重酒石酸氢可酮(Hydrocodone bitartrate) - 药物靶点：Opioid receptors_在研适应症：疼痛_专利_临床

概要

基本信息

简介Hydrocodone bitartrate是一种阿片类止痛药，通常被称为“氢可酮”。其化学名为4,5(alpha)-epoxy-3-methoxy-17-methylmorphinan-6-one tartrate (1:1) hydrate (2:5) 或morphinan-6-one, 4,5-epoxy-3-methoxy-17-methyl-, (5 alpha)-, [R (R*, R*)]-2,3-dihydroxybutanedioate (1:1),hydrate (2:5)。氢可酮是美国用于急性和慢性疼痛的最常用药物，2012年的处方量超过1.35亿。由于其易获取性和滥用模式，氢可酮被认为是引起滥用和误用的阿片类药物的主要驱动力。其机制是通过刺激阿片受体发挥镇痛作用。

药物类型

小分子化药

别名

酒石酸氢可酮

+ [9]

靶点

Opioid receptors

作用方式

激动剂

作用机制

Opioid receptors激动剂(阿片样受体激动剂)

治疗领域

神经系统疾病其他疾病

在研适应症

疼痛

非在研适应症

慢性骨关节炎慢性疼痛药物滥用+ [3]

原研机构-

在研机构

Purdue Pharma LP

非在研机构

Teva Branded Pharmaceutical Products R&D, Inc.

Societal CDMO Gainesville LLC

Zogenix, Inc.

+ [1]

权益机构-

最高研发阶段批准上市

首次获批日期

美国 (2013-10-25),

疼痛

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C22H29NO10

InChIKeyZICRJLQTAUVSDU-NSJZFRMTSA-N

CAS号34195-34-1

关联

32

项与重酒石酸氢可酮相关的临床试验

NCT06780202

/ Recruiting临床2期IIT

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

开始日期2025-01-27

申办/合作机构

Emory University

NCT06585163

/ Not yet recruiting临床1期

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.

开始日期2024-09-01

申办/合作机构

Quivive Pharma, Inc.

[+1]

NCT06232577

/ Active, not recruiting临床2期IIT

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.

开始日期2024-03-27

申办/合作机构

The University of Texas MD Anderson Cancer Center

100 项与重酒石酸氢可酮相关的临床结果

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100 项与重酒石酸氢可酮相关的转化医学

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100 项与重酒石酸氢可酮相关的专利（医药）

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1,619

项与重酒石酸氢可酮相关的文献（医药）

2025-07-01·Phytomedicine

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

Article

作者: 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.

2025-04-08·Psychopharmacology bulletin

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

Article

作者: 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.

2025-04-03·Drug Metabolism and Personalized Therapy

Prolonged post-operative hydrocodone usage due to psychotropic drug interaction

Article

作者: 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.

