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List of investigational attention deficit hyperactivity disorder drugs

From Wikipedia, the free encyclopedia

This is a list of investigational attention deficit hyperactivity disorder drugs, or drugs that are currently under development for clinical use in the treatment of attention deficit hyperactivity disorder (ADHD) but are not yet approved.

Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.

This list was last comprehensively updated in September 2021. It is likely to become outdated with time.

Under development

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Preregistration

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  • ATT-377  – Combination treatment of Methylphenidate ER, cyproheptadine [1]
  • TRN-110 [extended-release] – undefined mechanism / extended-release form of an undisclosed drug [2]

Phase 3 clinical trials

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  • Centanafadine [sustained-release] (centanafadine SR, CTN-SR, EB-1020, EB-1020 SR) – serotonin–norepinephrine–dopamine reuptake inhibitor [3]
  • Dexmethylphenidate [controlled release] (CTX-1301) – norepinephrine–dopamine reuptake inhibitor [4]
  • Edivoxetine (LY-2216684) – norepinephrine reuptake inhibitor [5]
  • Molindone [extended-release] (AFX-2201, EN-1733A, molindone XR, SPN-810, SPN-810M, Zalvari) – antipsychotic / dopamine D2 receptor antagonist and serotonin receptor modulator (e.g., serotonin 5-HT2B and 5-HT2A receptor antagonist) — specifically under development for impulsive aggression in ADHD [6][7][8]
  • Serdexmethylphenidate (KP-484) – dexmethylphenidate prodrug / norepinephrine–dopamine reuptake inhibitor [9] [10]
  • Solriamfetol (ADX-N05, ARL-N05, JZP-110, SKL-N05; Sunosi) – norepinephrine–dopamine reuptake inhibitor [11]

Phase 2 clinical trials

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  • CX-717 – ampakine / AMPA receptor modulator [12]
  • Mazindol [controlled release] (NLS-0, NLS-1, NLS-10, NLS-13, NLS-2, Nolazol, Quilience) – serotonin–norepinephrine–dopamine reuptake inhibitor [13]
  • PDC-1421 (BLI-1005) – norepinephrine reuptake inhibitor [14]

Phase 1 clinical trials

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  • AFX-2401 – "neurotransmitter modulator" [15]
  • Atomoxetine [oral solution] (TAH-9922) – norepinephrine reuptake inhibitor [16]
  • Dextroamphetamine [abuse-deterrent immediate-release] (ADAIR) – norepinephrine–dopamine releasing agent [17]

Preclinical/research

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  • Atomoxetine [oral suspension] – norepinephrine reuptake inhibitor [18]
  • Dextroamphetamine [controlled release] (CTX-1302) – norepinephrine–dopamine releasing agent [19]
  • NNI-351 – DYRK1A inhibitor and "neurogenesis enhancer" [20]

