate for patients who develop signs or symptoms of peripheral vasculopathy. (5.6) Long-Term Suppression of Growth in Pediatric Patients : Monitor height and weight at appropriate intervals in pediatric patients. (5.7) Acute Angle Closure Glaucoma : AZSTARYS-treated patients considered at risk for acute angle closure glaucoma (e.g., patients with significant hyperopia) should be evaluated by an ophthalmologist. (5.8) Increased Intraocular Pressure (IOP) and Glaucoma : Prescribe AZSTARYS to patients with open-angle glaucoma or abnormally increased IOP only if the benefit of treatment is considered to outweigh the risk. Closely monitor patients with a history of increased IOP or open angle glaucoma.

The following are discussed in more detail in other sections of the labeling: Abuse, Misuse, and Addiction [see Boxed Warning, Warnings and Precautions (5.1) , and Drug Abuse and Dependence (9.2 , 9.3) ] Known hypersensitivity to methylphenidate or other ingredients of AZSTARYS [see Contraindications (4) ] Hypertensive Crisis with Concomitant Use of Monoamine Oxidase Inhibitors [see Contraindications (4) ] Risks to Patients with Serious Cardiac Disease [see Warnings and Precautions (5.2) ] Increased Blood Pressure and Heart Rate [see Warnings and Precautions (5.3) ] Psychiatric Adverse Reactions [see Warnings and Precautions (5.4) ] Priapism [see Warnings and Precautions (5.5) ] Peripheral Vasculopathy, including Raynaud's Phenomenon [see Warnings and Precautions (5.6) ] Long-Term Suppression of Growth in Pediatric Patients [see Warnings and Precautions (5.7) ] Acute Angle Closure Glaucoma [see Warnings and Precautions (5.8) ] Increased Intraocular Pressure and Glaucoma [see Warnings and Precautions (5.9) ] Motor and Verbal Tics, and Worsening of Tourette’s Syndrome [see Warnings and Precautions (5.10) ] Based on accumulated data from other methylphenidate products, the most common (>5% and twice the rate of placebo) adverse reactions are appetite decreased, insomnia, nausea, vomiting, dyspepsia, abdominal pain, weight decreased, anxiety, dizziness, irritability, affect lability, tachycardia, and blood pressure increased. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Corium, LLC at 1-855-253-2407 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ADHD medications, including AZSTARYS, during pregnancy. Healthcare providers are encouraged to register patients by calling the National Pregnancy Registry for Psychostimulants at 1-866-961-2388. Risk Summary There are no available data on AZSTARYS use in pregnant women to evaluate for a drug- associated risk of major birth defects, miscarriage or other adverse maternal or fetal outcomes; however, AZSTARYS contains dexmethylphenidate and serdexmethylphenidate, a prodrug of dexmethylphenidate. Dexmethylphenidate is the d-threo enantiomer of racemic methylphenidate. Published studies and postmarketing reports on methylphenidate use during pregnancy have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. There may be risks to the fetus associated with the use of CNS stimulants use during pregnancy ( see Clinical Considerations ). Embryo-fetal development studies in rats showed delayed fetal skeletal ossification at doses up to 3 times the maximum recommended human dose (MRHD) of 40 mg/day dexmethylphenidate hydrochloride given to adults based on plasma levels.

Metabolism

Serdexmethylphenidate is a prodrug of dexmethylphenidate. Following a single dose administration of 52.3 mg/10.4 mg AZSTARYS and 40 mg of an dexmethylphenidate hydrochloride extended-release (ER) capsule in healthy volunteers under fasted conditions: The mean peak plasma concentration (C max ) of dexmethylphenidate was 14.0 ng/mL and 28.2 ng/mL, respectively; The mean area under concentration curve (AUC) of dexmethylphenidate was 186 hour*ng/mL and 248 hour*ng/mL, respectively.

