This list is regulary updated by Neurotransmitter.net's Drug Pipeline Expert, JR Becker (jrbecker76@hotmail.com). Shawn Thomas (shawn@neurotransmitter.net) is responsible for additions, editing, and fact-checking. Dr. Louis Sanfilippo, Professor of Clinical Psychiatry at Yale, is also a valued contributor to this groundbreaking and widely appreciated list.
Treatments for Depression and Anxiety
| Drug Name | Pharmacologic Action | Company | Indication | Developmental Phase | Links |
| Pristig ® (DVS-233 SR, desvenlafaxine) | Metabolite of Effexor ® (venlafaxine) | Wyeth | Depression, anxiety | Approved | [ClinicalTrials.gov] |
| Valdoxan (agomelatine, AGO 178) | 5-HT2C antagonist, 5-HT2B antagonist, melatonin M1/M2 receptor agonist | Servier, Novartis | Depression, anxiety, sleep disorders | EU: Resubmitted. Decision expected in mid-2008 US: Phase III |
[Receptor activity] [Oct 2005 press release] [ClinicalTrials.gov] |
| Saredutant (SR 48968) | NK2 neurokinin receptor antagonist | Sanofi-Aventis | Depression, anxiety | Phase III - submission expected in the second half of 2008 | [Effects of SR 48968 on rodents] [ClinicalTrials.gov] |
| Amibegron, SR 58611 | beta-3-adrenoceptor agonist | Sanofi-Aventis | Depression, anxiety | Phase III | [ClinicalTrials.gov] |
| Vilazodone | 5-HT1A partial agonist, serotonin reuptake inhibitor | Clinical Data Online, Inc. | Depression | Phase III | [January 2007 Press Release] [ClinicalTrials.gov] |
| Pexacerfont, BMS-562086 | CRF1 antagonist | Bristol-Myers Squibb | Depression, anxiety | Phase III | [ClinicalTrials.gov] |
| Lu AA21004 | bis-aryl-sulphanyl modulator | Lundbeck | Depression, anxiety | Phase III | [ClinicalTrials.gov] |
| PD-0332334 | Alpha2delta calcium channel blocker | Pfizer | Anxiety | Phase III | [ClinicalTrials.gov] |
| LY2216684 | Norepinephrine reuptake inhibitor | Eli Lilly | Depression, ADHD | Phase II | [ClinicalTrials.gov] |
| SSR149415 | V1B antagonist | Sanofi-Aventis | Depression, anxiety, hyperphagia | Phase II | [SSR149415 review] [ClinicalTrials.gov] |
| GSK 372475 (NS2359) | Dopamine, serotonin, and norepinephrine, reuptake inhibitor | GSK, NeuroSearch | Depression | Phase II | [ClinicalTrials.gov] |
| TIK-101 | NMDA partial agonist | Tikvah Pharmaceuticals | Anxiety disorders | Phase II | |
| GSK 856553 | P38 kinase inhibitor | GSK | Depression | Phase II | [ClinicalTrials.gov] |
| DOV 21, 947 | Dopamine, serotonin, and norepinephrine, reuptake inhibitor | DOV/Merck | Depression, ADHD, RLS | Phase II | [Antidepressant-like actions of DOV 21,947] [ClinicalTrials.gov] |
| AZD6765 | NMDA antagonist | AstraZeneca | Depression, anxiety | Phase II | [ClinicalTrials.gov] |
| SEP-225289 | DA/NE/5-HT reuptake inhibitor | Sepracor | Depression, anxiety | Phase II | [ClinicalTrials.gov] |
| JNJ-18038683 | E-mail shawn@neurotransmitter.net if you can share details about how this drug works. | Johnson & Johnson | Depression | Phase II | [ClinicalTrials.gov] |
| ORG 34517/34850 | GR antagonist | Schering-Plough | Depression | Phase II | [ClinicalTrials.gov] |
| Nemifitide (INN 00835) |
Pentapeptide analog of melanocyte-inhibiting factor (MIF-1) administered intravenously (mechanism unknown) | Tetragenex | Depression | Phase II | [Innapharma's info] [Antidepressant-like effects of a novel pentapeptide, nemifitide, in an animal model of depression] [MIF-1 may regulate ACTH secretion] [ClinicalTrials.gov] |
| Vabicaserin (SCA-136) | 5-HT2C agonist | Wyeth | Depression, anxiety | Phase II | [ClinicalTrials.gov] |
| Lu AA24530 | Mixed serotonin modulator | Lundbeck | Depression, anxiety | Phase II | [ClinicalTrials.gov] |
| Adipiplon (formerly NG2-73) | Partial GABA-A receptor agonist that is preferential for alpha3 subunit-containing receptors | Neurogen | Anxiety, sleep disorders | Phase II | |
| YKP-10A, R228060 | Phenylalanine derivative with unknown mechanism | Johnson & Johnson/SK Pharmaceuticals | Depression | Phase II | [First Phase II Study] [ClinicalTrials.gov] |