No development reported

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  • AFI-002 – undefined mechanism [21]
  • Altropane (123-I Altropane®, [123I]-E-IACFT Injection, [123I]NAV5001, CFT, Iodine-123-E-IACFT Injection, NAV-5001, O-587) – dopamine reuptake inhibitor / single-photon emission-computed tomography enhancer [22]
  • Amphetamine [oral abuse-deterrent immediate-release] (ADAIR) – norepinephrine–dopamine releasing agent [23]
  • Bavisant (BEN-2001, JNJ-1074, JNJ-31001074) – histamine H3 receptor antagonist [24]
  • BCWP-E003 – undefined mechanism [25]
  • BLI-1008 – undefined mechanism [26]
  • Brilaroxazine (RP-5000, RP-5063) – atypical antipsychotic / dopamine receptor partial agonist and serotonin receptor modulator [27]
  • Cannabidiol/gabapentin (Cannbleph) – cannabinoid receptor modulator and gabapentinoid [28]
  • Ciforadenant (CPI-444, V-81444) – adenosine A2A receptor antagonist [29]
  • CM-4612 (CM-ADHD, CM-AT, CM-PK) – gastrointestinal/pancreatic enzyme replacement therapy [30]
  • CRD-102 – undefined mechanism [31]
  • Dasotraline (DSP-225289, SEP-225289, SEP-0225289, SEP-225289-HCI, SEP-289) – serotonin–norepinephrine–dopamine reuptake inhibitor [32]
  • Dextroamphetamine [abuse-resistant] (PF-08, PFR 08001, PFR08026) – norepinephrine–dopamine releasing agent [33]
  • Dextroamphetamine sulfate [modified release capsules] (HLD-900, HLD-100) – norepinephrine–dopamine releasing agent [34]
  • Dopamine [intranasal] (DopaMat, MPP-18) – dopamine receptor agonist [35]
  • Eltoprazine (DU-28853) – serotonin 5-HT1A and 5-HT1B receptor agonist [36]
  • Fasoracetam [co-crystallised] (AEVI-004, NFC-1) – racetam / metabotropic glutamate receptor modulator [37]
  • GTS-21 (DMXB-A, DMXB-A sustained release, DMXB-A-SR) – α7 nicotinic acetylcholine receptor agonist [38]
  • Guanfacine [once-daily] (Guanfacine Carrier Wave, SPD-547) – α2-adrenergic receptor agonist [39]
  • IPX-233 (IPX233 ER C0003, IPX233-C0001, IPX233-C0002, IPX233-T0001, IPX233-T0002) – central nervous system stimulant [40]
  • Masupirdine (M1, M1 of SUVN-502, SUVN-502, SVN-502) – serotonin 5-HT6 receptor antagonist [41]
  • Methylphenidate [extended-release/abuse-resistant] (COL-171) – norepinephrine–dopamine reuptake inhibitor [42]
  • Methylphenidate [fast dissolve tablet] [Samyang Holdings Biopharmaceuticals] – norepinephrine–dopamine reuptake inhibitor [43]
  • Methylphenidate [transdermal system] (SHX-009) – norepinephrine–dopamine reuptake inhibitor [44] [45]
  • Methylphenidate/naltrexone (AVK-001) – norepinephrine–dopamine reuptake inhibitor and opioid receptor antagonist [46]
  • Nic-12 – undefined mechanism [47]
  • NLS-2 – antianaemic / heavy metal / iron replacement [48]
  • PD-3044 – dopamine reuptake inhibitor [49]
  • Pitolisant (tiprolisant; BF-2.649, BF-2649, Ozawade, Wakix) – histamine H3 receptor antagonist [50]
  • R-Sibutramine metabolite ((+)-desmethylsibutramine, (+)-didesmethylsibutramine, R-DDMS, R-desmethylsibutramine, R-didesmethylsibutramine) – serotonin–norepinephrine–dopamine reuptake inhibitor [51]
  • Selegiline [transdermal] (Emsam) – monoamine oxidase B inhibitor [52]
  • SKL-13865 (SKL-ADHD) – norepinephrine–dopamine reuptake inhibitor [53]
  • Sofinicline (A-422894.0, ABT-894) – α4β2 nicotinic acetylcholine receptor modulator [54]
  • SPN-811 – undefined mechanism [55]
  • Taminadenant (NIR-178, PBF-509) – adenosine A2A receptor antagonist [56]

Research programmes

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  • Ampakines / AMPA receptor modulators [RespireRx] (CX-516, CX-614, CX-707, CX-929, CX-1501, CX-1763, CX-1796, CX-1837, CX-1846, CX-1942, CX-2007, CX-2076) [57]
  • Cannabis extracts [Cannabis Science] (CBIS GAP-001, CBIS LC-001, CBIS OBLD-001, CBIS OCD-001, CBIS PC-001, CBIS PPC-001, CBIS PS-001, CBIS SD-001, CBIS SSA-001, CBIS-OS-001, CBIS-PTSD-001, CS NEURO 1, CS-S/BCC-1, CS-TATI-1) – cannabinoid receptor modulators [58]
  • Norepinephrine reuptake inhibitors / adrenergic receptor antagonists [Pfizer] (NRI-022, NRI-193, WAY-253203, WAY-256805, WAY-260022, WAY-315193, WAY-318068) [59]
  • Pim2 / PolyPhetamine [ITL Pharma] [60]
  • Subtype-selective glutamate NMDA receptor modulators / glutamate NR2B receptor modulators [Novartis] [61]

