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Last update 08 May 2025

Hydrocodone bitartrate

Last update 08 May 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

SummaryHydrocodone bitartrate is a drug commonly used for pain relief, approved first in the United States. The drug works by binding to opioid receptors in the brain, acting as a mu/kappa/delta agonist. Its chemical name is 4,5(alpha)-epoxy-3-methoxy-17-methylmorphinan-6-one tartrate (1:1) hydrate (2:5) or morphinan-6-one, 4,5-epoxy-3-methoxy-17-methyl-, (5 alpha)-, [R (R*, R*)]-2,3-dihydroxybutanedioate (1:1),hydrate (2:5). Hydrocodone bitartrate is widely used in the U.S. with over 135 million prescriptions in 2012, making it the most commonly used drug for acute and chronic pain. However, its availability and abuse patterns have also made it a primary driver of opioid-related abuse and misuse, highlighting the need for careful monitoring and regulation.

Drug Type

Small molecule drug

Synonyms

酒石酸氢可酮

+ [9]

Target

Opioid receptors

Action

agonists

Mechanism

Opioid receptors agonists(Opioid receptors agonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Pain

Inactive Indication

Chronic osteoarthritisChronic PainDrug abuse+ [3]

Originator Organization-

Active Organization

Purdue Pharma LP

Inactive Organization

Teva Branded Pharmaceutical Products R&D, Inc.

Societal CDMO Gainesville LLC

Zogenix, Inc.

+ [1]

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (25 Oct 2013),

Pain

Regulation-

Structure/Sequence

Molecular FormulaC22H29NO10

InChIKeyZICRJLQTAUVSDU-NSJZFRMTSA-N

CAS Registry34195-34-1

Clinical Trials associated with Hydrocodone bitartrate

NCT06780202

/ RecruitingPhase 2IIT

Assessment of Medrol Dosepak to Reduce Opioid Consumption in Foot and Ankle Surgical Patients

This clinical trial aims to determine the effects of a 6-day low-dose methylprednisolone course on pain, nausea, and total opioid consumption in patients undergoing foot and ankle surgeries.
The secondary objective of the study is to determine and monitor the effects of the course on complications following surgery and patient-reported outcomes

Start Date27 Jan 2025

Sponsor / Collaborator

Emory University

NCT06585163

/ Not yet recruitingPhase 1

A Phase 1, Randomized, Double-blind, Crossover Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of QEV-817 Oral Suspension in Healthy Volunteers

This study has been designed to assess the safety, tolerability, and pharmacokinetics of a therapeutic dose of hydrocodone bitartrate with and without an oral dose of doxapram hydrochloride in healthy volunteers who are naltrexone-blocked.

Start Date01 Sep 2024

Sponsor / Collaborator

Quivive Pharma, Inc.

[+1]

NCT06232577

/ Active, not recruitingPhase 2IIT

5x-Multiplier vs 3-Tier Model for Discharge Opioid Prescriptions After Intra-abdominal Cancer Surgery: A Randomized Clinical Trial

To compare 2 different models for prescribing opioid pain medication to provide better pain control to participants with an abdominal cancer who are having surgery.

Start Date27 Mar 2024

Sponsor / Collaborator

The University of Texas MD Anderson Cancer Center

100 Clinical Results associated with Hydrocodone bitartrate

100 Translational Medicine associated with Hydrocodone bitartrate

100 Patents (Medical) associated with Hydrocodone bitartrate

1,619

Literatures (Medical) associated with Hydrocodone bitartrate

01 Jul 2025·Phytomedicine

Integrated network pharmacology, metabolomics, and microbiome studies to reveal the therapeutic effects of Anacyclus pyrethrum in PD–MCI mice

Article

Author: Shataer, Samire ; Wu, Qin Fen ; Ma, Liang Ying ; Shan Li, Pei ; Chen, Yan ; Tuersong, Tayier ; Shataer, Munire ; Yong, Yu Xuan ; Yang, Xin Ling