| ONO-2333Ms | CRF1 antagonist | Ono Pharmaceuticals | Depression, anxiety | Phase II | [ClinicalTrials.gov] |
| ORG 26576 | AMPA receptor modulator | Schering-Plough | Depression | Phase II | [ClinicalTrials.gov] |
| TC-5214 | Nonselective Nicotinic acetylcholine receptor antagonist | Targacept | Depression | Phase II | [ClinicalTrials.gov] |
| TGWOOAD/AA | 5-HT1A agonist, 5-HT2 antagonist | Fabre-Kramer | Anxiety | Phase II | [Fabre-Kramer's info] [ClinicalTrials.gov] |
| TGBA01AD | Serotonin reuptake inhibitor, 5-HT2 agonist, 5-HT1A agonist, and 5-HT1D agonist | Fabre-Kramer | Depression | Phase II | [Fabre-Kramer's info] [ClinicalTrials.gov] |
| GW823296 (orvepitant) | NK1 antagonist | GSK | Depression, anxiety | Phase I | [ClinicalTrials.gov] |
| Tyrima™ | Reversible monoamine oxidase A (MAO-A) inhibitor | CeNeRx | Depression, anxiety | Phase I | [ClinicalTrials.gov] |
| PRE703 | MgluR agonist | Prescient | Anxiety | Phase I | [ClinicalTrials.gov] |
| Delucemine, NPS 1506 | NMDA antagonist | NPS | Depression, stroke | Phase I | |
| Lu AA34893 | E-mail shawn@neurotransmitter.net if you can share details about how this drug works. | Lundbeck | Bipolar depression, anxiety | Phase I | [ClinicalTrials.gov] |
| AFQ056 | mGluR5 receptor antagonist | Novartis | Anxiety | Phase I | [ClinicalTrials.gov] |
| JNJ-19567470, TS-041 | CRF1 antagonist | Janssen (Johnson & Johnson), Taisho | Depression, anxiety | Phase I | [ClinicalTrials.gov] |
| SSR 125543 | CRF1 antagonist | Sanofi-Aventis | Depression, anxiety, hyperphagia | Phase I | [ClinicalTrials.gov] |
| YKP3089 | Undisclosed mechanism of action | SK Pharmaceuticals | Anxiety | Phase I | [ClinicalTrials.gov] |
| GSK 588045 | 5-HT1 antagonist | GSK | Depression, anxiety | Phase I | [ClinicalTrials.gov] |
| GSK 163090 | 5-HT1 antagonist | GSK | Depression, anxiety | Phase I | [ClinicalTrials.gov] |
| TC-2216 | Nicotinic acetylcholine receptor (alpha4beta2) antagonist | Targacept | Depression | Phase I | [ClinicalTrials.gov] |
| AZD2327 | Enkephalinergic modulator | AstraZeneca | Anxiety | Phase I | [ClinicalTrials.gov] |
| R1647 | E-mail shawn@neurotransmitter.net if you can share details about how this drug works. | Roche | Depression, anxiety | Phase I | [ClinicalTrials.gov] |
| URB597 | FAAH (fatty acid amide hydrolase) inhibitor | Schering-Plough | Depression | Phase I | [ClinicalTrials.gov] |
| AZD7325 | GABA receptor partial agonist | AstraZeneca | Anxiety | Phase I | [ClinicalTrials.gov] |
| AZD6280 | GABA receptor partial agonist | AstraZeneca | Anxiety | Phase I | [ClinicalTrials.gov] |
| -- | CRF1 antagonist | Neurogen | Depression, anxiety | Pre-clinical | |
| SSR 126374 | CRF1 antagonist | Sanofi-Aventis | Depression, anxiety, hyperphagia | Pre-clinical | |
| SSR 411298 | FAAH (fatty acid amide hydrolase) inhibitor | Sanofi-Aventis | Depression, anxiety, hyperphagia | Pre-clinical | [ClinicalTrials.gov] |
| SSR 241586 | NK2/NK3 antagonist | Sanofi-Aventis | Depression, anxiety, IBS, COPD | Pre-clinical | |
| CRF1 antagonist (backup) | CRF1 antagonist | GSK/Neurocrine | Depression, anxiety | Pre-clinical | |
| R1661 | E-mail shawn@neurotransmitter.net if you can share details about how this drug works. | Roche | Anxiety | Pre-clinical | |
| SAR 102279 | NK2 receptor antagonist | Sanofi-Aventis | Depression, anxiety | Pre-clinical | |
| YKP581 | Undisclosed mechanism of action | SK Pharmaceuticals (J & J) | Depression | Pre-clinical | |
| Lu AA44608 | Neuropeptide Y receptor antagonist | Lundbeck | Depression, anxiety | Discontinued | [ClinicalTrials.gov] |
| GW876008 | CRF1 antagonist | Neurocrine/GSK | Depression, anxiety, IBS | Discontinued | [ClinicalTrials.gov] |
| Casopitant | NK1 antagonist | GSK | Depression, anxiety, emesis | Discontinued | [ClinicalTrials.gov] |
| Elzasonan, CP-448,187 | 5-HT1B and 5-HT1D receptor antagonist | Pfizer | Depression, anxiety | Discontinued | [ClinicalTrials.gov] |
