Propofol

In recent years, among the new anesthetic sedation drugs launched on the market, Remazolam has undoubtedly aroused widespread concern in the industry. The drug was designed and synthesized by GlaxoSmithKline (GSK) in 1999, and after several corporate transfers, it was approved for market in China, the United States, Europe and other countries and regions around 2020. However, there are significant differences in the market performance of remazolam across countries. According to 2023 data, the drug's sales in China are about $40 million, while in the United States it is only $800,000, accounting for only 2% of the Chinese market. The reasons for this difference are worth exploring in depth. Remazolam is an ultra-short-acting GABAA receptor agonist whose design is inspired by midazolam and remifentanil, combining the properties of both. It is rapidly metabolized by carboxylesterases in the liver to produce inactive metabolites, resulting in rapid sedation resolution and short sedation recovery time. Remazolam's development history dates back to 1999, when GSK designed and synthesized the drug based on remifentanil's properties and filed a patent application. The patent was then transferred to TheraSci in the United Kingdom. Paion began developing the drug in 2008. Due to the instability of remazolam's free base, Paion developed remazolam benzenesulfonate, while Hengrui Pharmaceuticals adopted remazolam in the form of (toluene sulfonate) salt. At present, these two salt types of remazolam have been listed, of which Remazolam toluene sulfonate is only listed in China, while Remazolam benzenesulfonate is listed in China, Japan, the United States, Europe and other countries, but there are differences in indications. In the Chinese market, RenFCM obtained the Chinese market rights of Remazolam besylate in 2012, and was approved by the State Food and Drug Administration for sedation in colonoscopy in 2020, followed by the induction and maintenance of general anesthesia and the indication of bronchoscopic sedation. In the United States, Remazolam besylate was approved in July 2020 under the trade name Byfavo for a 30-minute sedation procedure marketed by Eagle. Remazolam besylate is approved for induction and maintenance of general anesthesia in Japan and South Korea. It is worth noting that in the first quarter of 2024, Paion was acquired by China's Renfu Pharmaceutical, which means that the global interests of Remazolam besylate have been vested in Renfu Pharmaceutical. Remazolam toluene sulfonate was first approved for sale in China in 2019 for indications including induction and maintenance of general anesthesia and sedation during colonoscopy. The difference in sales in the U.S. and China markets may be related to the different range of indications approved for remazolam in different countries. In the United States, Remazolam is only approved for procedural sedation, while in China, its approved indications include general anesthesia and sedation, and sales are significantly higher than in the United States. In addition, the difference in sales performance between China and the United States may also be related to concerns about remazolam metabolites. Remazolam is metabolized in the body to produce methanol, which may be further oxidized to formaldehyde and formic acid, and formaldehyde is potentially cytotoxic. As a result, the FDA requires remazolam to be administered only within 0.5 hours to avoid the buildup of methanol and its metabolites to dangerous levels. At present, other anesthetic sedatives commonly used in clinical practice, such as propofol, benzodiazepines (represented by midazolam), and α-receptor agonists (represented by dexmetropil), all have their own shortcomings. Although Remazolam still has room for improvement in some aspects, its unique advantages, such as rapid onset, rapid metabolism, rapid sedation recovery, etc., make it a potential application value in the field of anesthesia sedation. With the advancement of medical technology and the in-depth exploration of clinical applications, there may be an improved version of remazolam in the future, bringing new options to the field of anesthesia sedation.