BACKGROUNDAnacyclus pyrethrum (l.) DC has potential value in treating Parkinson's disease (PD)-mild cognitive impairment (MCI), manifesting as impaired memory, attention, executive function, and language. However, the specific targets and modes of action of A. pyrethrum remain unclear.PURPOSEThe aim of this study was to identify the active components of A. pyrethrum and examine their effectiveness in treating a mouse model of PD-MCI.METHODSWe generated ethanol extracts of A. pyrethrum root (EEAP) and identified its active components and related targets using UHPLC-MS/MS and network pharmacology.The PD-MCI model was induced via intraperitoneal administration of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine(MPTP). After following continuous administration of EEAP,Altered learning or memory, as well as anxiety, were tested using the morris water maze, eight-arm radial arm maze (RAM), and open-field test,elevated plus-maze. Brain histopathology and ultrastructural changes were examined using brightfield microscopy, and electron microscopy, respectively. Furthermore, protein expression was assessed using western blotting.Stool samples were used for metabolomics analysis by UHPLC-MS/MS and for 16S rDNA sequencing to determine the compositional changes of the gut microbiota.We conducted a short-chain fatty acid targeted metabolomics experiment to study their role in the gut-brain axis in PD-MCI.RESULTSUsing UPLC-MS-MS, 126 compounds were identified from A. pyrethrum samples.After searching the databases and literature reports, 31 active components and 544 drug-disease targets were screened. Biological processes and molecular functions, such as energy channels, cell signaling, and metabolism, were discovered through GO analysis. The water maze experiment showed that the average swimming distance and escape latency of mice in EEAP groups decreased. The eight-arm maze experiment showed that model had a much higher number of errors related to working memory than the control mice. In the open field experiment, compared with the control group, the mice in the EEAP group exhibited an increase in the average movement speed and total movement distance, along with a decrease in the residence time.In the elevated plus maze, the control had less anxiety than the Model. Donepezil/Levodopa(D/l) mitigated anxiety-like behavior, and EEAP (100-400 mg/kg) showed a dose-dependent increase in open-arm metrics, suggesting it may ease anxiety in mice.Hippocampal tissue of mice treated with different doses of EEAP showed intact cellular layers and the hematoxylin-eosin-stained cones were slightly better;cells were arranged neatly; their morphology was normal, and were distributed uniformly. Electron microscopy revealed that the nuclear membrane, chromatin, and nucleoli were clearly demarcated in the hippocampus of mice treated with different doses of EEAP, contrary to that in the model group. In brain extracts of the EEAP group, lighter thinner bands for amyloid precursor protein (APP) and Aβ were observed compared to those in the model group. In model mice, APP and Aβ protein expression was higher than in the blank group, as shown by stronger bands. In EEAP-treated mice, the bands were weaker, indicating reduced expression. In the model group had lower Bcl-2 and higher Bax levels. EEAP treatment increased Bcl-2 and decreased Bax expression.Compared to the control group, the model showed substantially low glutathione peroxidase (GSH-Px),superoxide dismutase(SOD),catalase (CAT)activity (p < 0.05),much higher (p < 0.05) in the EEAP-H group than that in the model. EEAP intervention significantly modulated the fecal metabolic profile of PD-MCI mice. The abundance of steroid and lipid metabolites, including linoleylethanolamine, was markedly altered in the model group compared to the control group, with EEAP treatment reversing several of these abnormalities. PLS-DA and OPLS-DA revealed significant separation between groups (Q2= 0.542, p < 0.01), confirming a dose-dependent effect. Random forest analysis identified 15 key metabolic markers, such as dose-dependent changes in d-glutamine and hydrocodone. Metabolic pathway analysis demonstrated significant enrichment in phenylalanine, tyrosine, tryptophan metabolism, and arginine biosynthesis pathways (p < 0.05). The Support Vector Machine (SVM) model achieved an AUC approaching 1, indicating substantial differences in metabolite profiles. EEAP intervention significantly influenced the composition and functional profile of the intestinal microbiota. The Venn diagram illustrates that each group shared 342 operational taxonomic units (OTUs), with the EEAP 400 group exhibiting a distinct Bacteroidetes proportion. LEfSe analysis identified g_Prevotella as the characteristic bacterium in the control group, c_Epsilonproteobacteria in the model group, and g_Adlercreutzia in the EEAP 100 group. The Faith's Phylogenetic Diversity (PD) index was highest in the EEAP 100 group, and Non-metric Multidimensional Scaling (NMDS)/Principal Coordinates Analysis (PCoA) revealed significant differences in microbial community structure. Short-chain fatty acids (SCFAs) analysis indicated that acetic acid was the predominant metabolite, while EEAP dose-dependently regulated propionic acid and isovaleric acid levels (VIP > 1, p < 0.001). These findings demonstrate that EEAP exerts its regulatory effects by reshaping the structure and metabolic functions of the gut microbiota.CONCLUSIONEEAP holds great promise as a potential therapeutic agent for PD-MCI, exerting its effects through multiple mechanisms, including regulating protein expression, modulating the fecal metabolic profile, and reshaping the gut microbiota and its metabolites.

