Schizophrenia Research Forum: Drugs in Trials
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Drugs in Trials:Dopamine
Drug Development status Clinical Trial ID Company or Institution Mechanism Notes
A437203 Preclinical   Abbott D3 antagonist  
ABT925 POC Failed NCT00412620 Abbott D3-R antagonist Insufficient target engagement
AF11167 Phase 1   Lundbeck PDE inhibitor Also aimed at AD and HD
AMG579 Phase 2   Reviva PDE10 inhibitor  
Asenapine (Org5222) FDA Approved NCT00156104 Merck-Schering 5HT2-D2 antagonist  
AT-9242 Phase 1   ARYx Engineered antipsychotic clozapine-analog Origin Schwartz
AZ-004 (ALXZ-004) Phase 3   Alexza Pharmaceuticals Inhaled loxapine  
Bifeprunox Discontinued NCT00366327 Solvay 5HT2A & D2 partial agonist Development halted
BL-1020 Phase 3 Failed   Bio-LineRx DA antagonist with GABA modulation  
Blonanserine (AD5423) Phase 3   Dainippon DA-5HT2 antagonist  
Cariprazine (RGH188) Phase 3   Richter Pharma AG D2/D3 modulator Complete Response Letter by FDA
CLR151 Inactive   Clera Inc. Fast off D2R antagonist  
DAAOI-1 POC Ongoing NCT01390376 China Medical University Hospital Regulates D-serine levels Treatment-resistant schizophrenia patients stand-alone
DAR0100-Dihyrexidine (N-(N-Propyl)-Dihydrexidine) Phase 2   Purdue Pharma Partial D1 agonist; restores frontal dopaminergic deficit Add-on for negative symptoms, improves cognition
DAR-100 POC Failed     Full D1R agonist Matrics scale did not show improvement when added to D1R-sparing antipsychotics; 15 mg <1% target engagement
DAR201 Inactive   DAR Pharma D1 agonist No development reported
Dinapsolin Inactive   BioValve D1 agonist  
EGIS-11150 Preclinical   Egis Pharma D2R antagonist with effect on adrenergic and serotonergic receptors  
Eltoprazine POC Ongoing NCT01266174 Psychogenics 5-HT modulator Cognitive impairment augmentation therapy
Entacapone Inactive NCT00192855 Ramban Health Center COMT inhibitor Add-on for cognitive disorders
F15063 Discontinued   Fabre D2-D3 antagonist, D4 5HT1A agonist  
F17464 Phase 2 NCT02151656 Pierre Fabre Selective D3 antagonist/5-HT1A partial agonist Imaging study in healthy volunteers
F17807 Preclinical   Pierre Fabre D3/D2/alpha2C antagonist Treatment-resistant schizophrenia, CIAS
GSK773812 (G773812, SB-773812) Inactive NCT00259870 GlaxoSmithKline D2 5HT2 antagonist  
Iloperidone FDA Approved NCT00254202 Vanda DA-5HT2 antagonist Originally developed by Novartis
ITI-007 POC Successful NCT01499563 Intra-Cellular Therapeutics D2, 5HT2A antagonist, SERT block + dopamine phosphoprotein modulator inlicensed from BMS; successful Phase 2 trial compared to Risperdal, shows target engagement at 10 mg using PET
JNJ37822681 Inactive   Janssen Fast off D2R antagonist  
L-Dopa POC Ongoing NCT01636037 Center for Addiction & Mental Health Dopamine stabilization Augmentation therapy for negative/cognitive symptoms
Loxapine FDA Approved   Alexza Pharmaceuticals DA-5HT2A antagonist Addresses agitation, uses inhalation technology
Lu 31-130 Phase 2   Lundbeck DA-5HT2 antagonist  
Lurasidone (SM13496) FDA Approved   Dainippon D2 antagonist 5HT2A antagonist  
Modafinil POC Failed NCT00057707, NCT00573417 National Institute of Mental Health (NIMH) DA outflow enhancer Add-on trial failed
MP-10 Phase 2 NC1939548 Pfizer PDE10 inhibitor Augmentation therapy
NPD-001 Preclinical   Omeros Phosphodiesterase 10 inhibitor  
Ocaperidone Discontinued   Neuro3D D2 5HT2 antagonist Inlicensed from Janssen; development halted
OMS643762 POC Ongoing NCT01952132 Omeros PDE-10 inhibitor Cognition both stand-alone and as augmentation therapy
OPC-34712 (Brexpiprazole) Phase 2 NCT01451164 Otsuka Pharmaceutical Co., Ltd. Partial D2 agonist Dose-finding study
Paliperidone palmitate (9-hydroxyrisperidone) FDA Approved NCT00210548 Janssen DA-5HT2 antagonist (serotonin-dopamine antagonist, or SDA)  
PF-2545920 POC Failed NCT00463372 Pfizer PDE10 Collaboration with Biotie-elbion
PGX200097 Discontinued   Psychiatry Genomics D2R antagonist COMT inh  
Pimozide POC Failed NCT00158223 National Institute of Mental Health (NIMH) Antipsychotic No effect
PNU177864 Inactive   Pfizer D3 antagonist Severe skeletal myopathy in rodents
Pramipexol Inactive   St. Vincentís Hospital Westchester, Hanover, NJ D3 agonist Add-on to risperidone
Preclamol ((-)-3-(3-hydroxyphenyl)-N-n-propylpiperidine [(-)-3PPP) Inactive   University of Maryland D2 agonist; Partial D1 R agonist Cognitive enhancement
Pyrimidine-Ones Discontinued   Ferrer DA-5HT2 antagonist  
QF2004B Discontinued   Santiago de Compostela 5HT2A D2 antagonist  
RP5063 Phase 2 NCT01490086 Reviva DA-5HT stabilizer Substantial effect of 23 points on PANSS Total vs. 15 for aripiprazole
SB269235 Inactive   GlaxoSmithKline D3 antagonist  
SB-773812 Discontinued NCT00259870 GlaxoSmithKline D2, 5HT2A, 5HT6, D3 antagonist Target engagement data
SLV-314 Inactive   Solvay D2 antagonist SSRI  
SLV319 Inactive   Solvay D2 antagonist 5HT1A agonist CB1-R antagonist Also in development for obesity
ST2329 Discontinued   Sigma-Tau 5Ht2A-D3 antagonist  
Stepholidine POC Ongoing   University of Toronto D2 antagonist-D1 agonist Derived from Chinese herbs
Tolcapone Inactive NCT00044083 National Institute of Mental Health (NIMH) COMT inhibitor Add-on for cognitive disorders
Unknown: BMS Discovery     PDE10; Modulates dopamine dynamics on direct vs indirect pathway specifically in striatum  
Unknown: Janssen Phase 1   Janssen PDE10 inhibitor Collaboration with Biotie-Elbion
Unknown: Lundbeck Discovery   Lundbeck PDE10; Modulates dopamine dynamics on direct vs indirect pathway specifically in striatum  
Unknown: Roche Discovery   Roche PDE10; Modulates dopamine dynamics on direct vs indirect pathway specifically in striatum  
YKP1358 Phase 2   SK Bio-Pharmaceuticals D2, D3 5HT-2A antagonist, no action at adrenerge receptors PET imaging data available