An Adaptive, Randomized, Double Blind, Placebo Controlled Three Part Study of the Safety, Tolerability, and Pharmacokinetics of MRX-8 Administered Intravenously to Healthy Volunteers in Single Ascending and Multiple Ascending Dose Cohorts

This Phase 1 study is designed to assess the safety and tolerability of single and multiple intravenous (IV) doses of MRX-8, to assess the pharmacokinetics of MRX-8 and its primary metabolite following single and multiple IV doses, and to measure the elimination of MRX-8 and its metabolite in urine.

开始日期2020-11-29

申办/合作机构

MicuRx Pharmaceuticals, Inc.

[+1]

100 项与 MRX-8 相关的临床结果

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100 项与 MRX-8 相关的转化医学

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100 项与 MRX-8 相关的专利（医药）

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项与 MRX-8 相关的文献（医药）

2020-10-20·Antimicrobial agents and chemotherapy2区 · 医学

Pharmacodynamic Evaluation of MRX-8, a Novel Polymyxin, in the Neutropenic Mouse Thigh and Lung Infection Models against Gram-Negative Pathogens

2区 · 医学

Article

作者: Lepak, Alexander J. ; Wang, Wen ; Andes, David R.

MRX-8 is a novel polymyxin analogue in development for the treatment of infections caused by Gram-negative pathogens, including those resistant to other antibiotic classes. In the present study, we examined the pharmacodynamic activity of MRX-8 against a variety of common Gram-negative pathogens in the neutropenic mouse thigh and lung models. Additionally, we examined polymyxin B (PMB) as a comparator. Plasma pharmacokinetics of MRX-8 and PMB were linear over a broad dosing range of 0.156 to 10 mg/kg of body weight and had similar AUC 0–∞ (area under the drug concentration-time curve from 0 h to infinity) exposures of MRX-8, 0.

Antibiotics (Basel, Switzerland)

Pharmacokinetics and Nephrotoxicity of Polymyxin MRX-8 in Rats: A Novel Agent against Resistant Gram-Negative Bacteria

Article

作者: Li, Xin ; Guo, Chenxue ; Qu, Xingyi ; Xi, Lin ; Liu, Shaojun ; Zhang, Jing ; Liu, Xiaofen

MRX-8 is a novel polymyxin for carbapenem-resistant Gram-negative infections that has been recently evaluated in Phase I clinical trials. Herein, its pharmacokinetics (PK) and nephrotoxicity in rats are reported for the first time. This study aimed at pre-clinical PK and safety assessments. An LC-MS/MS method was developed to determine concentrations of MRX-8 and its major deacylation metabolite, MRX-8039, in rat plasma. Animals were administered a single dose of MRX-8 (2, 4, 6, and 8 mg/kg) or comparator polymyxin B (PMB) (4 and 8 mg/kg) to compare the kidney injury known for the polymyxin drug class. Nephrotoxicity was evaluated using serum creatinine, blood urea nitrogen (BUN) biomarkers, and renal histopathology. In rats, MRX-8 displayed linear PK within the range of 2–8 mg/kg, with approximately 4% of MRX-8 converted to MRX-8039. MRX-8 induced only mild increases in serum creatinine and BUN levels, with an apparent decrease in nephrotoxicity within 24 h, in contrast to PMB, which exhibited a significant and more persistent toxicity. Additional nephrotoxicity biomarkers (plasma NGAL and urinary NGAL, KIM-1, and TIMP-1) have confirmed attenuated MRX-8 kidney injury. Histopathology has revealed significantly greater cellular/tissue toxicity for PMB as compared to MRX-8 (variances of p = 0.008 and p = 0.048 vs. saline control, respectively). Thus, MRX-8 induces a mild and reversible kidney injury in rats compared to PMB. These data support a continued evaluation of the novel polymyxin in human trials.

Expert Review of Anti-Infective Therapy

Potentially effective antimicrobial treatment for pneumonia caused by isolates of carbapenem-resistant and extensively drug-resistant Acinetobacter baumannii complex species: what can we expect in the future?