Not under development

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Development discontinued

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  • ABT-418 – nicotinic acetylcholine receptor agonist [62]
  • Amphetamine [transdermal patch] [Noven/Takeda] – norepinephrine–dopamine releasing agent [63]
  • Ampreloxetine (TD-9855) – norepinephrine reuptake inhibitor [64]
  • AR-08 – adrenergic receptor agonist [65]
  • Aripiprazole (Abilify, Abilify Maintena, Abilify MyCite, Abilitat, Ao Pai, Aripiprazole depot, Aripiprazole ECER tablets, Arlemide; OPC-14597, OPC-14597 IMD, OPC-31) – atypical antipsychotic / dopamine receptor partial agonist and serotonin receptor modulator [66]
  • AZD-5213 – histamine H3 receptor antagonist [67]
  • Bifemelane (SON-216) – monoamine oxidase inhibitor and weak norepinephrine reuptake inhibitor [68]
  • Bradanicline (ATA-101, TC-0569, TC-5619, TC-5619-238) – α7 nicotinic acetylcholine receptor agonist [69]
  • Brexpiprazole (Rexulti, Rxulti; Lu-AF41156, OPC-34712, OPDC-34712) – atypical antipsychotic / dopamine receptor partial agonist and serotonin receptor modulator [70]
  • Buspirone [transdermal] (BuSpar Patch) – serotonin 5-HT1A receptor partial agonist, other actions [71]
  • Cipralisant (GT-2331; Perceptin) – histamine H3 receptor antagonist [72]
  • CX-516 (1-BCP, AMPAlex, BDP-12, SPD-420) – ampakine / AMPA receptor modulator [73]
  • CX-1739 – ampakine / AMPA receptor modulator [74]
  • Donepezil (Aricept, Aricept D, Aricept Dry Syrup, Aricept Evess, Aricept ODT, Aricept SR, Donepezil SR, E-2020, E-2022, Eranz) – acetylcholinesterase inhibitor [75]
  • Droxidopa (3,4-dihydroxyphenylserine, 3,4-threo-DOPS, L-threo-dihydroxyphenylserine, L-threodops, Northera, threo-dopaserine, threo-DOPS) – prodrug of norepinephrine / adrenergic receptor agonist [76]
  • Fasoracetam (AEVI-001, LAM-105, MDGN-001, NFC-1, NS-105) – racetam / metabotropic glutamate receptor modulator [77]
  • Ispronicline (AZD-3480, RJR-1734, TC 01734, TC-1734, TC-1734-112) – α4β2-nicotinic acetylcholine receptor agonist [78]
  • KP-106 (dextroamphetamine prodrug oral film) – norepinephrine–dopamine releasing agent [79]
  • Lauflumide (flmodafinil, bisfluoromodafinil; NLS-14, NLS-4) – weak dopamine reuptake inhibitor, possibly other actions [80]
