| Candidate ID: | R1603 |
| Source ID: | DB16629 |
| Source Type: | approved |
| Compound Type: |
small molecule
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| Compound Name: |
Serdexmethylphenidate
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| Synonyms: |
Serdexmethylphenidate
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| Molecular Formula: |
C25H29N3O8
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| SMILES: |
[H][C@@]1(CCCCN1C(=O)OC[N+]1=CC=CC(=C1)C(=O)N[C@@H](CO)C([O-])=O)[C@H](C(=O)OC)C1=CC=CC=C1
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| Structure: |
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| DrugBank Description: |
Attention Deficit Hyperactivity Disorder (ADHD) is an early-onset neurodevelopmental disorder that often extends into adulthood and is characterized by developmentally inappropriate and impaired attention, impulsivity, and motor hyperactivity. The underlying cause of ADHD is unclear but likely involves dysfunction in dopaminergic and noradrenergic neurotransmission, as evidenced by the clear beneficial effect of CNS stimulants such as and that increase extracellular dopamine and norepinephrine levels. Serdexmethylphenidate is a prodrug of the CNS stimulant , a common first-line treatment for ADHD, that is combined with to provide extended plasma concentrations and therapeutic benefit with once-daily dosing.
Serdexmethylphenidate was granted FDA approval on March 2, 2021, and is currently marketed as a combination capsule with under the trademark AZSTARYS™ by KemPharm, Inc.
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| CAS Number: |
1996626-29-9
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| Molecular Weight: |
499.52
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| DrugBank Indication: |
Serdexmethylphenidate is a prodrug of that is indicated in combination with for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) in patients aged six years and older.
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| DrugBank Pharmacology: |
Serdexmethylphenidate is a prodrug of the CNS stimulant , which increases extracellular levels of dopamine and norepinephrine in the CNS, leading to altered neurotransmission. As a CNS stimulant, serdexmethylphenidate carries a risk of abuse, misuse, and dependence, which should be monitored. Also, CNS stimulants are associated with increased blood pressure, heart rate, and risk of serious cardiovascular reactions, including stroke, myocardial infarction, and sudden death; patients should be assessed before starting therapy and monitored for cardiovascular abnormalities. Similarly, CNS stimulants may also result in peripheral vasculopathy, including Raynaud's phenomenon. Due to its ability to alter neurological function, serdexmethylphenidate may exacerbate pre-existing psychoses, induce manic episodes in patients with bipolar disorder, or result in newly diagnosable manic or psychotic symptoms. Frequent, sustained, and painful erections, which may require medical attention, have been observed in patients who have been treated for some time with serdexmethylphenidate, often associated with a dose increase. Finally, like other CNS stimulants, serdexmethylphenidate has been associated with weight loss and growth retardation, which may require treatment interruption in serious cases.
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| DrugBank MoA: |
Attention Deficit Hyperactivity Disorder (ADHD) is an early-onset neurodevelopmental disorder that often extends into adulthood and is characterized by developmentally inappropriate and impaired attention, impulsivity, and motor hyperactivity. Proper diagnosis is hindered by a lack of biological markers (based on symptoms alone), a spectrum of severity, and frequent comorbidities such as autism spectrum disorder, reading disabilities, developmental coordination disorders, and tic disorders. Although the underlying cause(s) is unclear, dopaminergic, noradrenergic, serotonergic, cholinergic, glutaminergic, and opioid neurotransmission likely plays a role.
Serdexmethylphenidate is a prodrug of the CNS stimulant (MPH), a common first-line treatment for ADHD. The main effect of MPH is to increase the extracellular levels of dopamine and norepinephrine, which has numerous potential downstream effects. This occurs mainly due to MPH's ability to inhibit the corresponding dopamine and norepinephrine monoamine transporters. Other studies have suggested additional possible MPH functions, including serotonin 5-HT1A receptor agonism, redistribution of vesicular monoamine transporter-2 (VMAT-2), and either direct or indirect activation of α2-adrenergic receptors. Overall, imaging studies reveal that MPH acts to alter brain activity in relevant regions associated with executive function, emotional regulation, reward processing, and working memory.
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| Targets: |
Sodium-dependent dopamine transporter inhibitor; Sodium-dependent noradrenaline transporter inhibitor; 5-hydroxytryptamine receptor 1A agonist
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| Inclusion Criteria: |
Therapeutic strategy associated
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