Opioid receptors antagonists(Opioid receptors antagonists), κ opioid receptor agonists(Kappa opioid receptor agonists), μ opioid receptor antagonists(Mu opioid receptor antagonists)

Therapeutic Areas

Other DiseasesSkin and Musculoskeletal Diseases

Active Indication

AlcoholismOpiate OverdosePruritus+ [1]

Inactive Indication

GamblingSmoking Cessation

Originator Organization

Baxter International, Inc.

Active Organization

Tharimmune, Inc.

Orexo AB

Purdue Pharma LP

+ [6]

Inactive Organization

Somaxon Pharmaceuticals, Inc.Hikma Pharmaceuticals USA, Inc.

Drug Highest PhaseApproved

First Approval Date

US (17 Apr 1995),

Opiate Overdose

RegulationFast Track (US), Priority Review (US)

Structure

Molecular FormulaC21H25NO3

InChIKeyWJBLNOPPDWQMCH-MBPVOVBZSA-N

CAS Registry55096-26-9

View All Structures (2)

Clinical Trials associated with Nalmefene Hydrochloride

NCT06408714 / RecruitingPhase 3IIT

Comparison of Nalmefene Hydrochloride Injection and Naloxone Hydrochloride Injection for the Treatment of Recurrent Respiratory Depression After Suspected Acute Opioid Overdose in the Emergency Department

The goal of this clinical trial is to compare naloxone to nalmefene for the treatment of opioid overdose in adults. The main questions it aims to answer are:
* Does nalmefene lower the number of doses of medicine participants need to treat opioid overdose?
* When participants are given nalmefene instead of naloxone, do they have fewer complications of opioid overdose such as being admitted to the hospital or having a breathing tube inserted?
Researchers will compare nalmefene to naloxone for the treatment of opioid overdose. Nalmefene and naloxone are both approved medicines to treat opioid overdose.
Participants who are brought to the emergency department after an opioid overdose will be given a dose of either nalmefene or naloxone if their breathing slows down again after an opioid overdose. Participants will:
* Stay in the emergency department for 8 hours after receiving a dose of nalmefene or naloxone.
* Receive a phone call 7 days after their emergency department to check on how they are doing.
Background information:
Naloxone (also known as Narcan) and nalmefene are opioid blocking medicines. When someone overdoses on an opioid, such as heroin or fentanyl, their breathing slows down or stops and they can die. By giving naloxone or nalmefene, the effect of the opioid can be blocked and the person can start breathing again. Naloxone is the most commonly used medicine to reverse an opioid overdose. The effect of naloxone lasts about an hour, and patients may need more than one dose of naloxone to keep them breathing. Sometimes patients overdose, get a dose of naloxone and wake up, and then some time later their breathing slows down again and they need another dose of naloxone. This can happen because the effect of the opioid they took lasts longer than the effect of the naloxone.
The effect of nalmefene lasts longer than naloxone, about four hours. If a person gets nalmefene, their opioid may wear off before the nalmefene wears off and they might not need any more doses of a reversal medicine. Both naloxone and nalmefene are approved medicines for treating opioid overdose.
Often, when a person overdoses on an opioid, someone gives them naloxone right away and then they are brought to the emergency department. In the emergency department, they are watched for several hours to make sure they don't stop breathing again when their naloxone wears off. If they do stop breathing again, they are given another dose of naloxone. In this study, participants will be given either nalmefene or naloxone if their breathing slows down while they are in the emergency department.

Start Date26 Aug 2024

Sponsor / Collaborator

The University of New Mexico

ChiCTR2400088347 / SuspendedPhase 4IIT

Application of different doses of nalmefene pre-injection in painless gastrointestinal enddoscopy

Start Date20 Aug 2024

Sponsor / Collaborator-

ChiCTR2400083472 / RecruitingPhase 1IIT

Observation on the effect of nalmefene pre-injection on the prevention of hypoxemia during painless gastroscopy in high-risk patients with difficult airway

Start Date10 May 2024

Sponsor / Collaborator-

100 Clinical Results associated with Nalmefene Hydrochloride

100 Translational Medicine associated with Nalmefene Hydrochloride

100 Patents (Medical) associated with Nalmefene Hydrochloride

476

Literatures (Medical) associated with Nalmefene Hydrochloride

01 Nov 2024·Hepatology Research

Brief intervention for chronic liver disease patients with alcohol use disorder in a hepatology outpatient unit: Effects and limitations