  • Manifaxine (BW-1555U88, GW-320659) – norepinephrine–dopamine reuptake inhibitor [81]
  • Mecamylamine (Inversine, Tridmac) – nicotinic acetylcholine receptor antagonist [82]
  • MEM-68626 – 5-HT6 receptor antagonist [83]
  • Metadoxine [sustained/extended-release] (pyridoxine-pyrrolidone carboxylate, pyridoxine pidolate; MDX, metadoxine SR, MG-01CI) – serotonin 5-HT2B receptor antagonist, GABA modulator, other actions [84]
  • Methylphenidate [transdermal patch] (TAH-9901) – norepinephrine–dopamine reuptake inhibitor [85]
  • MK-0249 – histamine H3 receptor antagonist [86]
  • Modafinil (AFT-801, Alertec, Attenace, CN-801, CRL-40476, Modasamil, Modasonil, Modavigil, Modiodal, Provigil, Sparlon, Vigil) – weak dopamine reuptake inhibitor, possibly other actions [87]
  • Nicotine/opipramol (ND-0801; opipramol/nicotine) – tricyclic antidepressant / monoamine and sigma receptor modulator and nicotinic acetylcholine receptor agonist [88]
  • NLS-8 – (melafenoxate) undefined mechanism [89][90]
  • NS-2359 (GSK-372475) – serotonin–norepinephrine–dopamine reuptake inhibitor [91]
  • OPC-64005 – serotonin–norepinephrine–dopamine reuptake inhibitor [92]
  • ORG-26576 (ORG26576) – ampakine / AMPA receptor modulator [93]
  • PF-3654746 (PF-03654746) – histamine H3 receptor antagonist [94]
  • Phacetoperane (NLS-3) – methylphenidate analogue / central nervous system stimulant / norepinephrine–dopamine reuptake inhibitor (?) [95]
  • Pirepemat (IRL-752) – "cortical enhancer" / serotonin 5-HT7 receptor antagonist and α2C-adrenergic receptor antagonist, other actions [96][97]
  • Pozanicline (A-87089.0, ABT-089) – α4β2 nicotinic acetylcholine receptor agonist [98]
  • SEP-225432 – serotonin–norepinephrine–dopamine reuptake inhibitor [99]
  • SGS-742 (CGP-36742, DVD-742, Lu-AE58479, SGS-742) – GABAB receptor antagonist [100]
  • SPD-483 – undefined mechanism [101]
  • SPD-554 (Guanfacine Carrier Wave project) – α2-adrenergic receptor agonist [102]
  • SPI-339 (NEO-339) – undefined mechanism [103]
  • TAK-137 – AMPA receptor potentiator [104]
  • TC-6683 (AZD 1446, TC-6683) – α4β2 nicotinic acetylcholine receptor agonist [105]
  • Tipepidine [sustained-release] (TS-141) – GIRK inhibitor [106]
  • Vortioxetine (Brintellix, LU-AA21004, LuAA 21004, Trintellix) – antidepressant / serotonin reuptake inhibitor and serotonin receptor modulator [107]