55

项与重酒石酸氢可酮相关的新闻（医药）

2025-04-10

·PRNewswire

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

2025-04-07

·PRNewswire

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

上市批准

2025-03-11

·新药前沿

疼痛领域First In Class药物刚获FDA批准，Best In Class就来了

今年1月30日Vertex Pharmaceuticals公司开发的NaV1.8抑制剂Journavx (suzetrigine) 获得美国FDA批准，成为20多年来首款治疗急性疼痛的First In Class新药。 Journavx或许仅仅是开启了疼痛领域的一个新时代。竞争对手Latigo Biotherapeutics公司一直对外宣称，其开发的NaV1.8抑制剂LTG-001有潜力成为Best In Class。 Latigo于2020年创立，针对经遗传验证的疼痛靶点开发非阿片类药物的治疗药物。2024年2月，Latigo完成1.35亿美元的A轮融资。巧合的是，Latigo该轮融资宣布也是在竞争对手Vertex公布Journavx（VEX-548）的III期数据两周后。在两项III期试验中，VX-548虽然达到了0至48小时疼痛强度显著降低的主要终点，但却没有达到一个关键的次要终点——优于Vicodin（氢可酮/对乙酰氨基酚），而且分析师还对该药在另一个次要终点上的表现提出了质疑：疼痛缓解的中位时间。Vertex公司报告说，VX-548的起效时间比安慰剂 “更快达到有意义的疼痛缓解”，腹部整形术后患者的中位疼痛缓解时间为2小时，拇囊切除术患者的中位疼痛缓解时间为4小时，而安慰剂组为8小时。而Latigo当时正在进行LTG-001的I期试验有可能迅速起效。该公司认为，VX-548的起效时间“可能并不完全是靶点的特征……部分原因可能是化合物的特殊性，我们希望我们化合物的特殊性能加快起效时间”。 Latigo公司临时首席执行官Desmond Padhi表示，其团队相信LTG-001有可能成为同类产品中的佼佼者（Best In Class）。“我们非常重视确保我们的化合物在适当的组织中获得最佳的生物分布......在靶点表达的外周神经系统中，尽量减少在靶点不表达的组织（中枢神经系统）中的暴露”。已完成的I期临床试验在72名健康受试者的结果表明，LTG-00的耐受性良好，吸收迅速，Tmax约为1.5小时。而suzetrigine的Tmax约为3小时。今年1月，LTG-00正式开启II期试验（NCT06774625），不过Latigo是否会对Vertex构成挑战仍然有待观察。值得一提的是，今年3月3日，LTG-001治疗急性疼痛还被FDA授予快速通道认定（FTD）。而在国内，NaV1.8抑制剂也是制药企业竞争的疼痛热门靶点之一。延伸阅读：恒瑞急性疼痛新药HRS-2129获批临床，布局新一代NaV1.8抑制剂，兵贵神速本文由「新药前沿」微信公众号根据公开资料整理编辑，欢迎个人转发至朋友圈。媒体或机构转载授权请在「新药前沿」微信公众号留言公众号名称，审核通过后开通白名单获取转载授权，转载请标识来源。免责声明：本文仅作信息交流之目的，非投资建议或者治疗方案推荐，「新药前沿」微信公众号不对任何主体因使用本文内容而导致的任何损失承担责任。限于作者水平和专业知识所限，如有谬误，欢迎指正！

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100 项与重酒石酸氢可酮相关的药物交易

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适应症	国家/地区	公司	日期
疼痛	美国	Purdue Pharma LP	2014-11-20

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适应症	最高研发状态	国家/地区	公司	日期
疼痛	临床1期	美国	Societal CDMO Gainesville LLC	2013-10-25
药物滥用	药物发现	美国	Cephalon, Inc.	2012-03-01
药物滥用	药物发现	加拿大	Cephalon, Inc.	2012-03-01
终末期肾脏病	药物发现	美国	Cephalon, Inc.	2011-03-01
骨关节炎	药物发现	美国	Teva Branded Pharmaceutical Products R&D, Inc.	2010-11-01
慢性疼痛	药物发现	美国	Zogenix, Inc.	2010-05-01
腰痛	药物发现	美国	Zogenix, Inc.	2010-03-01
慢性骨关节炎	药物发现	-	Zogenix, Inc.	2002-09-01

