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Re: DTGoody post# 1125

Wednesday, 02/14/2024 6:19:30 PM

Wednesday, February 14, 2024 6:19:30 PM

Post# of 1178
RSPI is going to be a Gold Mine:

Here is some research tracking:
CERECOR in September 2016 acquired right to Anti Epilepsy Drug LY3130481 from Eli Lilly Cerecor branded drug CERC-611
Cerecor and Aevi Genomic Medicine Merged Feb 2020
Cerecor rebranded into Avalo Therapeutics ticker AVTX $5.06
Avalo Therapeutics (formerly Cerecor) is developing AVTX 611 (formerly CERC 611)
November 2022 Avalo Therapeutics enters into an agreement with ES Therapeutics to sell its net economic rights to future payments of previously out-licensed assets including CERC 611
AVTX 611 got rebranded to ES 481 is being developed by ES Therapeutics for the treatment of Epilepsy.
Clinical development is underway in Australia and Canada.
Study Design
Total Participants: 24
Study Start date:
November 21, 2021
Estimated Completion Date:
December 31, 2023

This webpage mentions:
The value of human epileptic tissue in the characterization and development of novel antiepileptic drugs: The example of CERC-611 and KRM-II-81
https://www.sciencedirect.com/science/article/abs/pii/S000689931930410X




The value of human epileptic tissue in the characterization and development of novel antiepileptic drugs: The example of CERC-611 and KRM-II-81
Abstract
The need for improved antiepileptics is clearly mandated despite the existence of multiple existing medicines from different chemical and mechanistic classes. Standard of care agents do not fully control epilepsies and have a variety of side-effect and safety issues. Patients typically take multiple antiepileptic drugs and yet many continue to have seizures. Antiepileptic-unresponsive seizures are life-disrupting and life-threatening. One approach to seizure control is surgical resection of affected brain tissue and associated neural circuits. Although non-human brain studies can provide insight into novel antiepileptic mechanisms, human epileptic brain is the bottom-line biological substrate. Human epileptic brain can provide definitive information on the presence or absence of the putative protein targets of interest in the patient population, the potential changes in these proteins in the epileptic state, and the engagement of novel molecules and their functional impact in target tissue. In this review, we discuss data on two novel potential antiepileptic drugs. CERC-611 (LY3130481) is an AMPA receptor antagonist that selectively blocks AMPA receptors associated with the auxiliary protein TARP ?-8 and is in clinical development. KRM-II-81 is a positive allosteric modulator of GABAA receptors selectively associated with protein subunits a2 and a 3. Preclinical data on these compounds argue that patient-based biological data increase the probability that a newly discovered molecule will translate its antiepileptic potential to patients.

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