Article

Author: Hara, Nagisa ; Shiraki, Makoto ; Namisaki, Tadashi ; Eguchi, Yuichiro ; Nakao, Kazuhiko ; Ohama, Hideko ; Tada, Fujimasa ; Hiraoka, Atsushi ; Miyaaki, Hisamitsu ; Yoshiji, Hitoshi ; Nakai, Masato ; Takahashi, Hirokazu ; Sakamoto, Naoya ; Hisanaga, Takuro ; Takami, Taro

AbstractAimIt is not uncommon to encounter outpatients in the hepatology department with harmful alcohol habits. When treating such chronic liver disease (CLD) patients, an adequate intervention method for harm reduction of alcohol use, such as brief intervention (BI) or BI and nalmefene, should be considered. This study aimed to elucidate the clinical effectiveness of BI for CLD patients affected by harmful alcohol use.MethodsFrom June 2021 to 2023, 123 Japanese CLD outpatients (hepatitis B virus : hepatitis C virus : alcoholic liver disease : others = 32:18:42:31) with an Alcohol Use Disorders Identification Test (AUDIT) score of ≥8 at the initial interview and a repeat interview with AUDIT 9 months later were enrolled. Clinical features related to patient behavior following the initial AUDIT interview were retrospectively evaluated, and compared between patients without and with BI treatment.ResultsFor the non‐BI and BI groups, baseline AUDIT score (median 10 [interquartile range (IQR) 9–13] vs. 12 [IQR 10–17], p = 0.016) and relative change in AUDIT score (median 0 [IQR −3 to 2] vs. −3 [IQR −7 to 0], p < 0.01) showed significant differences, whereas there was no significant difference between the groups for AUDIT score at the time of the second interview (p = 0.156). Following BI, significant improvements were observed for items 1, 2, 3, 4, 5, 8, and 10 of AUDIT (each p < 0.05).ConclusionPatients with an alcohol use disorder as well as those with alcohol dependency who received BI showed a significant decline in AUDIT score, although the score of the follow‐up AUDIT indicated continued alcohol use disorder. In addition to BI, medication with nalmefene should be considered, based on individual factors.

01 Oct 2024·Clinical and Molecular Hepatology

Immunological mechanisms in steatotic liver diseases: An overview and clinical perspectives

Review

Author: Gao, Wenyuan ; Yan, Mengyao ; Ma, Long ; Huang, Luqi ; Guo, Lanping ; Man, Shuli

Steatotic liver diseases (SLD) are the principal worldwide cause of cirrhosis and end-stage liver cancer, affecting nearly a quarter of the global population. SLD includes metabolic dysfunction-associated alcoholic liver disease (MetALD) and metabolic dysfunction-associated steatotic liver disease (MASLD), resulting in asymptomatic liver steatosis, fibrosis, cirrhosis and associated complications. The immune processes include gut dysbiosis, adiposeliver organ crosstalk, hepatocyte death and immune cell-mediated inflammatory processes. Notably, various immune cells such as B cells, plasma cells, dendritic cells, conventional CD4<sup>+</sup> and CD8<sup>+</sup> T cells, innate-like T cells, platelets, neutrophils and macrophages play vital roles in the development of MetALD and MASLD. Immunological modulations targeting hepatocyte death, inflammatory reactions and gut microbiome include N-acetylcysteine, selonsertib, F-652, prednisone, pentoxifylline, anakinra, JKB-121, HA35, obeticholic acid, probiotics, prebiotics, antibiotics and fecal microbiota transplantation. Understanding the immunological mechanisms underlying SLD is crucial for advancing clinical therapeutic strategies.