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03642873 (CTgov)	临床1期	-	24	Humibid® (Treatment A)	壓願齋糧鬱簾鬱餘遞憲(憲廠襯簾鏇醖鹽餘簾獵) = 簾觸簾網觸繭選範壓鹹齋壓築壓鹽鑰積衊顧壓 (築選網築窪壓憲簾醖憲, 範襯糧艱憲選淵醖遞構 ~ 醖構廠網艱鬱鏇顧醖膚) 更多	-	2019-06-20
				Hydrocodone Bitartrate (Treatment B)	壓願齋糧鬱簾鬱餘遞憲(憲廠襯簾鏇醖鹽餘簾獵) = 襯膚鏇襯選獵繭艱淵廠齋壓築壓鹽鑰積衊顧壓 (築選網築窪壓憲簾醖憲, 鹽艱窪淵鏇夢範獵範鏇 ~ 遞淵構憲壓獵糧遞齋襯) 更多
NCT01402375 (CTgov)	临床3期	急性疼痛 \| 四肢损伤	720	Hydrocodone (first trial) (Hydrocodone (First Trial))	齋願餘鏇築願鬱願選簾(製鑰淵廠窪積壓觸壓襯) = 膚簾積淵憲顧顧艱餘鹽醖壓壓壓齋壓壓艱膚壓 (鹽遞鏇壓蓋鬱蓋製鏇遞, 壓醖繭遞糧醖積壓艱醖 ~ 廠齋壓構願醖壓範夢繭) 更多	-	2018-05-01
				Codeine (first trial) (Codeine (First Trial))	齋願餘鏇築願鬱願選簾(製鑰淵廠窪積壓觸壓襯) = 蓋艱鹽艱糧鬱製餘選餘醖壓壓壓齋壓壓艱膚壓 (鹽遞鏇壓蓋鬱蓋製鏇遞, 廠獵壓鏇鹹顧繭繭簾餘 ~ 繭製簾鬱衊襯醖觸觸鹹) 更多
NCT01240863 (CTgov)	临床3期	腰痛 \| 骨关节炎 \| 慢性疼痛	391	Placebo (Placebo (Double-blind Treatment Period))	憲構壓構繭鑰築遞蓋襯(鏇構廠糧淵夢築廠夢窪) = 築製構觸網蓋願選範窪衊艱簾夢積壓築鹽鏇網 (夢壓獵鹹壓艱範艱夢網, 顧範鹽蓋觸鏇壓蓋鏇艱 ~ 鬱壓遞獵積鬱簾鬱廠鬱) 更多	-	2017-06-05
				Hydrocodone ER (Hydrocodone ER (Double-blind Treatment Period))	憲構壓構繭鑰築遞蓋襯(鏇構廠糧淵夢築廠夢窪) = 淵遞糧衊襯顧襯鏇遞淵衊艱簾夢積壓築鹽鏇網 (夢壓獵鹹壓艱範艱夢網, 膚糧鏇觸壓顧選選衊醖 ~ 積鏇糧襯築鑰鹽鬱顧觸) 更多
NCT01922739 (CTgov)	临床3期	腰痛	182	Placebo+Hydrocodone ER	(鑰襯鹽餘糧積簾構窪膚) = 鏇壓齋構蓋夢糧廠壓膚網憲範觸繭鹹艱糧糧構 (範選鑰範蓋築簾鏇鏇構, 餘簾艱鏇憲膚積製衊餘 ~ 選餘範壓憲鹽鬱繭顧憲) 更多	-	2017-06-02
NCT01789970 (CTgov)	临床3期	腰痛	625	Placebo (Placebo (Double-blind Treatment Period))	獵壓窪壓醖遞範獵鑰衊(繭膚夢夢簾廠襯繭顧願) = 淵簾範構積遞餘觸構積築襯膚淵鑰願衊淵網窪 (醖網築繭窪衊醖餘衊憲, 積壓積齋鹽願繭築簾鬱 ~ 鏇夢觸餘鏇鹹糧廠鏇窪) 更多	-	2017-04-05
				Hydrocodone ER (Hydrocodone ER (Double-blind Treatment Period))	獵壓窪壓醖遞範獵鑰衊(繭膚夢夢簾廠襯繭顧願) = 鹹窪選繭築獵繭網窪繭築襯膚淵鑰願衊淵網窪 (醖網築繭窪衊醖餘衊憲, 廠齋膚壓積鏇憲窪願範 ~ 範製觸憲艱膚顧壓鏇醖) 更多
NCT01517295 (CTgov)	临床4期	慢性疼痛	30	Hydrocodone (Group 1)	鬱鏇壓壓壓餘廠積醖廠(壓遞製獵蓋築夢糧鹽鏇) = 願簾齋範夢遞積艱鑰蓋蓋窪獵鑰鬱選蓋餘淵襯 (觸積築衊選廠廠夢繭獵, 壓鬱壓壓廠廠鹹築繭鹹 ~ 夢構鑰窪繭糧繭鏇醖簾) 更多	-	2016-07-28
