NV-5138 – (2095886-80-7)

NV-5138, also known as SPN-820, is an investigational new drug being developed by Navitor Pharmaceuticals and Supernus Pharmaceuticals for the treatment of major depressive disorder (MDD). It functions by binding to and modulating sestrin2, a cellular sensor protein for the amino acid leucine, which naturally activates the mammalian target of rapamycin complex 1 (mTORC1) signaling pathway. This pathway is crucial as it is the same one activated by the NMDA receptor antagonist ketamine in the medial prefrontal cortex (mPFC) to produce its rapid-acting antidepressant effects.

NV-5138 has been shown to increase mTORC1 signaling within a physiological range, stimulate synaptogenesis in the mPFC, and induce rapid antidepressant effects in multiple animal models of depression. These effects are long-lasting, persisting for up to 7 days after a single dose, and are similar to those observed with ketamine. The antidepressant actions of NV-5138 require the signaling of brain-derived neurotrophic factor (BDNF), similar to ketamine.

The drug has undergone several clinical trials, starting with a Phase 1 trial in 2018 to evaluate its safety, tolerability, and pharmacokinetics in healthy volunteers and patients with treatment-resistant depression (TRD). Following the initial study, larger Phase 2 trials were initiated to further investigate the efficacy and safety of NV-5138 as an adjunctive treatment for adults with TRD.

The above information is displayed for information purpose only, and has not been reviewed by EON nor does EON attests or validates the accuracy nor does it constitutes a recommendation or validation.

Sources:

https://en.wikipedia.org/wiki/NV-5138
https://pubchem.ncbi.nlm.nih.gov/compound/129050791
https://www.medchemexpress.com/nv-5138.html
https://www.medkoo.com/products/46010
https://www.nature.com/articles/s41598-019-40693-5
https://pmc.ncbi.nlm.nih.gov/articles/PMC6546442/