bigtalan
1 day ago
AI Overview
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The results of the RespireRx Pharmaceuticals (RSPI) $1.8 million Department of Defense (DoD) grant for Phase 2A and 2B clinical trials testing CX1739 in spinal cord injured patients have not yet concluded. The trials are ongoing and the results are expected to be published in the future.
Here's a more detailed explanation:
The Grant:
RSPI received a $1.8 million DoD grant to fund a two-stage Phase 2A and 2B clinical study. The study is evaluating the safety and efficacy of CX1739, RespireRx's lead AMPAkine, in improving bladder function and motor activity in individuals with spinal cord injury (SCI).
Phase 2A and 2B:
The trial is divided into two phases. Phase 2A is a safety and efficacy study, and Phase 2B is a double-blind, placebo-controlled study.
Timeline:
The trial is ongoing and the results are expected to be published in the future.
Purpose:
The purpose of the study is to determine whether CX1739 can safely and effectively improve bladder function and motor activity in individuals with SCI.
Research Partner:
The study is being conducted by Shirley Ryan AbilityLab, a research and clinical center focused on rehabilitation.
LTListener
1 day ago
Good to hear. It will be interesting as to how they structure the assets and funding moving forward, exiting EM and which avenues they take immediately.
Tier 3/IND enabling for pain for almost 18 months now. What is the status/timeline of submitting IND and getting KRM-ll-81 into phase 1 trials.
And related, did they get the SBIR award for epilepsy IND enabling?
Then the amapkine platform has the phase 2 DOD funding sitting out there for a year now, waiting on what? And related, how will they approach ADHD and is that the source of the expected additional grant applications?
I guess also related to the ampakine platform. All the publication efforts are leading to what end? Are they looking to sell that platform like they had in the past? Or are they looking to add additional medical indications to pursue with CX-1739, like various cognitive disorders?
OSA program still viable?
The company internally valued themselves around 50 million according to one slide, but reality is any significant deal for the gabakine for phase 1 clinicals or additional grant funding will be multiples additive. Watching and waiting. Good luck to all.
bigtalan
2 days ago
AI Overview
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Yes, there are published papers on Ampalex-d10. Ampalex-d10, also known as CX-516-d10, is a deuterated version of the compound CX-516, which is a positive allosteric modulator of the AMPA receptor. It is used in research to study the pharmacology and effects of AMPA receptors and the compound's potential for therapeutic applications.
Here's a more detailed breakdown:
CX-516:
This is a compound that enhances the activity of AMPA receptors, which are essential for learning and memory.
Deuterated versions:
Deuteration (replacing hydrogen atoms with deuterium) is a common technique in research to study the metabolism and pharmacokinetic properties of drugs. Ampalex-d10 allows researchers to track the compound's fate in the body more accurately.
Ampalex-d10:
The deuterated version of CX-516, it is used to study the effects of AMPA receptor modulation on various processes, such as memory, learning, and cognitive function.
Published papers:
Several studies have been published on CX-516, including its effects on:
Memory enhancement in rats.
Cognitive deficits in schizophrenia.
Potential treatment for Alzheimer's disease and mild cognitive impairment (MCI).
Clinical trials:
Some clinical trials have investigated CX-516, including a placebo-controlled add-on trial in schizophrenia, according to the National Institutes of Health (NIH) (.gov).
BenchChem:
BenchChem offers Ampalex-d10 for research use, indicating its availability and continued use in scientific research.
In summary, Ampalex-d10 is a well-studied compound, and numerous papers have been published exploring its effects and potential applications, according to Selleckchem.com and other scientific resources.
bigtalan
2 days ago
AI Overview
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Yes, there are published research papers on Ampalex-d10, also known as deuterated Ampalex or deuterated CX516.
What is Ampalex-d10?
Ampalex-d10 is a deuterated analog of Ampalex (CX516), a positive allosteric modulator (PAM) of the AMPA receptor.
Deuteration involves replacing hydrogen atoms with deuterium, which can alter the metabolic stability and pharmacokinetic properties of a compound.
AMPA receptors are crucial for synaptic transmission and plasticity, and enhancing their activity is a potential therapeutic strategy for cognitive deficits.