08 Apr 2025·Psychopharmacology bulletin

Trends in Outpatient Buprenorphine Prescribing for Chronic Pain: A Retrospective Analysis Over 18 Months.

Article

Author: Hasoon, Jamal ; Viswanath, Omar ; Varrassi, Giustino ; Urits, Ivan ; Imani, Farnad ; Chitneni, Ahish

BackgroundBuprenorphine, a partial opioid agonist, has gained attention for its use in chronic pain management due to its lower risk of abuse and respiratory depression compared to traditional opioids. The utilization of buprenorphine for chronic pain has increased in recent years. This study aimed to analyze trends in buprenorphine prescribing for chronic pain in an outpatient setting over an 18-month period, excluding buprenorphine-naloxone combinations used for opioid use disorder and opioid dependence.MethodsA retrospective chart review was conducted, examining outpatient buprenorphine and long-acting opioid prescriptions issued by three pain management physicians between January 1, 2023, and June 30, 2024. Prescription data were collected from electronic medical records (EMRs) and analyzed across three six-month intervals: January 1, 2023, to June 30, 2023; July 1, 2023, to December 31, 2023; and January 1, 2024, to June 30, 2024. Only unique buprenorphine prescriptions for chronic pain management were included, while buprenorphine-naloxone prescriptions for opioid use disorder were excluded. Long-acting opioids analyzed included extended release (ER) formulations including tramadol ER, morphine ER, hydrocodone ER, oxycodone ER, fentanyl, and methadone.ResultsOver the 18-month study period, a total of 61 unique buprenorphine prescriptions for chronic pain were issued by the three physicians. The number of prescriptions increased across each six-month period: 18 prescriptions were issued between January 1, 2023, and June 30, 2023; 20 prescriptions from July 1, 2023, to December 31, 2023; and 23 prescriptions from January 1, 2024, to June 30, 2024. This represents a 27.8% increase over the entire 18-month period. During the same timeframe, 117 long-acting opioid prescriptions (excluding buprenorphine) were issued in the first six-month period, 121 prescriptions in the second period, and 108 prescriptions in the third period. Buprenorphine prescriptions accounted for 13.3% of all long-acting opioid prescriptions in the first period (18 out of 135 total prescriptions), 14.2% in the second period (20 out of 141 total prescriptions), and 17.6% in the third period (23 out of 131 total prescriptions). Notably, while the absolute number of buprenorphine prescriptions increased steadily, its proportion relative to total long-acting opioid prescriptions also grew over time.ConclusionsThe findings demonstrate a steady increase in buprenorphine prescribing for chronic pain in the outpatient setting, while long-acting opioid prescriptions exhibited a slight decline in the later periods. The proportion of buprenorphine prescriptions relative to long-acting opioids increased over time, suggesting growing acceptance of buprenorphine as a safer alternative for chronic pain management. Further research is needed to explore the factors driving these prescribing patterns and the long-term clinical outcomes associated with buprenorphine use in chronic pain management.

03 Apr 2025·Drug Metabolism and Personalized Therapy

Prolonged post-operative hydrocodone usage due to psychotropic drug interaction

Article

Author: Malkani, Arthur L. ; Roach, Abbey R. ; Yakkanti, Madhusudhan R. ; Jortani, Saeed A. ; Renfrow, Ruby E. ; Karimi, Viana F. ; Gaskins, Jeremy T. ; Hartley, Brandi ; Whitt, Aaron G.