01 Sep 2024·Environmental Toxicology and Pharmacology

Targeting α1- and α2-adrenergic receptors as a countermeasure for fentanyl-induced locomotor and ventilatory depression

Article

Author: Alilain, Warren J ; Turner, Jill R ; Denehy, Emily D ; Martin, Jocelyn R ; Taylor, Chase E ; Luo, Dan ; Shaykin, Jakob D ; Sunshine, Michael D ; Chandler, Cassie M ; Prisinzano, Thomas E ; Bardo, Michael T

This study assessed the ability of α₁ and α₂-adrenergic drugs to decrease fentanyl-induced locomotor and ventilatory depression. Rats were given saline or fentanyl, followed by: (1) naltrexone, (2) naloxone, (3) nalmefene, (4) α₁ agonist phenylephrine, (5) α₁ antagonist prazosin, (6) α_1D antagonist BMY-7378, (7) α₂ agonist clonidine, (8) α₂ antagonist yohimbine or (9) vehicle. All µ-opioid antagonists dose-dependently reversed fentanyl-induced locomotor and ventilatory depression. While the α₁ drugs did not alter the effects of fentanyl, clonidine dose-dependently decreased locomotion and respiration with and without fentanyl. Conversely, yohimbine given at a low dose (0.3-1 mg/kg) stimulated ventilation when given alone and higher doses (>1 mg/kg) partially reversed (∼50 %) fentanyl-induced ventilatory depression, but not locomotor depression. High doses of yohimbine in combination with a suboptimal dose of naltrexone reversed fentanyl-induced ventilatory depression, suggestive of additivity. Yohimbine may serve as an effective adjunctive countermeasure agent combined with naltrexone to rescue fentanyl-induced ventilatory depression.

News (Medical) associated with Nalmefene Hydrochloride

30 Sep 2024

·www.biospace.com

Study Examining Use of Nalmefene HCI Injection for Opioid Overdose Reversal in Emergency Departments Concludes Observational Period

