Table 1. Glutamate mates. Compounds in development for autism spectrum disorders (ASD), schizophrenia and depression.

Target

Company

Product

Development stage

Indication

Glutamatergic targets

 

 

 

 

Glycine transporter type 1 (GlyT1; SLC6A9)

Roche (SIX:ROG; OTCQX:RHHBY)

Bitopertin (R1678)

Phase III

Schizophrenia

NMDAR NR2B subtype (GRIN2B; NR2B)

AstraZeneca plc (LSE:AZN; NYSE:AZN)

AZD6765

Phase II

Depression

GRIN2B (NR2B)

Addex Therapeutics Ltd. (SIX:ADXN); Johnson & Johnson (NYSE:JNJ)

ADX71149

Phase II

Depression; schizophrenia

NMDAR

Johnson & Johnson

Esketamine

Phase II

Depression

NMDAR

Naurex Inc.

GLYX-13

Phase II

Depression

Metabotropic glutamate receptor subtype 5 (mGluR5; GRM5)

Roche

RG7090

Phase II

Depression

GRIN2B (NR2B)

Cerecor Inc.

CERC-301

Phase I

Depression

NMDAR

Naurex

NRX-1074

Phase I

Depression

mGluR2 (GRM2)

BrainCells Inc.

BCI-838

Phase I

Depression

AMPA glutamate receptor (GRIA; GLUR)

Pfizer Inc. (NYSE:PFE)

PF-04958242

Phase I

Schizophrenia

mGluR5

Seaside Therapeutics Inc.

STX110

Preclinical

ASD

mGluR4 (GRM4)

Domain Therapeutics S.A.

DT1687

Preclinical

Schizophrenia

 mGluR2

Addex Therapeutics

mGluR2 negative allosteric modulator (NAM)

Preclinical

Depression

mGluR7 (GRM7)

Addex Therapeutics

mGluR7 NAM

Discovery

Depression

mGluR5

Heptares Therapeutics Ltd.

mGluR5 modulator

Discovery

ASD; depression

Other receptor targets

 

 

 

 

s-1 Receptor

M's Science Corp.

SA4503

Phase II

Depression

Nicotinic acetylcholine receptor α7 (CHRNA7)

Targacept Inc. (NASDAQ:TRGT)

TC-5619

Phase II

Schizophrenia

CHRNA7

AbbVie Inc. (NYSE:ABBV)

ABT-126

Phase II

Schizophrenia

k-Opioid receptor (OPRK1; KOR); OPRM1 (MOR)

Alkermes plc (NASDAQ:ALKS)

ALKS 5461

Phase II

Depression

Corticotropin-releasing factor receptor 1

Neurocrine Biosciences Inc. (NASDAQ:NBIX)

561679

Phase II

Depression

Vasopressin 1a (V1a) receptor

Roche

RGS7314

Phase II

ASD

CHRNA7

Aniona ApS

NSD-761

Preclinical

Schizophrenia

Muscarinic acetylcholine receptor M1 (CHRM1; HM1)

Heptares Therapeutics

HM1 agonist

Preclinical

Schizophrenia

Nonreceptor targets

 

 

 

 

Enzyme replacement therapy

Curemark LLC

CM-AT

Phase III

ASD

Helminth-based treatment

Coronado Biosciences Inc. (NASDAQ:CNDO)

CNDO-201

Phase II

ASD

Phosphodiesterase-10 (PDE-10)

Omeros Corp. (NASDAQ:OMER)

OMS824

Phase II

Schizophrenia

PDE-10A

Takeda Pharmaceutical Co. Ltd. (Tokyo:4502)

TAK-063

Phase I

Schizophrenia

PDE-10A

Roche

RG7203

Phase I

Schizophrenia

PDE-10

EnVivo Pharmaceuticals Inc.

EVP-6308

Phase I

Schizophrenia

PDE-1

Intra-Cellular Therapies Inc.

IC200214 (ITI-002)

Preclinical

Schizophrenia