Brexanolone is an allosteric modulator
of GABAA receptors and "a new molecular entity not currently marketed anywhere in the world for any indication," according to the FDA document.
Another imminent innovative antidepressant mechanism of action is represented by brexanolone, an allosteric modulator
of GABA-A receptors (which are known to become dormant during pregnancy and are not reactivated after delivery in women who develop postpartum depression).
In vitro, activation of the CaSR with [Ca.sup.2+] or positive allosteric modulator
increased PTHrP secretion by BrCa cells [26, 33].
Ganaxolone, a positive allosteric modulator
of GABAA, is being developed in three different dose forms (intravenous, capsule, and liquid) intended to maximise therapeutic reach to adult and pediatric patient populations in both acute and chronic care settings.
Brexanolone (SAGE-547) is an allosteric modulator
of both synaptic and extrasynaptic GABAA receptors.
SAGE-718 is a novel, oral, first-in-class, oxysterol-based positive allosteric modulator
of N-methyl-D-aspartate receptors.
According to Addex, ADX71943 is a potent and selective positive allosteric modulator
of gamma-aminobutyric acid subtype B (GABA-B) receptors.
ADX71943 is an orally available positive allosteric modulator
(PAM) of the GABA(B) receptor that has potential for treatment of osteoarthritis pain and chronic nociceptive pain as well as other indications.
The company said that its allosteric modulator
platform enabled this breakthrough discovery, advancing the understanding of GLP-1 mediated gpcr signalling.
BNC210 is a small molecule, orally-administered, highly-selective negative allosteric modulator
of the alpha-7 nicotinic acetylcholine receptor which is being developed for anxiety and stressor-related disorders.
According to the company, SAGE-547 is an allosteric modulator
of GABAA receptors in development for the treatment of adult patients with refractory status epilepticus who have not responded to standard regimens (super-refractory status epilepticus, or SRSE).
Proceeds will be used by the company to advance its two proprietary platform technologies, a core protein allosteric modulator
, or CpAM, programme aimed at developing novel oral agents for chronic hepatitis B infection (HBV) and an orally-delivered microbiome therapeutics technology for clostridium difficile infection (CDAD).