Areas of Research:
Research papers on Ampalex-d10 and related compounds explore the following areas:
AMPA Receptor Modulation:
Studies investigate how Ampalex-d10 enhances the response of AMPA receptors to glutamate, leading to increased synaptic transmission.
Researchers examine the effects of AMPA receptor potentiation on synaptic plasticity and cognitive function.
Cognitive Enhancement:
Research explores the potential of Ampalex-d10 to improve cognitive function in animal models of various neurological disorders.
Studies assess its effects on memory, learning, and other cognitive processes.
Neuroprotection:
Some research indicates that Ampalex-d10 may possess neuroprotective properties, potentially protecting neurons from damage or stress.
Studies investigate its role in reducing neuronal apoptosis and promoting neuronal survival.
Therapeutic Potential:
Ampalex-d10 has been investigated for its potential therapeutic applications in conditions like Alzheimer's disease, schizophrenia, and attention deficit hyperactivity disorder (ADHD).
Research focuses on its ability to alleviate symptoms and improve cognitive deficits associated with these disorders.
Note:
It's important to remember that much of the research on Ampalex-d10 is preclinical (conducted in vitro or in animal models). More clinical trials are needed to determine its efficacy and safety in humans.
meixatech
2 days ago
Deuterium in drug discovery: progress, opportunities and challenges
Rita Maria Concetta Di Martino, Brad D. Maxwell & Tracey Pirali
Nature Reviews Drug Discovery volume 22, pages562–584 (2023)
Abstract
Substitution of a hydrogen atom with its heavy isotope deuterium entails the addition of one neutron to a molecule. Despite being a subtle change, this structural modification, known as deuteration, may improve the pharmacokinetic and/or toxicity profile of drugs, potentially translating into improvements in efficacy and safety compared with the non-deuterated counterparts. Initially, efforts to exploit this potential primarily led to the development of deuterated analogues of marketed drugs through a ‘deuterium switch’ approach, such as deutetrabenazine, which became the first deuterated drug to receive FDA approval in 2017. In the past few years, the focus has shifted to applying deuteration in novel drug discovery, and the FDA approved the pioneering de novo deuterated drug deucravacitinib in 2022. In this Review, we highlight key milestones in the field of deuteration in drug discovery and development, emphasizing recent and instructive medicinal chemistry programmes and discussing the opportunities and hurdles for drug developers, as well as the questions that remain to be addressed.
meixatech
2 days ago
From AI:
Deuterium, a stable isotope of hydrogen, is increasingly used in medicine to improve drug properties, particularly pharmacokinetics and toxicity profiles. Deuterated drugs are created by replacing hydrogen atoms with deuterium in a drug molecule, potentially slowing metabolism, increasing half-life, and reducing the production of toxic metabolites. This approach can lead to improved efficacy, safety, and tolerability.
Elaboration:
Deuterated Drugs:
These are medications where hydrogen atoms in the drug molecule are replaced with deuterium.
Benefits of Deuteration:
Improved Pharmacokinetics: Deuteration can slow down drug metabolism, leading to longer half-lives and potentially reducing the need for frequent dosing.
Reduced Toxicity: By altering metabolic pathways, deuteration can decrease the formation of toxic metabolites.
Enhanced Selectivity: It can help reduce the formation of non-selective metabolites, improving the drug's target selectivity.
Increased Bioavailability: In some cases, deuteration can enhance the oral absorption of drugs.
Examples:
Deutetrabenazine (Austedo): The first FDA-approved deuterated drug, used for Huntington's disease.
Deucravacitinib: Approved for treating autoimmune diseases like Sjögren's syndrome, rheumatoid arthritis, and psoriasis.
Mechanism:
The kinetic isotope effect (deuterium has a slightly larger mass than hydrogen) can influence the rate of reactions, including those involving metabolic enzymes.
Application:
Deuterium is used in various stages of drug discovery and development, including:
Designing new lead compounds.
Improving the properties of existing drugs.
Understanding drug metabolism.
Challenges:
While promising, the use of deuterium in drug development also faces challenges, including the need for further research and understanding of the impact of deuteration on various drug properties.
bigtalan
2 days ago
AI Overview
Yes, RSPI (RespireRx Pharmaceuticals Inc.) and Ampalex-d10 are related, as Ampalex-d10 is a deuterated analog of Ampalex, a compound that was initially developed by Cortex Pharmaceuticals, a company that later became RespireRx Pharmaceuticals.