STAMFORD, Conn.--(BUSINESS WIRE)--Purdue Pharma has completed the first phase of a study examining the use of nalmefene hydrochloride (HCI) injection in real-world emergency department (ED) settings. Researchers are now conducting data analysis, with study results expected later this year. The research was funded by Purdue. Nalmefene hydrochloride injection is available as a 2mg/2mL (1mg/1mL) vial, and is an opioid antagonist indicated for the complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids and in the management of known or suspected overdose. Nalmefene hydrochloride injection is contraindicated in patients with a known hypersensitivity to the product. 1 “We distribute nalmefene injection for no profit, as part of our commitment to providing opioid overdose treatments that can help save lives in communities across the country,” said Craig Landau, MD, President and CEO, Purdue. “We look forward to learning about the results of the study.” The Clinical Outcomes from Injectable Nalmefene in the Emergency Department (COINED) study is designed to measure the frequency of successful reversal of acute opioid toxicity following administration of nalmefene or naloxone, as well as the dosages used. The study is also evaluating the clinical course of patients after receiving an opioid antagonist, including length of stay in the ED, frequency of precipitated withdrawal, and any additional medications used to treat patient symptoms. “The study was designed to better understand how long-acting reversal agents impact patients in today’s rapidly evolving opioid environment,” said Justin Seltzer, MD, Emergency Medicine Physician and Medical Toxicologist at UC San Diego Health. “The results of this study could provide information that can help health care providers make informed treatment decisions for their patients.” The COINED study is a 14-month observational retrospective cohort study with secondary data analysis from electronic health records and medical charts of approximately 60 patients who were administered nalmefene with or without naloxone in the ED and approximately 60 patients who were administered only naloxone in the ED. The study took place in Emergency Departments at UC San Diego Health and El Centro Regional Medical Center. Choice of opioid antagonist administration was made according to the clinical judgements of patients’ health care providers. “Consistent with recent recommendations from the American College of Medical Toxicology and the American Academy of Clinical Toxicology 2 , we hope this study will provide robust data on nalmefene administrations including the effectiveness of nalmefene in ED settings,” said Thomas Alfieri, PhD, Director of Medical Affairs Strategic Research at Purdue Pharma. Health care professionals can learn more about nalmefene at . IMPORTANT SAFETY INFORMATION INDICATIONS AND USAGE Nalmefene Hydrochloride Injection is indicated for the complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids. Nalmefene Hydrochloride Injection is indicated in the management of known or suspected opioid overdose. CONTRAINDICATION Nalmefene Hydrochloride injection is contraindicated in patients with a known hypersensitivity to the product. WARNINGS AND PRECAUTIONS Use of Nalmefene Hydrochloride injection in Emergencies Nalmefene Hydrochloride injection, like all drugs in this class, is not the primary treatment for ventilatory failure. In most emergency settings, treatment with Nalmefene Hydrochloride injection should follow, not precede, the establishment of a patent airway, ventilatory assistance, administration of oxygen, and establishment of circulatory access. Risk of Recurrent Respiratory Depression Accidental overdose with long acting opioids [such as methadone and levo -alpha-acetylmethadol (LAAM)] may result in prolonged respiratory depression. Respiratory depression in both the postoperative and overdose setting