- |||||||||| allopregnanolone (LYT-300) / PureTech
Trial completion, Phase classification, Enrollment change, Trial completion date, Trial primary completion date: LYT-300 in Healthy Volunteers (clinicaltrials.gov) - Nov 13, 2023
P1/2, N=186, Completed,
LYT-300 has PD and PK properties that warrant further clinical development. Recruiting --> Completed | Phase classification: P1 --> P1/2 | N=90 --> 186 | Trial completion date: Apr 2023 --> Oct 2023 | Trial primary completion date: Dec 2022 --> Oct 2023
- |||||||||| Review, Journal: GABAkines - Advances in the discovery, development, and commercialization of positive allosteric modulators of GABA receptors. (Pubmed Central) - May 19, 2022
Traditional GABAkines like diazepam have safety and tolerability concerns that include sedation, motor-impairment, respiratory depression, tolerance and dependence...The compounds that are presently being developed and commercialized include several neuroactive steroids (an allopregnanolone formulation (brexanolone), an allopregnanolone prodrug (LYT-300), Sage-324, zuranolone, and ganaxolone), the α2/3-preferring GABAkine, KRM-II-81, and the α2/3/5-preferring GABAkine PF-06372865 (darigabat)...Medicinal chemistry efforts are also ongoing to identify novel and improved GABAkines. The data document gaps in our understanding of the molecular pharmacology of GABAkines that drive differential pharmacological profiles, but emphasize advancements in the ability to successfully utilize GABA receptor potentiation for therapeutic gain in neurology and psychiatry.
- |||||||||| KRM-81 / RespireRx, Ztalmy (ganaxolone oral) / Marinus
Review, Journal: The imidazodiazepine, KRM-II-81: An example of a newly emerging generation of GABAkines for neurological and psychiatric disorders. (Pubmed Central) - Mar 9, 2022
These GABAkines and non-steroid compounds (GRX-917, a TSPO binding site ligand), darigabat (CVL-865), an α2/3/5-preferring GABAkine, SAN711, an α3-preferring GABAkine, and the α2/3-preferring GABAkine, KRM-II-81, bring new therapeutic promise to this highly utilized medicinal target in neurology and psychiatry...KRM-II-81 also produces anxiolytic- and antidepressant-like effects in rodent models. Other key features of the pharmacology of this compound are its low sedation rate, lack of tolerance development, and the ability to prevent the development of seizure sensitization.
- |||||||||| allopregnanolone (LYT-300) / PureTech
Enrollment open: LYT-300 in Healthy Volunteers (clinicaltrials.gov) - Jan 3, 2022
P1, N=90, Recruiting,
Other key features of the pharmacology of this compound are its low sedation rate, lack of tolerance development, and the ability to prevent the development of seizure sensitization. Not yet recruiting --> Recruiting
- |||||||||| allopregnanolone (LYT-300) / PureTech
LYT-300: An Orally Bioavailable Prodrug of Allopregnanolone With Anticonvulsant Activity ([VIRTUAL]) - Nov 28, 2021 - Abstract #ACNP2021ACNP_1304;
In mice, oral administration of LYT-300 produced dose-dependent increases in plasma exposure of ALLO and evidence of anticonvulsant efficacy. These data provide proof of concept that LYT-300 (p.o.) can deliver the pharmacologically active compound ALLO at levels that produce ALLO-related pharmacological effects.
- |||||||||| allopregnanolone (LYT-300) / PureTech
LYT-300: An Orally Bioavailable Prodrug of Allopregnanolone With Anticonvulsant Activity (Exhibit Hall C) - Nov 28, 2021 - Abstract #ACNP2021ACNP_436;
In mice, oral administration of LYT-300 produced dose-dependent increases in plasma exposure of ALLO and evidence of anticonvulsant efficacy. These data provide proof of concept that LYT-300 (p.o.) can deliver the pharmacologically active compound ALLO at levels that produce ALLO-related pharmacological effects.
- |||||||||| allopregnanolone (LYT-300) / PureTech
New P1 trial: LYT-300 in Healthy Volunteers (clinicaltrials.gov) - Nov 21, 2021
P1, N=90, Not yet recruiting,
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