Here's a breakdown of the connection:
1. RespireRx Pharmaceuticals (RSPI):
RSPI is a biopharmaceutical company focused on developing therapies for neurological and respiratory disorders.
They have a drug platform called EndeavourRx, which includes the AMPAkines program.
2. Ampakines and Ampalex:
Ampakines are a class of drugs that act as positive allosteric modulators (PAMs) of AMPA receptors.
Ampalex (CX-516) was the first ampakine developed by Cortex Pharmaceuticals (now RespireRx).
3. Ampalex-d10:
Ampalex-d10 is a deuterated version of Ampalex.
Deuteration involves replacing hydrogen atoms with deuterium, which can enhance metabolic stability and allow for better tracking in pharmacokinetic studies.
In Summary:
Ampalex-d10 is a research tool derived from Ampalex, which was originally developed by the company that eventually became RespireRx Pharmaceuticals. Therefore, RSPI and Ampalex-d10 are connected through their shared history and the ongoing development of AMPAkine-based therapies.
LTListener
3 days ago
Yes. Respire has multiple avenues for potential success and significant valuation reset compared with this peanuts valuation it has be stricken with since the inception of going quiet on the EM and really well before that as well. As some have stated though, it gave some of us the opportunity to acquire dirt cheap postions a year or two ago...
Obviously, with KRM-ll-81 advancing towards clinical trials along two potential lucrative pathways... Pain and Epilepsy, this is the bell cow and positioned to see one of those amazing pharma stock runs as it emerges into funding/partnerships/clinical trials...
Not to discount the potential in the ampakine CX-1739. My interpretation of their commentary is they would love to see that phase 2 SCI kick off with DOD funding and move it towards ADHD trials which is a much more lucrative market. That has to be their #1 objective for ampakines before exploring anything else in that space as there is a history to overcome with ampakines in general from my readings. The OSA program holds significant potential as well, but it is unclear why that is completely stalled.
I think this just adds to the consternation of the situation on the EM. Not only does it derail confidence in the leadership here, but all the secondary assets and possibilities appear stalled as well, eroding value. Hopefully, indeed they are preparing to emerge with a strategy soon and funding whether venture or BP cash to not only get the bell cow into clinics but prepare and move the ball forward on the other platforms as well. Fast and Furious corrections happen in pharma all the time. GLTA.
meixatech
1 week ago
RespireRx Pharmaceuticals Inc.'s (RSPI) potential for success
AI: Based on its pipeline, consider these key aspects:
1. RSPI's Pipeline and Target Areas:
RespireRx focuses on developing treatments for neurological and psychiatric disorders.
They have two main drug platforms:
ResolutionRx: Pharmaceutical cannabinoids, including dronabinol, targeting conditions like chemotherapy-induced nausea, anorexia in AIDS patients, and obstructive sleep apnea (OSA).
EndeavourRx: Neuromodulators, including:
AMPAkines: Positive allosteric modulators of glutamate receptors, potentially for CNS disorders, spinal cord injury, and orphan diseases.
GABAkines: Positive allosteric modulators of GABAA receptors, potentially for epilepsy and pain.
Specifically, they're developing treatments for conditions like epilepsy, pain, ADHD, spinal cord injury recovery, certain orphan diseases, and OSA.
2. Potential for Success:
Addressing Unmet Needs: RespireRx targets areas with limited or poor treatment options, which could be a significant advantage if their drugs prove effective and safe.
Novel Drug Platforms: They utilize proprietary compounds and target specific receptors, potentially leading to unique efficacy profiles and reduced side effects, giving them a competitive edge.
Advancing Clinical Trials: They've received a Department of Defense award to fund a Phase 2 clinical study for CX1739 (an AMPAkine) to improve bladder function in spinal cord injury patients, indicating progress in their pipeline.
Collaboration & Grants: Their collaboration with Shirley Ryan AbilityLab and receipt of the DOD grant suggests a proactive approach to research and development, which can be a positive sign for future success.
3. Challenges and Considerations:
Clinical Trial Success: The success of any pharmaceutical company hinges on the outcome of clinical trials. Even promising drugs can fail at this stage.
Regulatory Approvals: Obtaining regulatory approval can be a lengthy and costly process.