may be complex and involve the effects of anesthetic agents, neuromuscular blockers, and other drugs. While Nalmefene Hydrochloride injection has a longer duration of action than naloxone in fully reversing doses, the physician should be aware that a recurrence of respiratory depression is possible, even after an apparently adequate initial response to Nalmefene Hydrochloride injection treatment. Patients treated with Nalmefene Hydrochloride injection should be observed until, in the opinion of the physician, there is no reasonable risk of recurrent respiratory depression. Cardiovascular Risks with Narcotic Antagonists Pulmonary edema, cardiovascular instability, hypotension, hypertension, ventricular tachycardia, and ventricular fibrillation have been reported in connection with opioid reversal in both postoperative and emergency department settings. In many cases, these effects appear to be the result of abrupt reversal of opioid effects. Although Nalmefene Hydrochloride injection has been used safely in patients with pre-existing cardiac disease, all drugs of this class should be used with caution in patients at high cardiovascular risk or who have received potentially cardiotoxic drugs. Risk of Precipitated Withdrawal Nalmefene Hydrochloride injection, like other opioid antagonists, is known to produce acute withdrawal symptoms and, therefore, should be used with extreme caution in patients with known physical dependence on opioids or following surgery involving high doses of opioids. Imprudent use or excessive doses of opioid antagonists in the postoperative setting has been associated with hypertension, tachycardia, and excessive mortality in patients at high risk for cardiovascular complications. Incomplete Reversal of Buprenorphine Preclinical studies have shown that nalmefene at doses up to 10 mg/kg (437 times the maximum recommended human dose) produced incomplete reversal of buprenorphine-induced analgesia in animal models. This appears to be a consequence of a high affinity and slow displacement of buprenorphine from the opioid receptors. Hence, Nalmefene Hydrochloride injection may not completely reverse buprenorphine-induced respiratory depression. Use in Pediatric Patients Safety and effectiveness of nalmefene hydrochloride injection in pediatric patients have not been established. ADVERSE REACTIONS The most common adverse reactions (>1%) reported in clinical trials with nalmefene injection were nausea (18%), vomiting (9%), tachycardia (5%), hypertension (5%), postoperative pain (4%), fever (3%), and dizziness (3%). To report SUSPECTED ADVERSE REACTIONS, contact Purdue Pharma L.P. at 1-888-726-7535 or FDA at 1-800-FDA-1088 or . Please read Prescribing Information available here . For more information, visit . About Purdue Pharma L.P. Purdue Pharma and its subsidiaries develop, manufacture and market medications to meet the evolving needs of healthcare professionals, patients, and caregivers. Purdue and its subsidiaries focus on balancing innovative science with clinically effective, compassionate care. The Company’s goal is to serve patients who rely on its medicines, pursue its pipeline of branded and generic medications, and introduce medicines that will help save and improve lives. Purdue continues to work tirelessly with creditors to reach a new settlement that delivers billions of dollars of value for opioid crisis abatement. For more information, visit . References Nalmefene Hydrochloride Injection 2mg/2mL (1mg/1mL) [Full Prescribing Information]. Stamford, CT: Purdue Pharma L.P., 02/08/2022. . Accessed August 5, 2024. Stolbach AI, Mazer-Amirshahi M, Nelson LS, et al.; American College of Medical Toxicology and the American Academy of Clinical Toxicology Position Statement: Nalmefene should not replace naloxone as the primary opioid antidote at this time. J Med Toxicol. 2024; 20:64–67. MR-08578 Contacts Media Contact: news@pharma.com