AbstractObjectivesTo explore pain outcomes in patients prescribed hydrocodone and psychotropic medications with or without CYP2D6 inhibition activity.MethodsPatients hospitalized for lower/limited upper extremity injuries who were prescribed hydrocodone alongside a psychotropic medication were considered for this study (n=224). A subset of these patients (n=178) was prescribed a psychotropic medication known to inhibit CYP2D6, while the remainder (n=46) were prescribed psychotropic medications without CYP2D6 inhibition activity. Patient demographics and pain outcomes were collected by electronic health record review and interviews.ResultsPatients taking a psychotropic inhibitor of CYP2D6 exhibited longer duration of opioid use post-discharge (median 33 days [IQR 10–99]) compared with patients taking a psychotropic non-inhibitor (4 days [2–20], p<0.001). No significant differences were observed with in-hospital pain outcomes, including total dose of hydrocodone administered, duration of hydrocodone use, pain index scores, and the occurrence of common mild/moderate/severe hydrocodone side effects.ConclusionsPatients prescribed at least one psychotropic inhibitor of CYP2D6 were more likely to continue using hydrocodone for up to 3 months following surgery. Knowledge of these critical drug-drug interactions could enhance clinical practice and improve patient outcomes. This study highlights negative post-operative pain outcomes in patients prescribed hydrocodone alongside a psychotropic inhibitor of CYP2D6. The results of this study indicate that patients taking psychotropic medications that inhibit CYP2D6 are at increased risk for prolonged hydrocodone use following orthopedic surgery.

News (Medical) associated with Hydrocodone bitartrate

10 Apr 2025

·www.prnewswire.com

Newborn Brains Are Smaller When Exposed to Opioids During Gestation

An important "first dive" into data from the 4-site Outcomes of Babies with Opioid Exposure (OBOE) study features a Cincinnati Children's expert as co-first author CINCINNATI, April 10, 2025 /PRNewswire/ -- When pregnant women take opioids during pregnancy, even opioids such as buprenorphine or methadone to treat opioid use disorder, the developing brains of their children can be significantly affected, according to a study published April 7, 2025, in JAMA Pediatrics. Continue Reading Antenatal opioid exposure is associated with smaller neonatal brain volumes, with varying impact depending on the type and number of exposures, according to research published in JAMA Pediatrics. Stephanie Merhar, MD, MS, at Cincinnati Children's was first co-author. Total brain volume was nearly 5% smaller among 173 newborns with antenatal opioid exposure compared to 96 unexposed newborns, based on magnetic resonance imaging (MRI) scans. More specifically, reduced volumes among opioid-exposed newborns occurred in cortical gray matter, deep gray matter, white matter, cerebellum, brainstem, and the right and left amygdala. There were notable differences in the location and scale of the effects, which varied depending on the type of opioid involved, and whether other drugs were also taken during pregnancy. "We have known for a while that children exposed to opioids during pregnancy are at risk of later developmental and behavioral problems, but it was hard to know whether that was due to the opioids themselves or other factors such as other exposures or lower birth weight," says co-first author Stephanie Merhar, MD, MS, a neonatologist at Cincinnati Children's. "This study was launched because we needed a large study where we were able to control for things like nicotine exposure and birth weight. Our next step is to follow the children in the study to see whether having smaller brain volumes in the newborn period affects later development and behavior." The double-threat opioids pose to mothers and children Nearly 1 in 12 newborns in the United States in 2020 – or about 300,000 infants – were exposed to alcohol, opioids, marijuana or cocaine before they were born, according to the Substance Abuse and Mental Health Services Administration (SAMHSA). Prenatal substance exposure in rural areas often exceeds overall national averages. Opioids include illegal drugs like heroin and fentanyl, prescription drugs like oxycodone and hydrocodone, and medications for opioid use disorder like buprenorphine and methadone. Opioid use often goes hand in hand with smoking and use of other substances such as alcohol and marijuana. This study compared newborns born to mothers who took opioids only and newborns born to mothers who used other substances as well as opioids. Newborns exposed to opioids plus other substances had smaller brain volumes in more regions compared to those exposed to opioids only. The most common opioids among participants in the new study were buprenorphine (68.8%) and methadone (26%). Both of these opioids are routinely used to treat opioid use disorder (OUD) and are both recommended for treatment of OUD during pregnancy by the American College of Obstetricians and Gynecologists. "We know that buprenorphine and methadone are life-saving medications for women with OUD," Merhar says. "We don't want to imply that women with OUD should wean off these medications, but we agree with the ACOG recommendation for more research on medically supervised withdrawal in pregnant women." The study was praised in an accompanying editorial penned by Nethra Madurai, MD, and Lauren Jantzie, PhD, both of Johns Hopkins University School of Medicine. Other small studies have shown fetal brain changes caused by opioids. But this multi-center study is the first to be large enough to convincingly distinguish effects linked to opioids versus confounding factors such as maternal smoking, birth weight, education levels. The study authors "present compelling evidence of the direct effects of opioids on the developing brain," the editorial states. "Given the prospective design of the trial, they account for other postnatal factors…allowing us to dispel previous uncertainty surrounding the direct impacts of opioids on the brain vs the confounding effects of other environmental factors." What's next? Having more precise information about the affected parts of the brain could allow scientists to focus on interventions to support healthy brain development for children born after opioid exposure. "Indeed, we must shift our focus beyond the initial withdrawal symptoms associated with POE [prenatal opioid exposure] if we are to improve the lifelong health and well-being of infants and children impacted by the opioid epidemic," the editorial states. Read more about Merhar's research related to opioid exposure: 'Eat, Sleep, Console' Approach Slashes ICU Stays for Opioid-Exposed Newborns In Utero Opioid Exposure Impacts Fetal Brain Size and Development $8M Grant Funds Long-Term Opioid Exposure Study SOURCE Cincinnati Children's Hospital Medical Center WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