Funding & Resources: Developing and commercializing drugs requires substantial financial resources, which can be a challenge for smaller companies.
Competition: The pharmaceutical industry is competitive, and RespireRx will need to differentiate itself to succeed.
Market Adoption: Even with approvals, market acceptance and adoption of their products will be critical to commercial success.
In Conclusion:
RespireRx's pipeline shows promise, targeting areas with high unmet medical needs. Their focus on novel drug platforms and recent progress in clinical trials are encouraging signs. However, like all pharmaceutical companies, they face significant challenges related to clinical trial success, regulatory approvals, funding, and market competition. The potential for a successful company depends on their ability to navigate these challenges and bring their drugs to market effectively.
LTListener
1 week ago
Thing is they already spun out the OSA formulation to ResolutionRX. And I believe the intent was to have that entity trading somewhere at some point in time. It hasn't done anything since 2023, so even with funds committed, there must be a significant hurdle remaining. Maybe USA regulations with cannibas/cannibas derived, but that is just speculation since the company is silent about everything.
I would guess considering the history of the ampakine platform, they need to prove a lot before they get significant investment beyond this DOD funding which they can't even get going for some reason. Maybe some SBIR funds will come in for another indication like ADHD, maybe they can take some cash from say any gabakine platform deal and make progress. But if you were a major investor you wouldn't want the ampakine and gabakine platforms intertangled... At least I would not.
So would they reverse merge everything? Or sell off the other two platforms? In the shareholder letter they talked about individual asset valuation, funding the LLC, etc, etc... Is the OTC trading venue a place for a company with a prime asset that may garner upfront cash and huge milestone payments in the months and years to come? Seems like there would be a ton of logic to find a way onto the NASDAQ with the gabakine asset.
They have to do something sooner or later. Material events need to be disclosed and if they are approaching IND submission or funding or BP/partnership news, they better have a strategy to freaking communicate and have the company trading on a liquid platform.
meixatech
1 week ago
AI output concerning LBF Dronabinol. Another multi-billion dollar platform for RSPI?
The acronym "LBF" in the context of Dronabinol likely refers to Lipid-Based Formulations.
Here's why and what that implies:
1. What are Lipid-Based Formulations (LBFs)?
LBFs are drug delivery systems that utilize lipids (fats) and oils to improve the absorption and bioavailability of poorly water-soluble drugs, which is a common characteristic of many pharmaceutical compounds.
They can take various forms, such as self-emulsifying drug delivery systems (SEDDS), liposomes, and microemulsions.
2. Why Use LBFs for Dronabinol?
Dronabinol, a synthetic form of THC, is known to have low oral bioavailability due to its poor water solubility and extensive first-pass metabolism.
LBFs can help to improve the absorption of dronabinol by enhancing its solubility in the gastrointestinal tract and protecting it from degradation.
They may also help to reduce the food effect on dronabinol absorption, meaning that the drug's effectiveness is less dependent on whether it is taken with or without food.
3. LBFs and Dronabinol:
Research has explored the use of LBFs to deliver dronabinol, including the comparison of a dronabinol oral solution (Syndros) with dronabinol capsules (Marinol), where the solution may be considered a type of LBF.
Studies have investigated how LBFs can help overcome the food effect on dronabinol's pharmacokinetics, which can vary with different formulations and food intake.
In general, LBFs are considered promising strategies for improving the delivery of poorly water-soluble drugs like dronabinol.
In summary: "LBF" Dronabinol suggests a formulation of the drug designed to improve its absorption and bioavailability, potentially reducing variability and increasing its effectiveness, by utilizing a lipid-based drug delivery system.
loanranger
1 week ago
"So regardless whether Respire finally relays a strategy to update filings and get off the EM, it looks like this becomes a quotable and thus slightly more liquid entity come July 1st."
That's not the import of this statement:
"Issuers that do not provide updated information, ongoing reporting and the required management certifications will see their securities transition to the Pink Limited Market or to the Expert Restricted Market, whichever is applicable. This will make it clear that the issuer has no ongoing relationship with OTC Markets Group, while still allowing broker-dealers to serve clients willing to trade these securities."
Broker-dealers can trade Expert Market securities NOW, they just can't quote them and they just choose not to take on any new positions. Nothing will change regarding RSPI trading in July unless they address their filing failure.