Inventory of new small molecule antidepressant drugs in research worldwide

Apimostinel

BTRX-246040

CERC-301

CERC-501

Liafensine

JNJ-39393406

 

Apimostinel

Mechanism: NMDA receptor partial agonist
Status: Phase II (IV) and Phase I (oral) clinical trials
Developer: Allergan
Also known as NRX-1074, is a drug originally developed by Naurex to treat depression-but is currently being jointly researched by Naurex and Allergan (acquired Naurex). The drug has a selective partial agonist function for NMDA receptors, especially in the allosteric site of the glycine binding site. Although Apimostinel shows a similar mechanism of action to GLYX-13 (another drug being developed by Naurex), it differs from GLYX-13 in that its weight is more significant.
A comparative analysis showed that Apimosinel is thousands of times more potent than GLYX-13 by weight. Earlier I discussed the potential benefits of using NRX-1074 to treat depression, and mentioned that it is fast onset, has no psychotropic effects and seems to be well tolerated. Preliminary evidence suggests that after taking Apimostinel, depressive symptoms may disappear within 24 hours.
In addition, the mood enhancing effect of Apimosinel seems to be dose-dependent, so the antidepressant effect of higher doses is more pronounced. It is worth mentioning that in the early trials, a single dose of Apimostinel provided a higher rate of relief from symptoms of depression than SSRIs lasting for several weeks.

BTRX-246040

CAS  : 1307245-86-8

Mechanism: NOC receptor antagonist
Status: Phase II
Developer: BlackThorn Therapeutics
The drug was originally studied by Eli Lilly, but now it seems to be associated with blackthorn therapy and has a new chemical
Academic name. A proof-of-concept study published in 2016 stated that LY-2940094 (40 mg) is safe, well tolerated, and effective for treating depression in humans-lasting more than 8 weeks.
Its initial efficacy as an antidepressant is demonstrated by a significant change in the total score of 17 total scores from baseline to 8 weeks on the GRID-Hamilton Depression Rating scale. In addition, the study also found that LY-2940094 changed the processing of emotional stimuli within the first week of treatment-in the emotional test series, the cognitive enhancement of positive facial expressions relative to negative facial expressions is evidence. The preliminary survey data of LY-2940094 is the first data showing the potential of NOP receptor antagonists to treat depression.
There is still some controversy as to whether BTRX-246040 will continue to be used to treat major depression, or whether it will be investigated as a treatment for other neurological diseases. However, compared with most antidepressant drugs, BTRX-246040 shows a unique mechanism of action. Antagonizing NOC receptors seems to increase monoamine concentrations in several areas of the brain, enhance neurogenesis, and regulate the activation of the hypothalamic-pituitary-adrenal axis.