07 Apr 2025

·www.prnewswire.com

Elysium Therapeutics Announces Development of Overdose Rescue Technology Specifically Designed for Oral Fentanyl

Synthetic Opioid Overdose Prevention and Reversal (SOOPR™) targets an unmet challenge in the illicit opioid crisis as current rescue medications are not designed for synthetic opioids, including oral fentanyl. LYONS, Colo., April 7, 2025 /PRNewswire/ -- Elysium Therapeutics, an emerging biopharmaceutical company developing treatments specifically designed to rescue and reverse overdoses caused by oral opioids, including synthetic opioids like fentanyl, announced its plan to accelerate development of its Synthetic Opioid Overdose Prevention and Reversal (SOOPR™) technology. The company has completed in vivo proof-of-concept studies and expects to file an Investigational New Drug (IND) application in 2026. SOOPR is a rapid-onset, long-acting rescue agent specifically designed to address overdose from synthetic opioids, including oral fentanyl. SOOPR utilizes a proprietary long-acting naloxone prodrug formulation with faster onset kinetics versus Narcan® delivered via long-acting injection (LAI) technology. The technology is designed to rapidly restore respiration and provide 18 to 24 hours of effective opioid blockade to minimize the risk of re-narcotization, while also providing protection from same-day re-use of opioids. "Fentanyl overdoses often require very high, or repeated, doses of short-acting opioid antagonists to effect a successful rescue," said Greg Sturmer, Co-Founder and CEO of Elysium Therapeutics. "Unfortunately, many who overdose face a rapid recurrence of symptoms, known as re-narcotization, which can lead to respiratory depression and increase the likelihood of hypoxic brain injury or death. SOOPR is designed to address this situation, and Elysium is now focused on advancing its development as a potential first-ever, faster-onset, longer-acting opioid rescue therapy specifically intended to treat fentanyl overdose." Currently approved short-acting opioid antagonists like Narcan and Opvee® were designed to effectively counteract overdoses from opioids such as heroin and oxycodone. However, these rescue agents are frequently ineffective in the management of synthetic opioid overdoses1, with 20 to 45% of overdose victims initially rescued with naloxone experiencing a re-narcotization event. According to reports from multiple state-affiliated health agencies, 31 to 39% of fentanyl overdose decedents had been administered naloxone.2 Data from in vivo proof-of-concept studies of SOOPR demonstrated a more rapid onset of action versus naloxone (Narcan) and a significantly longer duration of action. This profile is especially useful in counteracting oral fentanyl overdoses associated with prolonged fentanyl absorption and exposure that often outlast the short-acting profile of Narcan. "In designing SOOPR, Elysium recognized that synthetic opioids – now the number one killer of adults aged 18 to 45 in the U.S. – are particularly lethal," said Tom Jenkins, Ph.D., Co-Founder and Chief Scientific Officer of Elysium Therapeutics. "Patients initially treated with a rapid-acting, long-duration reversal agent, such as SOOPR, are expected to have less risk of hypoxic brain injury, cardiovascular events, re-narcotization, and death. Further, rescue interventions with SOOPR are expected to require less intensive monitoring in both the ambulance and emergency department and increase the likelihood of survival. Additionally, SOOPR is designed to be delivered by intramuscular injection, either using a pre-filled syringe or autoinjector, which has been demonstrated to be more rapid and predictable than intranasal delivery in urgent settings, where every second counts." "In addition to preventing overdose deaths from recreational, illicit use, the Department of Defense (DOD) has made clear the importance of improving opioid overdose rescue as a needed medical countermeasure," added Sturmer. "The DOD reported that the availability of synthetic opioids, such as fentanyl and its derivatives, represents a significant threat as a chemical weapon, which could be easily disseminated as a weapon of mass destruction into air, water or food supplies, putting countless lives at risk. We look forward to working with defense and government organizations as we develop SOOPR as a tool to prevent injury and death in these worrisome scenarios." About SOOPR™ (Synthetic Opioid Overdose Prevention and Rescue) SOOPR (Synthetic Opioid Overdose Prevention and Reversal) is a rapid-onset, long-acting rescue agent specifically designed to address overdose from synthetic opioids, including oral fentanyl. SOOPR utilizes a proprietary long-acting naloxone reversal formulation with faster onset kinetics versus Narcan® delivered via long-acting injection (LAI) technology. The technology is designed to rapidly restore respiration and provide 18 – 24 hours of effective opioid blockade to minimize the risk of re-narcotization, while also providing protection from same-day re-use of opioids. SOOPR has been endorsed by first responders and OUD treatment professionals as the effective solution urgently needed to address the global opioid overdose epidemic. About Elysium Therapeutics Elysium is an emerging biopharmaceutical company developing treatments specifically designed to rescue and reverse overdoses caused by oral synthetic opioids, including fentanyl. Elysium is working to establish 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 technology, SOOPR™ (Synthetic Opioid Overdose Prevention and Reversal), is 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. In addition, Elysium is developing oral-overdose protected (O2P™) hydrocodone for the treatment of moderate-to-severe acute pain. For more information, please visit . 1 Rachael Rzasa Lynn and JL Galinkin Ther Adv Drug Saf 2018, Vol. 9(1) 63–88 (Also see footnotes 8, 9, and 10 for additional discussion). 2 Watson, W.A., Steele, M.T., Muelleman, R.L., Rush, M.D., 1998. Opioid toxicity recurrence after an initial response to naloxone. J. Toxicol. Clin. Toxicol. 36 (1-2), 11–17. . SOURCE Elysium Therapeutics WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug Approval