Clinical Effects of Overdose Overdose of CNS stimulants is characterized by the following sympathomimetic effects: Cardiovascular effects including tachyarrhythmias, and hypertension or hypotension. Vasospasm, myocardial infarction, or aortic dissection may precipitate sudden cardiac death. Takotsubo cardiomyopathy may develop. CNS effects including psychomotor agitation, confusion, and hallucinations. Serotonin syndrome, seizures, cerebral vascular accidents, and coma may occur. Life-threatening hyperthermia (temperatures greater than 104°F) and rhabdomyolysis may develop. Overdose Management Consider the possibility of multiple drug ingestion. The pharmacokinetic profile of AZSTARYS should be considered when treating patients with overdose. Because methylphenidate has a large volume of distribution and is rapidly metabolized, dialysis is not useful. Consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdose management recommendations.

• Mar 2, 2021NDANDA212994Commave Sub

1. 1Drug Ineffective8612%
2. 2Therapeutic Response Shortened588.2%
3. 3Headache425.9%
4. 4Anxiety415.8%
5. 5Insomnia385.4%
6. 6Irritability385.4%
7. 7Decreased Appetite334.7%
8. 8Nausea314.4%
9. 9Disturbance In Attention273.8%
10. 10Fatigue263.7%
11. 11Product Dose Omission Issue233.3%
12. 12Emotional Disorder223.1%
13. 13Heart Rate Increased223.1%
14. 14Anger213.0%
15. 15Suicidal Ideation213.0%

The 7 most recently updated of 7 ClinicalTrials.gov registrations naming Serdexmethylphenidate as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Safety/Tolerability and PK Study With Azstarys® in Children With ADHD
  Completed · Phase 4 · Interventional · 123 enrolled · Corium, Inc.
  NCT05721235updated 2026-05-08
• Duration and Efficacy of Azstarys on Adult ADHD Symptoms and Executive Function in Early Evening
  Completed · Phase 4 · Interventional · 29 enrolled · NYU Langone Health
  NCT06000501updated 2025-07-29
• An Efficacy and Safety Study w/ Azstarys® in Children 4-12 Years of Age With ADHD
  Completed · Phase 4 · Interventional · 246 enrolled · Corium, Inc.
  NCT05685732updated 2025-05-13
• Placebo-Controlled, Double-Blind, Study to Determine the Safety and Efficacy of SDX in Patients With IH
  Completed · Phase 2 · Interventional · 50 enrolled · Zevra Therapeutics
  NCT05668754updated 2025-02-03
• A Study to Evaluate the Efficacy, Safety and Tolerability of Oral AK0901 in Children With ADHD
  Unknown · Phase 3 · Interventional · 50 enrolled · Shanghai Ark Biopharmaceutical Co., Ltd.
  NCT06359899updated 2024-04-11
• KP415 Open-Label Safety Study in Children (6-12 Years of Age) With ADHD
  Completed · Phase 3 · Interventional · 282 enrolled · Zevra Therapeutics
  NCT03460652updated 2021-07-19
• KP415 Classroom Study in Children (6-12 Years of Age) With ADHD
  Completed · Phase 3 · Interventional · 155 enrolled · Zevra Therapeutics
  NCT03292952updated 2021-06-30

Frequently asked questions

How does Serdexmethylphenidate work?

Serdexmethylphenidate is a prodrug of dexmethylphenidate. Dexmethylphenidate HCl is a central nervous system (CNS) stimulant.

What is Serdexmethylphenidate used for?

According to FDA labeling, Serdexmethylphenidate carries indications including: AZSTARYS is indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) in patients 6 years of age and older. Limitations of Use The use of AZSTARYS is not recommended in pediatric patients younger than 6 years of age because they had higher plasma exposure and a higher incidence of adverse reactions (e.g., weight loss) than patients 6 years and older at the same dosage [see Warnings and Precautions ( 5.7 ), Use in Specific Populations ( 8.4 )].. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Serdexmethylphenidate?

Serdexmethylphenidate is classified as Monoamine Oxidase Inhibitors, Central Nervous System Stimulation.

What are the brand names for Serdexmethylphenidate?

Serdexmethylphenidate is marketed under brand names including Azstarys.

What are the contraindications for Serdexmethylphenidate?

Serdexmethylphenidate labeling lists contraindications including: AZSTARYS is contraindicated in patients: with known hypersensitivity to serdexmethylphenidate, methylphenidate, or other components of AZSTARYS. Bronchospasm, rash, and pruritus have been reported in patients who received AZSTARYS.. Always consult the full prescribing information and a clinician.