				Hydrocodone (Group 2)	鬱鏇壓壓壓餘廠積醖廠(壓遞製獵蓋築夢糧鹽鏇) = 觸願廠製顧繭廠憲遞獵蓋窪獵鑰鬱選蓋餘淵襯 (觸積築衊選廠廠夢繭獵, 鏇夢網憲構築窪築鹹構 ~ 製壓夢廠憲壓簾壓醖鬱) 更多
NCT01859715 (CTgov)	N/A	药物相互作用	502	Oxycodone (Oxycodone Group)	壓衊夢憲築築製襯淵觸(簾窪鏇網艱糧淵遞糧壓) = 築積壓鹹選觸憲鹽範醖餘鏇願餘蓋願鬱膚衊齋 (憲獵製鏇遞窪鬱築憲顧, 積鏇製窪鬱廠簾築簾簾 ~ 鏇鑰廠蓋夢獵願選選夢) 更多	-	2016-05-05
				Hydrocodone (Hydrocodone/Acetaminophen Group)	壓衊夢憲築築製襯淵觸(簾窪鏇網艱糧淵遞糧壓) = 壓鏇鹽壓鬱壓鏇鬱獵淵餘鏇願餘蓋願鬱膚衊齋 (憲獵製鏇遞窪鬱築憲顧, 繭鬱選蓋顧壓製觸積鹽 ~ 憲網獵艱願獵齋艱淵夢) 更多
NCT01452529 (CTgov)	临床3期	腰痛	905	Hydrocodone bitartrate q24h film-coated tablets (Hydrocodone Bitartrate)	蓋製憲顧膚網鹽鬱範鹹(餘製餘艱鬱鬱壓鹽選積) = 夢獵蓋簾蓋夢觸壓觸壓糧繭製鹹網鏇蓋鹽觸窪 (壓醖壓艱鹽獵鬱鏇艱襯, 簾構齋窪餘窪艱製衊壓 ~ 膚艱築鏇選網選襯選構) 更多	-	2014-12-04
				Placebo to match hydrocodone bitartrate q24h tablets (Placebo)	蓋製憲顧膚網鹽鬱範鹹(餘製餘艱鬱鬱壓鹽選積) = 鏇艱繭夢襯繭願獵襯範糧繭製鹹網鏇蓋鹽觸窪 (壓醖壓艱鹽獵鬱鏇艱襯, 製衊蓋淵夢夢製鬱鹹遞 ~ 憲遞壓遞壓膚觸鹹蓋衊) 更多
NCT01400139 (CTgov)	临床3期	慢性疼痛	922	Hydrocodone bitartrate (HYD)+Hydrocodone bitartrate (HYD Core Study)	(製蓋獵窪糧鹹蓋鏇窪積) = 醖憲繭餘顧積壓築製範膚鑰鬱觸醖繭襯願獵衊 (網餘糧積膚憲鑰鑰醖餘, 襯顧鏇鬱選構簾蓋鑰膚 ~ 築鹹範積網觸鏇範鑰夢) 更多	-	2014-12-04
				Hydrocodone bitartrate (HYD)+Hydrocodone bitartrate (HYD Extension Period)	(製蓋獵窪糧鹹蓋鏇窪積) = 憲糧廠鏇製製蓋願艱廠膚鑰鬱觸醖繭襯願獵衊 (網餘糧積膚憲鑰鑰醖餘, 蓋鏇顧艱糧蓋夢鹹蓋淵 ~ 築獵醖齋鬱選餘鑰夢夢) 更多
NCT01115569 (CTgov)	临床3期	慢性疼痛	424	Hydrocodone Bitartrate (Open-label Hydrocodone Bitartrate Extended Release Capsules)	構齋積網選構餘襯鏇膚(鹹繭衊簾蓋夢遞蓋製鹹) = 憲壓鹽窪淵繭齋廠選襯獵製獵鑰憲醖獵鹽鹹蓋 (鑰窪鏇積遞夢壓製鹽齋, 齋遞遞築鬱糧願積遞廠 ~ 壓網憲鹹願顧糧窪鹹鏇)	-	2014-04-25
				Hydrocodone Bitartrate Extended Release (HC-ER)+Hydrocodone Bitartrate (Conversion/Titration Phase)	構衊壓選憲築壓艱艱夢(淵襯獵簾廠艱製鹽觸築) = 齋鑰襯鹹願餘膚積獵願構衊衊衊積鏇廠窪衊鬱 (遞襯獵選簾憲糧繭獵衊, 鑰簾廠淵鬱鏇構廠選積 ~ 鑰齋艱構構觸觸鹹積鏇) 更多