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 Hydrocodone bitartrate

External Link

KEGG	Wiki	ATC	Drug Bank
-	Hydrocodone bitartrate	R05DA03	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Pain	United States	Purdue Pharma LP	20 Nov 2014

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Pain	Phase 1	United States	Societal CDMO Gainesville LLC	25 Oct 2013
Drug abuse	Discovery	United States	Cephalon, Inc.	01 Mar 2012
Drug abuse	Discovery	Canada	Cephalon, Inc.	01 Mar 2012
Kidney Failure, Chronic	Discovery	United States	Cephalon, Inc.	01 Mar 2011
Osteoarthritis	Discovery	United States	Teva Branded Pharmaceutical Products R&D, Inc.	01 Nov 2010
Chronic Pain	Discovery	United States	Zogenix, Inc.	01 May 2010
Low Back Pain	Discovery	United States	Zogenix, Inc.	01 Mar 2010
Chronic osteoarthritis	Discovery	-	Zogenix, Inc.	01 Sep 2002

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03642873 (CTgov)	Phase 1	-	24	Humibid® (Treatment A)	mwegfpujxz(gvqezgltuv) = vxolsuvbjv uooqgexdtt (yztxjxbrpy, lptwyjwxjw - igrwyukauu) View more	-	20 Jun 2019
				Hydrocodone Bitartrate (Treatment B)	mwegfpujxz(gvqezgltuv) = wmeefuufmf uooqgexdtt (yztxjxbrpy, tlimfojgix - qjoebztssb) View more
NCT01402375 (CTgov)	Phase 3	Acute Pain \| Limb injury	720	Hydrocodone (first trial) (Hydrocodone (First Trial))	wvksnfumks(vdnjqlatvr) = aqlqzepmuj zknqorctlh (iojvqddzap, imwfzkibmo - ruxiotyekw) View more	-	01 May 2018
				Codeine (first trial) (Codeine (First Trial))	wvksnfumks(vdnjqlatvr) = aftqxxnjcm zknqorctlh (iojvqddzap, vtifdczyjw - gtvhjvtaar) View more
NCT01240863 (CTgov)	Phase 3	Low Back Pain \| Osteoarthritis \| Chronic Pain	391	Placebo (Placebo (Double-blind Treatment Period))	dlbsfvdlnd(ywjoaxdowl) = eichtozgdi warnfounbv (vypiqdqezu, shvpcuachy - enuzcjwwdg) View more	-	05 Jun 2017
				Hydrocodone ER (Hydrocodone ER (Double-blind Treatment Period))	dlbsfvdlnd(ywjoaxdowl) = guidgcotup warnfounbv (vypiqdqezu, fvfruaxkdv - jpjrfxtcqv) View more
NCT01922739 (CTgov)	Phase 3	Low Back Pain	182	Placebo+Hydrocodone ER	(rjzelxkztc) = muoluwrdtk kailbqyuvj (vuchxyvikt, zoblgvcohq - uflfksmfqc) View more	-	02 Jun 2017