| PRX-00023 | 5-HT1A agonist, sigma receptor antagonist | Epix | Depression | Discontinued | [Compound Profile] [ClinicalTrials.gov] |
Treatments for Sleep Disorders
| Drug Name | Pharmacologic Action | Company | Indication | Developmental Phase | Links |
| Indiplon IR; Indiplon MR | GABA-A modulator (at BZ1 sites) | Neurocrine | Sleep disorders | Approvable, FDA requested more data | [Neurocrine's info] [ClinicalTrials.gov] |
| Silenor® (doxepin) | Doxepin is a potent antagonist at histamine H1 and H2 receptors. It may weakly inhibit the reuptake of norepinephrine and serotonin. Doxepin is also an antagonist at alpha-1-adrenoceptors. The drug binds to both serotonin 5-HT2A and 5-HT2C receptors. In addition, it is an antagonist at all subtypes of muscarinic acetylcholine receptors (references provided elsewhere). |
Somaxon | Sleep disorders | NDA Submitted 1/08 | |
| Eplivanserin, SR 46349 | 5-HT2A receptor antagonist | Sanofi-Aventis | Sleep disorders | Phase III - submission expected in the second half of 2008 | [ClinicalTrials.gov] |
| VEC-162 | Melatonin receptor agonist | Vanda Pharmaceuticals | Sleep disorders, depression | Phase III | [Vanda's info] [ClinicalTrials.gov] |
| ORG 50081 (esmirtazapine) | 5-HT2 antagonist, H1 antagonist, alpha-2-adrenoceptor antagonist | Schering-Plough | Sleep disorders, hot flashes | Phase III | [ClinicalTrials.gov] |
| Volinanserin, M-100907 | 5-HT2A antagonist | Sanofi-Aventis | Sleep disorders | Phase III | |
| Almorexant, ACT-078573 | Orexen OX1 and OX2 receptor antagonist | Actelion | Sleep disorders | Phase III | [Actelion's Web Site] [ClinicalTrials.gov] |
| Adipiplon, NG2-73 | Partial GABA-A receptor agonist that is preferential for alpha3 subunit-containing receptors | Neurogen | Sleep disorders, anxiety | Phase II | |
| APD125 | 5-HT2A inverse agonist | Arena | Sleep disorders | Phase II | [ClinicalTrials.gov] |
| PD-6735 | Melatonin receptor agonist | Phase 2 Discovery | Sleep Disorders | Phase II | [ClinicalTrials.gov] |
| Pimavanserin, ACP-103 | Serotonin 5-HT2A receptor inverse agonist, dopamine D2/D3 receptor partial agonist, acetylcholine M1 receptor agonist | Acadia | Sleep disorders, Parkinson's disease psychosis, schizophrenia co-therapy | Phase II | [June 07 Press Release] [ClinicalTrials.gov] |
| PD-200,390 | Voltage-gated calcium channel alpha(2)delta subunit modulator | Pfizer | Sleep disorders | Phase II | [ClinicalTrials.gov] |
| LY2624803, HY10275 | 5-HT2A and histamine H1 receptor antagonist | Depression, ADHD | Phase II | [ClinicalTrials.gov] | |
| TIK-301, LY156735 | Melatonin agonist, 5-HT2B/5-HT2C antagonist | Tikvah Pharmaceuticals | Sleep disorders | Phase II | [ClinicalTrials.gov] |
| AVE 8488 | 5-HT2A antagonist | Sanofi-Aventis | Sleep disorders | Pre-clinical |
Treatments for Psychosis/Bipolar Disorder
| Drug Name | Pharmacologic Action | Company | Indication | Developmental Phase | Links |
| Zomaril (iloperidone) | Selective DA/NE/5-HT antagonist | Vanda Pharmaceuticals | Psychosis | NDA Submitted | [ClinicalTrials.gov] |
| Asenapine (ORG 5222) | 5-HT2 antagonist, D2 partial agonist | Schering-Plough | Psychosis | NDA Submitted | [ClinicalTrials.gov] |
| Corlux ® (AKA mifepristone or RU-486) | Glucocorticoid receptor type II (GRII) antagonist, progesterone receptor antagonist | Corcept | Psychosis, depression | Phase III | [Corcept's info] [ClinicalTrials.gov] |
| Pardoprunox, SLV 308 | D2 partial agonist, 5-HT1A agonist | Solvay | Psychosis, Parkinson's disease | Phase III | [ClinicalTrials.gov] |
| LIC477D (licarbazepine) | Voltage-gated sodium channel inhibitor | Novartis | Psychosis | Phase III | [ClinicalTrials.gov] |
| Pimavanserin, ACP-103 | Serotonin 5-HT2A receptor inverse agonist, dopamine D2/D3 receptor partial agonist, acetylcholine M1 receptor agonist | Acadia | Antipsychotic-induced side effects, Parkinson's disease psychosis | Phase III | [June 07 Press Release] [ClinicalTrials.gov] |
| Ocaperidone | D2/5-HT2 antagonist | Neuro3d, Janssen | Psychosis | Phase II |