Research programmes

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  • Potassium channel modulators [Astellas Pharma/Icagen] [108]

Formal development never or not yet started

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Clinically used drugs

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Approved drugs

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Norepinephrine–dopamine releasing agents

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Norepinephrine–dopamine reuptake inhibitors

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Norepinephrine reuptake inhibitors

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α2-Adrenergic receptor agonists

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Off-label drugs

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See also

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References

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  1. ^ "ClinicalTrials.gov". clinicaltrials.gov.
  2. ^ "TRN 110 - AdisInsight". adisinsight.springer.com.
  3. ^ "Centanafadine - Otsuka Pharmaceutical - AdisInsight". adisinsight.springer.com.
  4. ^ "Dexmethylphenidate controlled release - Cingulate Therapeutics - AdisInsight". adisinsight.springer.com.
  5. ^ "Edivoxetine - AdisInsight". adisinsight.springer.com.
  6. ^ "Molindone - Supernus Pharmaceuticals - AdisInsight". adisinsight.springer.com.
  7. ^ Ceresoli-Borroni G, Nasser A, Adewole T, Liranso T, Xu J, Schwabe S, Findling RL (September 2021). "A Double-Blind, Randomized Study of Extended-Release Molindone for Impulsive Aggression in ADHD". J Atten Disord. 25 (11): 1564–1577. doi:10.1177/1087054720909084. PMID 32338106. S2CID 216556900.
  8. ^ Robb AS, Connor DF, Amann BH, Vitiello B, Nasser A, O'Neal W, Schwabe S, Ceresoli-Borroni G, Newcorn JH, Candler SA, Buitelaar JK, Findling RL (March 2020). "Closing the gap: unmet needs of individuals with impulsive aggressive behavior observed in children and adolescents". CNS Spectr. 26 (5): 448–456. doi:10.1017/S1092852920001224. hdl:2066/241059. PMID 32228725. S2CID 214750205.
  9. ^ "KP484". Archived from the original on 2018-03-08.
  10. ^ Marino, Dan (March 4, 2019). "PRODRUG TECHNOLOGY - Prodrugs for ADHD Treatments: Opportunities & Potential to Fill Unmet Medical Needs".
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  27. ^ "Brilaroxazine - Reviva Pharmaceuticals - AdisInsight". adisinsight.springer.com.
  28. ^ "Research programme: cannabinoid-based therapeutics - Axim Biotechnologies - AdisInsight". adisinsight.springer.com.
  29. ^ "Ciforadenant - Corvus Pharmaceuticals - AdisInsight". adisinsight.springer.com.
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  41. ^ "Masupirdine - Suven Life Sciences - AdisInsight". adisinsight.springer.com.
  42. ^ "Methylphenidate extended-release/abuse-resistant - Collegium Pharmaceutical - AdisInsight". adisinsight.springer.com.
  43. ^ "Research programme: fast dissolve tablet therapeutics - Samyang - AdisInsight". adisinsight.springer.com.
  44. ^ "SHX 009 - AdisInsight". adisinsight.springer.com.
  45. ^ https://www.dazhoubiomed.com/cpgx
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  50. ^ "Pitolisant - Bioprojet - AdisInsight". adisinsight.springer.com.
  51. ^ "R-sibutramine metabolite - Sepracor - AdisInsight". adisinsight.springer.com.
  52. ^ "Selegiline transdermal - Somerset Pharmaceuticals - AdisInsight". adisinsight.springer.com.
  53. ^ "SKL 13865 - AdisInsight". adisinsight.springer.com.
  54. ^ "Sofinicline - AdisInsight". adisinsight.springer.com.
  55. ^ "SPN 811 - AdisInsight". adisinsight.springer.com.
  56. ^ "Taminadenant - Novartis/Palobiofarma - AdisInsight". adisinsight.springer.com.
  57. ^ "Research programme: AMPA receptor agonists - RespireRx - AdisInsight". adisinsight.springer.com.
  58. ^ "Research programme: cannabis extract therapeutics - Cannabis Science - AdisInsight". adisinsight.springer.com.
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  61. ^ "Research programme: subtype-selective NMDA receptor modulators - Novartis - AdisInsight". adisinsight.springer.com.