NCT01789970 (CTgov)	Phase 3	Low Back Pain	625	Placebo (Placebo (Double-blind Treatment Period))	gmyvmetlkt(njdcytachx) = jlwitpiyyk jnnpgwatek (xtryxtlnau, uoycjpvtqb - jpbdlucarw) View more	-	05 Apr 2017
				Hydrocodone ER (Hydrocodone ER (Double-blind Treatment Period))	gmyvmetlkt(njdcytachx) = rwpdyzwbtg jnnpgwatek (xtryxtlnau, xcqgswtkho - vqoyibvswo) View more
NCT01517295 (CTgov)	Phase 4	Chronic Pain	30	Hydrocodone (Group 1)	kpvkkacwwl(rfgosinqhm) = qolkxavdxc meedyhygsk (tobrwbxlfh, ugrhzrgwuj - uwplklxcgq) View more	-	28 Jul 2016
				Hydrocodone (Group 2)	kpvkkacwwl(rfgosinqhm) = thbqtpgtkd meedyhygsk (tobrwbxlfh, opncjjdxlz - acihgfkoqd) View more
NCT01859715 (CTgov)	Not Applicable	Medication interactions	502	Oxycodone (Oxycodone Group)	okbygkfxbf(jkihchkjpz) = ikivtwdkuu otqueaepip (asyczstxop, rkawpvcdem - botvgesjiv) View more	-	05 May 2016
				Hydrocodone (Hydrocodone/Acetaminophen Group)	okbygkfxbf(jkihchkjpz) = isjoddhvss otqueaepip (asyczstxop, jgxyenvkui - ebwmperjqw) View more
NCT01452529 (CTgov)	Phase 3	Low Back Pain	905	Hydrocodone bitartrate q24h film-coated tablets (Hydrocodone Bitartrate)	unoqtpomcn(uytilzputi) = pkzlprzhll fafaiedidh (ioltvzvhhe, rfszkilokz - kxdgiculad) View more	-	04 Dec 2014
				Placebo to match hydrocodone bitartrate q24h tablets (Placebo)	unoqtpomcn(uytilzputi) = shtbsotztc fafaiedidh (ioltvzvhhe, gcrlvpxkwn - kmzmcgjulx) View more
NCT01400139 (CTgov)	Phase 3	Chronic Pain	922	Hydrocodone bitartrate (HYD)+Hydrocodone bitartrate (HYD Core Study)	(eiadavbyhh) = skkzjpgmwj lucqjsjewt (iuietsxyrp, ghrtpxsvgx - mplrbuuqsb) View more	-	04 Dec 2014
				Hydrocodone bitartrate (HYD)+Hydrocodone bitartrate (HYD Extension Period)	(eiadavbyhh) = cgvzlxnalg lucqjsjewt (iuietsxyrp, qvfhxosuhl - gwyeigknpx) View more
NCT01115569 (CTgov)	Phase 3	Chronic Pain	424	Hydrocodone Bitartrate (Open-label Hydrocodone Bitartrate Extended Release Capsules)	reniedfgbm(fuqzghqnof) = uloprbstko mkooilimfu (khxyeftsmn, zidzzpsqxa - tlgesompaa)	-	25 Apr 2014
				Hydrocodone Bitartrate Extended Release (HC-ER)+Hydrocodone Bitartrate (Conversion/Titration Phase)	lichielmln(mvptqfxwec) = rntuuzgxpa aoktxwcdpe (dhzkvnxpds, olcbrohxth - mteamqdqzx) View more

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