The New Patent Covers ENA-001 Methods of Treating Respiratory Depression Caused by Propofol, a Widely Used, Centrally Acting AnestheticPRINCETON, NJ / ACCESSWIRE / November 14, 2024 / Enalare Therapeutics Inc., a clinical-stage biopharmaceutical company dedicated to developing novel compounds for the treatment of life-threatening critical care conditions and community health emergencies, today announced that the U.S. Patent and Trademark Office (USPTO) has granted U.S. Patent No. 12,138,267 on November 12, 2024, titled, "Methods of Treating Respiratory Depression Modulated by a Non-Opioid Agent," covering methods of treatment for the Company's novel proprietary agnostic respiratory stimulant product candidate, ENA-001. The granted patent has a term until January 2043 and builds upon the existing catalog of intellectual property for ENA-001, including composition of matter protection. "We are excited to have been granted this new patent for ENA-001 by the USPTO based on the innovative clinical activity of our scientific team," stated Joe Pergolizzi, M.D., Chief R&D Officer of Enalare Therapeutics. "Being able to fortify and extend the market exclusivity for a novel new chemical entity (NCE) like ENA-001 with this granted method of use patent helps ensure that we properly develop this one-of-a-kind agnostic respiratory stimulant with the potential to improve the lives of those impacted by several life-threatening conditions, including post-operative respiratory depression and community drug overdose, as well as a potential medical countermeasure in the case of mass-casualty events.""Being granted this new patent from the USPTO is recognition of ENA-001's therapeutic potential which is based on its novel and effective mechanism of action," stated Bob Raffa, Ph.D., Co-Founder and Head of Preclinical Development of Enalare Therapeutics. "We believe that ENA-001's differentiated approach to stimulating breathing by inhibiting Big Potassium (BK) ion channels in the carotid bodies, thus stimulating breathing across multiple etiologies of respiratory depression, regardless of its causality, offers the promise of becoming an important treatment option for patients experiencing a multitude of life-threatening conditions."This project has been funded in whole or in part with federal funds from the Department of Health and Human Services, Administration for Strategic Preparedness and Response, Biomedical Advanced Research and Development Authority, under contract number 75A50122C00072.The development of ENA-001 is also supported by the National Institute on Drug Abuse (NIDA) of the National Institutes of Health (NIH) under award number R44DA057133. The content of this document is the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health.About Enalare Therapeutics Inc.Enalare Therapeutics Inc. is a clinical-stage biopharmaceutical company dedicated to developing novel therapies for patients suffering from life-threatening critical care conditions and community-based health emergencies, including post-operative respiratory depression, community drug overdose, and apnea of prematurity. Enalare plans to initiate additional clinical studies for ENA-001 across multiple indications in the near term.About ENA-001Enalare's lead compound, ENA-001, is a one-of-a-kind new chemical entity (NCE) designed as an agnostic respiratory stimulant. The compound has a novel mechanism of action that affects ventilation via the peripheral chemoreceptor pathways in the carotid body. It utilizes the body's own ventilation control system to beneficially influence breathing and has been shown to be effective and well-tolerated in five human studies to date. With its novel mechanism of action and findings to date, it could potentially improve the lives of those impacted by several life-threatening conditions, including community drug overdose, post-operative respiratory depression, and apnea of prematurity. ENA-001 is an investigational compound and is not approved for use by the FDA.Forward-Looking Statement DisclaimerThis press release and any statements of representatives and partners of Enalare Therapeutics Inc. (the "Company") related thereto contain, or may contain, among other things, certain "forward-looking statements" within the meaning of the Private Securities Litigation Reform Act of 1995. Such forward-looking statements involve significant risks and uncertainties. Such statements may include, without limitation, statements with respect to the Company's plans, objectives, projections, expectations and intentions and other statements identified by words such as "projects," "may," "will," "could," "would," "should," "believes," "expects," "anticipates," "estimates," "intends," "plans," "potential" or similar expressions. Because forward-looking statements relate to the future, they are subject to inherent uncertainties, risks and changes in circumstances that are difficult to predict and many of which are outside of the Company's control. The Company's actual results may differ materially from those indicated in the forward-looking statements. Therefore, you should not rely on any of these forward-looking statements. Any forward-looking statements that the Company makes in this press release speak only as of the date of this press release. The Company assumes no obligation to update its forward-looking statements whether as a result of new information, future events or otherwise, after the date of this press release.###CONTACT:Morgan WagnerInvestor and Media Relations[email protected]SOURCE: Enalare Therapeutics Inc. View the original press release on newswire.com.Source: Enalare Therapeutics