TABLE 1.
Drugs approved for ADHD and other indications encountered in clinical trials.
| Agent name | Agent type | Agent class | Approval overall | Approval ADHD | Targets | First approved indication |
|---|---|---|---|---|---|---|
| Memantine hydrochloride | Small molecule | Dementia therapeutic agent | 2003 | GRIN1; GRIN2A; GRIN2B; GRIN2C; GRIN2D; GRIN3A; GRIN3B | Dementia of the Alzheimer’s type | |
| Methylphenidate hydrochloride | Small molecule | CNS stimulant | 1955 | 1955 | SLC6A3 | ADHD |
| Methylphenidate transdermal system | Small molecule | CNS stimulant | 2006 | 2006 | SLC6A3 | ADHD |
| Lisdexamfetamine dimesylate | Small molecule | CNS stimulant | 2007 | 2007 | SLC6A2; SLC6A3 | ADHD |
| Viloxazine | Small molecule | Selective noradrenaline reuptake inhibitor | 2021 | 2021 | SLC6A2 | ADHD |
| Amiloride hydrochloride | Small molecule | Diuretic | 1981 | SCNN1A; SCNN1B; SCNN1G; SCNN1D | Congestive heart failure; Hypertension | |
| Amphetamine sulfate | Small molecule | CNS stimulant | 1984 | 1984 | SLC18A2; SLC6A2; SLC6A3; CARTPT; TAAR1; VMAT2; MAOA; MAOB | ADHD |
| Dextroamphetamine sulfate | Small molecule | CNS stimulant | 1976 | 1976 | SLC18A2; SLC6A2; SLC6A3 | ADHD |
| Dexmethylphenidate hydrochloride | Small molecule | CNS stimulant | 2001 | 2001 | SLC6A3; SLC6A2 | ADHD |
| Mixed amphetamine salts | Small molecule | CNS stimulant | 2001 | 2001 | SLC18A2; SLC6A2; SLC6A3 | ADHD |
| Atomoxetine | Small molecule | Selective noradrenaline reuptake inhibitor | 2002 | 2002 | SLC6A2 | ADHD |
| Guanfacine hydrochloride | Small molecule | Alpha2 adrenergic receptor agonist | 1986 | 2009 | ADRA2A | Hypertension |
| Clonidine hydrochloride | Small molecule | Alpha2 adrenergic receptor agonist | 1974 | 2010 | ADRA2A; ADRA2B; ADRA2C | Hypertension |
| Molindone hydrochloride | Small molecule | Typical antipsychotic | 1974 | DRD2 | Schizophrenia | |
| Modafinil | Small molecule | CNS stimulant | 1998 | SLC6A3 | Narcolepsy; OSA; SWD | |
| Galantamine hydrobromide | Small molecule | Dementia therapeutic agent | 2001 | ACHE; CHRNA7 | Dementia of the Alzheimer’s type | |
| SDX CL/d-MPH Cl | Small molecule | CNS stimulant | 2021 | 2021 | SLC6A3; SLC6A2 | ADHD |
| Quetiapine | Small molecule | Atypical antipsychotic | 1997 | HTR2A; DRD2 | Schizophrenia | |
| Naltrexone hydrochloride | Small molecule | Opiate antagonist | 1984 | OPRD1; OPRM1; OPRK1; SIGMAR1 | Opioid dependence | |
| Ramelteon | Small molecule | Sedative-hypnotic | 2005 | MTNR1A; MTNR1B | Insomnia | |
| Amantadine | Small molecule | Antiparkinson agent | 1966 | M; GRIN3A; DRD2 | Parkinson’s disease | |
| Bupropion hydrochloride | Small molecule | Antidepressant | 1985 | SLC6A2; SLC6A3 | Major depressive disorder | |
| Vortioxetine | Small molecule | Antidepressant | 2013 | SLC6A4; HTR3A; HTR7; HTR1B; HTR1A | Major depressive disorder | |
| Aripiprazole | Small molecule | Atypical antipsychotic | 2002 | DRD2; HTR2A | Schizophrenia | |
| Mazindol | Small molecule | Anoretic | 1973 | SLC6A2; SLC6A3; SLC6A4 | Duchenne muscular dystrophy | |
| Varenicline | Small molecule | Smoking cessation aid | 2006 | CHRNA4 | Smoking addiction | |
| Droxidopa | Small molecule | Antiparkinson agent | 2014 | ADRA1A; ADRA1B; ADRA1D; ADRA2A; ADRA2B; ADRA2C; ADRB1; ADRB2; ADRB3 | Neurogenic orthostatic hypotension | |
| Carbidopa | Small molecule | Antiparkinson agent | 2014 | DDC | Parkinson’s disease | |
| Duloxetine hydrochloride | Small molecule | Antidepressant | 2004 | SLC6A4; SLC6A2 | MDD; GAD; DPNP; Fibromyalgia; CMP | |
| Zolpidem tartrate | Small molecule | Sedative-hypnotic | 1992 | GABRA1 | Insomnia | |
| Eszopiclone | Small molecule | Sedative-hypnotic | 2004 | GABRA1; GABRA2; GABRA3; GABRA4; GABRA5; GABRA6; GABRB1; GABRB2; GABRB3; GABRD; GABRE; GABRG1; GABRG2; GABRG3; GABRP; GABRQ | Insomnia | |
| Buspirone hydrochloride | Small molecule | Anxiolytic agent | 1986 | HTR1A; DRD2 | Anxiety disorders | |
| Valproate sodium | Small molecule | Anticonvulsant agent | 1996 | HDAC9 | Complex partial seizures; Simple and complex absence seizures | |
| Risperidone | Small molecule | Atypical antipsychotic | 1993 | DRD2; HTR2A | Schizophrenia | |
| Brexpiprazole | Small molecule | Atypical antipsychotic | 2015 | HTR1A; DRD2; HTR2A; ADRA2C; ADRA1B | MDD; Schizophrenia | |
| Divalproex sodium | Small molecule | Anticonvulsant agent | 1983 | HDAC9 | Complex partial seizures; Simple and complex absence seizures | |
| Olanzapine | Small molecule | Atypical antipsychotic | 1996 | HTR2A; DRD2 | Schizophrenia; BD-I; Agitation associated with schizophrenia/BD-I | |
| Oxytocin | Biotech | Uterotonic agent | 1980 | OXTR | Initiation or improvement of uterine contractions | |
| Fluvoxamine maleate | Small molecule | Antidepressant | 1994 | SLC6A4 | OCD |
This table presents information about drug agents approved either for ADHD or other indications that appeared in clinical trials on ADHD. All data regarding agent name, agent type, agent class, years of approval overall and for ADHD, targets, and first approved indication was taken directly from go.drugbank.com, genome. jp, and fda.gov. Gene names were used for the indication of targets. For a list of all protein names, see Supplementary Material S5 (box). Data is due 4 January 2021. Abbreviations: CNS, central nervous system; ADHD, attention deficit hyperactivity disorder.