  62. ^ "ABT 418 - AdisInsight". adisinsight.springer.com.
  63. ^ "Research programme: transdermal amfetamine patch - Noven/Takeda - AdisInsight". adisinsight.springer.com.
  64. ^ "Ampreloxetine - Theravance Biopharma - AdisInsight". adisinsight.springer.com.
  65. ^ "AR 08 - AdisInsight". adisinsight.springer.com.
  66. ^ "Aripiprazole - Bristol-Myers Squibb/Otsuka Pharmaceutical - AdisInsight". adisinsight.springer.com.
  67. ^ "AZD 5213 - AdisInsight". adisinsight.springer.com.
  68. ^ "Research programme: attention deficit hyperactivity disorder therapies - Nxera Pharma - AdisInsight". adisinsight.springer.com.
  69. ^ "Bradanicline - CODA Biotherapeutics - AdisInsight". adisinsight.springer.com.
  70. ^ "Brexpiprazole - Lundbeck/Otsuka - AdisInsight". adisinsight.springer.com.
  71. ^ "Buspirone transdermal - Bristol-Myers Squibb/Elan - AdisInsight". adisinsight.springer.com.
  72. ^ "Cipralisant - AdisInsight". adisinsight.springer.com.
  73. ^ "CX 516 - AdisInsight". adisinsight.springer.com.
  74. ^ "CX 1739 - AdisInsight". adisinsight.springer.com.
  75. ^ "Donepezil - Eisai - AdisInsight". adisinsight.springer.com.
  76. ^ "Droxidopa - Sumitomo Pharma/Lundbeck - AdisInsight". adisinsight.springer.com.
  77. ^ "Fasoracetam - Avalo Therapeutics - AdisInsight". adisinsight.springer.com.
  78. ^ "Ispronicline - AdisInsight". adisinsight.springer.com.
  79. ^ "KP 106 - AdisInsight". adisinsight.springer.com.
  80. ^ "Lauflumide - NLS Pharmaceutics Ltd - AdisInsight". adisinsight.springer.com.
  81. ^ "Manifaxine - AdisInsight". adisinsight.springer.com.
  82. ^ "Mecamylamine - Targacept - AdisInsight". adisinsight.springer.com.
  83. ^ "Research programme: serotonin 6 receptor antagonists - Memory Pharmaceuticals - AdisInsight". adisinsight.springer.com.
  84. ^ "Metadoxine extended-release - Arcturus Therapeutics - AdisInsight". adisinsight.springer.com.
  85. ^ https://adisinsight.springer.com/drugs/800053853
  86. ^ "MK 0249 - AdisInsight". adisinsight.springer.com.
  87. ^ "Modafinil - Teva Pharmaceutical Industries - AdisInsight". adisinsight.springer.com.
  88. ^ "Nicotine/opipramol - NeuroDerm - AdisInsight". adisinsight.springer.com.
  89. ^ "NLS 8 - AdisInsight". adisinsight.springer.com.
  90. ^ "NLS Pharmaceutics Announces an R&D Update Webcast to Review the Company's Growing Portfolio of Pre-Clinical Compounds".
  91. ^ "NS 2359 - AdisInsight". adisinsight.springer.com.
  92. ^ "OPC 64005 - AdisInsight". adisinsight.springer.com.
  93. ^ "ORG 26576 - AdisInsight". adisinsight.springer.com.
  94. ^ "PF 3654746 - AdisInsight". adisinsight.springer.com.
  95. ^ "Phacetoperane - NLS Pharmaceutics Ltd - AdisInsight". adisinsight.springer.com.
  96. ^ "Pirepemat - Integrative Research Laboratories - AdisInsight". adisinsight.springer.com.
  97. ^ Hjorth S, Waters S, Waters N, Tedroff J, Svensson P, Fagerberg A, Edling M, Svanberg B, Ljung E, Gunnergren J, McLean SL, Grayson B, Idris NF, Neill JC, Sonesson C (September 2020). "(3S)-3-(2,3-difluorophenyl)-3-methoxypyrrolidine (IRL752) -a Novel Cortical-Preferring Catecholamine Transmission- and Cognition-Promoting Agent". J Pharmacol Exp Ther. 374 (3): 404–419. doi:10.1124/jpet.120.000037. hdl:10454/17970. PMID 32605972. S2CID 220283184.
  98. ^ "Pozanicline - AdisInsight". adisinsight.springer.com.
  99. ^ "SEP 228432 - AdisInsight". adisinsight.springer.com.
  100. ^ "SGS 742 - AdisInsight". adisinsight.springer.com.
  101. ^ "SPD 483 - AdisInsight". adisinsight.springer.com.
  102. ^ "SPD 554 - AdisInsight". adisinsight.springer.com.
  103. ^ "SPI 339 - AdisInsight". adisinsight.springer.com.
  104. ^ "TAK 137 - AdisInsight". adisinsight.springer.com.
  105. ^ "TC 6683 - AdisInsight". adisinsight.springer.com.
  106. ^ "Tipepidine - Taisho Pharmaceutical - AdisInsight". adisinsight.springer.com.
  107. ^ "Vortioxetine - Lundbeck - AdisInsight". adisinsight.springer.com.
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Further reading

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