Drug Approval

16 Sep 2024

·pipelinereview.com

Tharimmune Acquires Global License and Partners With Intract Pharma to Develop an Oral Formulation of Infliximab

BRIDGEWATER, NJ, USA and LONDON, UK I September 16, 2024 I Tharimmune, Inc . (NASDAQ:THAR) (“Tharimmune” or the “Company”), a clinical-stage biotechnology company developing a portfolio of therapeutic candidates in inflammation and immunology, announced today that it has entered into a definitive agreement with Intract Pharma to exclusively license INT-023/TH023, an oral anti-tumor necrosis factor-alpha (TNF-α) monoclonal antibody, infliximab. This strategic partnership aims to expand Tharimmune’s therapeutic pipeline and reinforce its commitment to pioneering novel treatments for autoimmune diseases. Under the terms of the agreement, Tharimmune licensed global development and commercialization rights (outside of South Korea) to Intract Pharma’s Soteria ® and Phloral ® delivery platform along with an existing supply agreement for infliximab to be used in the oral product development program. Intract Pharma received an upfront payment and is eligible to receive additional payments upon an equity financing of the Company and is eligible for future development, regulatory and commercial milestones, as well as mid-single digit royalties based on net product sales. The agreement retains a right of first refusal to continue development and commercialization after a Phase 2 clinical trial. In addition, Tharimmune has the option to exercise the license to Intract’s platform for up to four additional targets. Infliximab is a purified, recombinant DNA-derived chimeric IgG monoclonal antibody protein that contains both murine and human components that inhibit TNF-α. Tumor necrosis factor-alpha is a signaling protein involved in acute phase reactions and systemic inflammation. Infliximab is sold by Janssen Biotech under the Remicade ® brand for numerous indications including Crohn’s disease, ulcerative colitis, rheumatoid diseases and plaque psoriasis. Traditionally administered through intravenous infusions, oral delivery of antibodies such as infliximab is challenging due to the complexity of navigating such large molecules through the gastrointestinal tract. This new partnership aims to overcome these challenges using Intract’s delivery platform, making it possible to administer infliximab in a pill form. An oral route of administration holds potential to improve patient compliance and quality of life, while also reducing the burden on the healthcare system associated with long-term intravenous therapy. “The integration of Intract’s innovative technology, combined with the high-quality infliximab monoclonal antibody provided by their existing supply agreement, holds tremendous potential to accelerate and reinforce our commitment to immunology. This new collaboration not only broadens our therapeutic focus, but also aligns with our mission to improve patient outcomes by developing more convenient and accessible treatment options,” said Randy Milby, CEO of Tharimmune. “An oral form of infliximab represents a significant advancement in the treatment of chronic inflammatory diseases, and the opportunity for Tharimmune to compete in a multibillion-dollar global market.” This partnership enables the targeted delivery of antibody therapeutics directly to the colon or small intestine. By leveraging Intract’s platform, Tharimmune aims to enhance the effectiveness of TNF-α inhibitors such as infliximab through precision delivery that maximizes proteolytic stabilization and tissue permeation. This novel approach offers significant potential for directly addressing inflammatory conditions within the gastrointestinal tract, including inflammatory bowel disease, as well as systemic inflammatory disorders where TNF-α plays a critical role in disease progression. “Safer and orally available biological treatments for long term use in chronic inflammation and immune mediated diseases represents a major area of medical need for millions of patients” said Vipul Yadav, CEO of Intract. “We are delighted to be partnering with Tharimmune and bringing on board their clinical development expertise in immunology to further advance together our oral anti-TNFα antibody into the clinic”. About Intract Pharma Intract is a biopharmaceutical company developing disruptive oral antibody delivery solutions to significantly improve the efficacy and safety of emerging and established protein therapeutics, as well as improve patient experience and outcomes in inflammation and immunology indications. Its platform leverages the advantage of precision targeting of large proteins and antibodies to the colon, while also protecting the biologics from enzymatic breakdown, allowing tissue/systemic uptake to create next-generation oral antibody medicines. For more information, please visit www.intractpharma.com About Tharimmune Tharimmune, Inc. is a clinical-stage biotechnology company developing a portfolio of therapeutic candidates for inflammation and immunology. The Company’s lead clinical-stage asset, TH104, is known to suppress chronic, debilitating pruritus or “uncontrollable itching” in PBC, a rare and orphan liver disease with no known cure. The Company’s early-stage immunology pipeline includes novel multi-specific antibodies targeting unique epitopes with novel mechanisms of action against well-known, validated targets in multiple solid tumors, including PD-1, HER2 and HER3. Tharimmune has a license agreement with OmniAb, Inc. to access the company’s antibody discovery technology platform against these and other specified targets. For more information, please visit www.tharimmune.com . SOURCE: Tharimmune

