THE 5-HT6 RECEPTOR ANTAGONIST PLATFORM
The best selective and multi-target serotonin 5-HT6 receptor antagonists for the treatment of CNS diseases such as cognitive dysfunction, neurodegenerative and anxiety disorders, which affect millions of people worldwide.
A SELECTIVE 5-HT6 RECEPTOR ANTAGONIST PLATFORM
AVISETRON (AVN-211) is a highly selective 5-HT6 receptor antagonist (IC50 = 6 nM, Kib=2.1 nM). It has a lesser affinity towards 5-HT2B, receptors (IC50 = 249 nM) and practically no affinity to a multitude of other therapeutic targets.
AVISETRON is in Phase II/III Clinical trials for the treatment of Schizophrenia.
AVN-322 is a highly selective 5-HT6 receptor antagonist with a high binding affinity (Ki=389 pM) and high potency to functionally block the receptor (Ki = 2.85±0.46 nM). The AVN-322 has a much lesser affinity towards 5HT-2B receptors (IC50~1 µM in radioligand competitive binding assay and 6.2 µM in a cell-based functional assay). The AVN-322 does not interact at 1 µM with other therapeutic targets (a panel of 70 receptors and enzymes}.
AVN-322 is ready to entering Phase II clinical trials for treating diseases associated with cognitive dysfunction.
Backup compounds AVN-492, AVN- 3205 are in preclinical development.
AVISETRON, AVN-322, AVN-492, and AVN- 3205 possess excellent DMPK/tox and behavioral profiles.
A MULTI-TARGET PLATFORM
AVN-101 is safe and orally bioavailable multi-target drug candidate with potential for treatment of the CNS diseases associated with memory loss, cognitive dysfunction, neurodegeneration, depression, and general anxiety.
AVN-101 is a substance with a very high affinity to the 5-HT7 receptor (Ki=153 pM). It has a lesser affinity towards 5-HT6, 5-HT2A, and 5HT2C receptors (Ki range between 1.2 and 2.0 nM) and it also exhibits relatively high affinity towards histamine H1 (Ki = 580 pM), adrenergic ?2A, ?2B, and ?2C receptors (Ki range between 410 and 3,600 pM).
AVN-101 possess excellent DMPK/tox and behavioral profiles.
AVN-101 is now in clinical development for the treatment of disorders associated with the general anxiety and cognitive dysfunctions.
