mefluleucine

Mefluleucine is an orally bioavailable small-molecule analogue of leucine that selectively binds to and modulates the leucine sensor protein sestrin2, resulting in direct activation of the mammalian target of rapamycin complex 1 (mTORC1) signaling pathway in the brain.[1][4][13][16] By engaging sestrin2, mefluleucine increases mTORC1 signaling within a physiological range, promotes synaptogenesis in the medial prefrontal cortex, and produces rapid and sustained antidepressant-like effects in preclinical models, mechanistically overlapping with the mTORC1-dependent component of ketamine’s activity.[1][4][12][13] The drug has been developed by Navitor Pharmaceuticals and subsequently by Supernus Pharmaceuticals (as SPN-820) and is in clinical development as an oral treatment for adults with major depressive disorder, particularly treatment-resistant depression.[1][4][10][18]

Other names

mefluleucine hydrochloride