License out/inImmunotherapyDrug ApprovalPhase 2ADC

03 Sep 2024

·www.prnewswire.com

Elysium Therapeutics Presents Phase 1 Proof-of-Concept Results for Novel SMART™ O2P Opioid Technology for Acute Pain that Reduces the Potential for Abuse, Diversion, and Risk of Oral Overdose at PAINWeek 2024

SMART™ opioid prodrugs leverage Elysium's O2P (Oral Overdose Protected) technology to effectively mitigate non-oral and oral abuse while safely delivering FDA-cleared opioid agonists, which continue to play a vital role in the treatment of acute pain Phase 1 results demonstrated effective acute pain relief while simultaneously mitigating the major risks of existing opioids by protecting against abuse, diversion, and fatal overdose LYONS, Colo., Sept. 3, 2024 /PRNewswire/ -- Elysium Therapeutics, an emerging biopharmaceutical company establishing new standards for safety in the opioid industry by developing SMART™ (Safer Medicines Alleviate Risks and Trauma) products, first- and best-in-class medicines to address the limitations and dangers associated with opioids and overdose rescue agents, today announced its Phase 1, human-proof-of-concept study investigating the company's proprietary Oral Overdose Protected (O2P™) hydrocodone prodrug for the treatment of moderate-to-severe acute pain will be presented at PAINWeek 2024 being held September 3-6 in Las Vegas. The poster titled, "SMART™ Opioids with Unprecedented Protection Against Abuse and Oral Overdose – Human Proof-of-Concept", evaluates the safety, tolerability, and pharmacokinetics of oral O2P Hydrocodone relative to a hydrocodone bitartrate (HCBT) comparator following single oral doses in healthy adult subjects. The presentation of the successful Phase 1 study outlines a promising and novel approach, providing effective acute pain relief while simultaneously mitigating the major risks of existing opioids by protecting against abuse, diversion, and fatal overdose. The Phase 1 study achieved several key milestones, demonstrating a significant reduction in the number of prescribed doses that mitigates misuse, abuse, and diversion. Additionally, the authors were able to show that oral O2P Hydrocodone has the potential to limit the number of euphoric experiences that may serve to initiate and reinforce abusive behavior. "A key finding we look forward to presenting is the sustained plasma exposure of hydrocodone with O2P Hydrocodone, which is consistent with a once-daily dosing regimen," said Tom Jenkins, Ph.D., Co-Founder and Chief Scientific Officer of Elysium Therapeutics and inventor of trypsin-activated opioid prodrugs and concomitant use of trypsin inhibition to govern opioid exposure. "As a consequence, we anticipate being able to significantly reduce the number of prescribed tablets for O2P Hydrocodone compared to currently prescribed hydrocodone. Additionally, the O2P Hydrocodone technology is designed to attenuate hydrocodone exposures when supratherapeutic doses are ingested dramatically reducing the number of euphoric experiences available from an O2P Hydrocodone prescription." "Elysium is on a mission to establish a new standard of safety in the opioid industry, so we look forward to presenting our Phase 1 Proof-of-Concept findings for our O2P Hydrocodone technology, which we believe can significantly reduce the risk of fatal overdoses while providing the unmatched effective management of acute pain possible with opioid treatment," said Greg Sturmer, Co-Founder and CEO of Elysium Therapeutics. "For decades, as the opioid crisis has ravaged the nation, drug developers have largely failed to bring effective solutions for pain management to the clinic that offer a solution to the broader problems of abuse. We believe O2P Hydrocodone can be an important step in bringing solutions to this immense challenge." Poster Information: Title: SMART™ Opioids with Unprecedented Protection Against Abuse and Oral Overdose – Human Proof-of-Concept Authors: T. Jenkins, Ph.D., Lynn R. Webster, M.D., Leela Vrishabhendra, M.D., A. Greg Sturmer Time & Location: PAINWeek 2024, September 3-6 at The Cosmopolitan of Las Vegas About O2P™ Hydrocodone Elysium's lead product candidate – oral-overdose protected (O2P) hydrocodone – is a hydrocodone prodrug being developed for the treatment of moderate-to-severe acute pain. Elysium leverages its proprietary bifunctional prodrug technology, containing a trypsin-activated opioid delivery subunit that efficiently releases therapeutic levels of hydrocodone when exposed to the digestive enzyme trypsin in the lumen of the small intestine, and a trypsin inhibitor subunit that progressively inhibits trypsin, attenuating the release of hydrocodone when supratherapeutic doses are ingested. About the Phase 1 O2P-001 Study O2P-001 was a Phase 1, human proof-of-concept, randomized, open-label, two-part study designed to evaluate the safety and pharmacokinetics of O2P hydrocodone in healthy adult subjects. The key objectives of the study were to (i) evaluate the safety, tolerability, and pharmacokinetics of O2P hydrocodone relative to a hydrocodone comparator following single oral doses in healthy adult subjects with naltrexone blockade; and (ii) demonstrate reduced dose-proportional plasma exposures of hydrocodone (i.e., oral overdose protection) of O2P hydrocodone relative to an escalated comparator dose of hydrocodone. A total of 93 subjects were enrolled in the study. About Elysium Therapeutics Elysium is an emerging biopharmaceutical company that is establishing new standards of safety in the opioid industry by developing SMART™ (Safer Medicines Alleviate Risks and Trauma) products, first- and best-in-class medicines that address the limitations and dangers associated with opioids and overdose rescue agents to reduce suffering from opioid-use disorder, opioid overdose, and acute pain. Elysium's lead SMART opioid product candidate – oral-overdose protected (O2P™) hydrocodone – is being developed for the treatment of moderate-to-severe acute pain. Elysium is also developing its SMART rescue medicine, SOOPR™ (Synthetic Opioid Overdose Prevention and Reversal), a long-acting opioid antagonist specifically designed to address oral synthetic opioid, including fentanyl, overdose. Tens of thousands of unnecessary overdose deaths each year exemplifies the critical shortcomings of currently available rescue agents, including naloxone and nalmefene. For more information, please visit . SOURCE Elysium Therapeutics

Phase 1Clinical Result

100 Deals associated with Nalmefene Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
D02104	Nalmefene Hydrochloride	N07BB05	DB06230

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Alcoholism	LI	H. Lundbeck A/S	24 Feb 2013
Alcoholism	EU	H. Lundbeck A/S	24 Feb 2013
Alcoholism	IS	H. Lundbeck A/S	24 Feb 2013
Alcoholism	NO	H. Lundbeck A/S	24 Feb 2013
Opiate Overdose	CN	Chengdu Tiantaishan Pharmaceutical Co., Ltd.	22 Sep 2008

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Pruritus	Phase 2	-	Avior Bio, Inc.Startup	24 Mar 2022
Opioid-Related Disorders	Phase 1	US	Titan Pharmaceuticals, Inc.	05 Jul 2022
Alcoholism	Phase 1	RU	H. Lundbeck A/S	01 Mar 2009
Gambling	Phase 1	-	Somaxon Pharmaceuticals, Inc.	01 Aug 2005
Alcoholism	Preclinical	UA	H. Lundbeck A/S	01 Mar 2009
Smoking Cessation	Preclinical	US	Somaxon Pharmaceuticals, Inc.	01 Sep 2005

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Company_Website Manual	Phase 1	Chronic liver disease	12	TH104 (Child-Pugh A)	(nhxnitrbho) = hmnjwqdslf sfgpsmpcbw (yeahjfzbmb ) View more	Positive	28 Oct 2024
				TH104 (Child-Pugh B)	(nhxnitrbho) = gjlpskxbtx sfgpsmpcbw (yeahjfzbmb ) View more
NCT04759768 (CTgov)	Phase 1	-	68	Nalmefene Hydrochloride (Intranasal Nalmefene)	(hjgudheseq) = ivekfbuxjo wfkecsszts (adkmqqvkbg, mfxbrogjzg - sxfllrlnmo) View more	-	13 Aug 2024
				Nalmefene (Intramuscular Nalmefene)	(hjgudheseq) = gfyaczxzit wfkecsszts (adkmqqvkbg, dohazibuot - lowvwqwfeq) View more
NCT05219669 (CTgov)	Phase 1	Opiate Overdose	24	Nalmefene Hydrochloride (Intranasal Nalmefene 1 Spray in 1 Nostril)	(cssirmqmcc) = nbrpzbnycc zmxofzqsma (kkgnywtnmk, pyzjkrfiew - tgfbvmhtad) View more	-	05 Aug 2024
				Nalmefene Hydrochloride (Intranasal Nalmefene 2 Sprays in 1 Nostril)	(cssirmqmcc) = sbwmndjojq zmxofzqsma (kkgnywtnmk, lqtfungczo - dagmpamvrf) View more
Biospace Manual	Phase 1	Chronic liver disease	12	TH104	(axxewqcofq) = qqxhgvdsjq phcuvuvobz (yqfpaffgem ) View more	Positive	11 Dec 2023
				TH104 (Child-Pugh A)	(axxewqcofq) = yrrhyuiyqi phcuvuvobz (yqfpaffgem ) View more
Biospace Manual	Phase 1	Cholestatic pruritus	-	TH104	(skmcwnviyo) = The Cmax and AUC0-∞ of TH104 was observed to be higher than the tablet product because of a possible reduced presystemic metabolism in the lower GI and liver, which is potentially advantageous for patients with an impaired liver. The half-life and Tmax was observed to be similar for both products. spoajmcizg (lejltjxwds ) View more	Positive	27 Nov 2023
NCT03278886 (PETER PAIN, CTgov)	Phase 1/2	Pain \| Inflammation \| HIV Infections \| Alcohol-Related Disorders	11	Low dose naltrexone (Low Dose Naltrexone)	qupqettxnj(entclqtdal) = iphkecpmng twrgoiyvca (jitsztvmgo, ofrydzgyfy - sablbxydkm) View more	-	03 Aug 2020
				Nalmefene (Nalmefene)	qupqettxnj(entclqtdal) = bijfadjhmy twrgoiyvca (jitsztvmgo, ldovubzlww - ixtsdtzqrx) View more
NCT02382276 (CTgov)	Phase 3	Alcoholism	405	Nalmefene (Nalmefene 20 mg in the lead-in Study)	ferzzhtqzc(tylbhwkfnz) = ntwkeumfjm lgunvrbkcn (jfcgsilfaw, clmxzzlyco - jfkemlxtym) View more	-	20 Jul 2020
				Nalmefene (Nalmefene 10 mg in the lead-in Study)	ferzzhtqzc(tylbhwkfnz) = ztcodjrzwh lgunvrbkcn (jfcgsilfaw, toxhgbccio - enxagsatyy) View more
NCT02364947 (CTgov)	Phase 3	Alcoholism	678	Nalmefene hydrochloride (Nalmefene Hydrochloride 20 mg)	tiahiusmgb(vtjzrxwrcz) = tnyxlfnarj fxbszhynqo (tlnqtcloio, yizckcraje - tbxyrqonvz) View more	-	30 Sep 2019
				Nalmefene hydrochloride (Nalmefene Hydrochloride 10 mg)	tiahiusmgb(vtjzrxwrcz) = zglwrwwdso fxbszhynqo (tlnqtcloio, pcgrryrndw - bodhemlkrq) View more
NCT02679469 (CTgov)	Phase 1	Alcoholism	7	nalmefene hydrochloride 10 mg	micpfazfrc(lbbaxblbbz) = ntepbkqqti pxzkxkmdzx (nqyutcdmqg, xmulczavgz - qjfigyomun) View more	-	18 Apr 2017
NCT00811941 (SENSE, CTgov)	Phase 3	Alcoholism	665	Placebo	lwmqpwqdtt(kzoszemria) = vawlmnmrgk wtbjmvnccp (nkdmthtcic, depqqrqmsh - khytqkhwuo) View more	-	07 Aug 2013

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