Review

作者: Huang, Tzu-Yu ; Liu, I-Min ; Jean, Shio-Shin ; Lai, Chih-Cheng ; Hsueh, Po-Ren ; Hsieh, Po-Chuen ; Liu, Chia-Ying

INTRODUCTION:

Acinetobacter baumannii complex (Abc) is currently a significant cause of difficult-to-treat pneumonia. Due to the high prevalence rates of carbapenem- and extensively drug-resistant (CR, XDR) phenotypes, limited antibiotic options are available for the effective treatment of pneumonia caused by CR/XDR-Abc.

AREAS COVERED:

In vitro susceptibility data, relevant pharmacokinetic profiles (especially the penetration ratios from plasma into epithelial-lining fluid), and pharmacodynamic indices of key antibiotics against CR/XDR-Abc are reviewed.

EXPERT OPINION:

Doubling the routine intravenous maintenance dosages of conventional tigecycline (100 mg every 12 h) and minocycline (200 mg every 12 h) might be recommended for the effective treatment of pneumonia caused by CR/XDR-Abc. Nebulized polymyxin E, novel parenteral rifabutin BV100, and new polymyxin derivatives (SPR206, MRX-8, and QPX9003) could be considered supplementary combination options with other antibiotic classes. Regarding other novel antibiotics, the potency of sulbactam-durlobactam (1 g/1 g infused over 3 h every 6 h intravenously) combined with imipenem-cilastatin, and the β-lactamase inhibitor xeruborbactam, is promising. Continuous infusion of full-dose cefiderocol is likely an effective treatment regimen for CR/XDR-Abc pneumonia. Zosurabalpin exhibits potent anti-CR/XDR-Abc activity in vitro, but its practical use in clinical therapy remains to be evaluated. The clinical application of antimicrobial peptides and bacteriophages requires validation.

项与 MRX-8 相关的新闻（医药）

2024-10-18

·PRNewswire

MicuRx Pharmaceuticals Showcases the Pipeline Status of MRX-5 and MRX-8 at BIO Investor Forum

SAN FRANCISCO, Oct. 18, 2024 /PRNewswire/ -- Dr. Regis Vilchez, Chief Medical Officer of MicuRx Pharmaceuticals, presented the latest advancements of company's development program, MRX-5 and MRX-8, at the BIO Investor Forum (BIF). These development programs offer new potentials for the future treatment of Nontuberculous Mycobacterial (NTM) pulmonary diseases and Pseudomonas aeruginosa (PsA) pulmonary infections. Continue Reading MRX-5, a novel benzoxaborole antibiotic, is developed for the treatment of rare chronic pulmonary disease caused by NTM infection. MRX-5 exhibits excellent antibacterial activity against common NTM pathogens and demonstrates good safety in animal trials.MABC affects approximately 12,000 to 20,000 patients in the US and requires treatment durations exceeding 12 months. MRX-5 holds promise for addressing NTM infections. MRX-8, a novel antibiotic in the polymyxin class, is designed to treat severe infections caused by multidrug-resistant Gram-negative bacteria. Traditional polymyxins are limited in clinical use due to high risks of nephrotoxicity and neurotoxicity. MRX-8, with its novel chemical structure, maintains or improves therapeutic efficacy while significantly reducing these risks. The company also aims to explore the clinical and commercial potential of developing an inhaled formulation targeting chronic lung infections. In mouse models of PsA lung infections, nebulized MRX-8 demonstrated significant reduction in bacterial load in lung tissues, indicating strong bactericidal activity. At the forum, Dr. Regis Vilchez focused on presenting the development progress and future plans for MRX-5 and MRX-8, while analyzing the significant market demand for treatments targeting NTM lung disease and chronic PsA pulmonary infections. These two pipeline products are expected to fill gaps in the treatment of NTM lung disease and chronic PsA pulmonary infections, offering patients safer and more effective new treatment options. MicuRx Pharmaceuticals remains committed to discovering, developing, and commercializing innovative medicines to meet unmet clinical needs, providing patients with differentiated therapeutic solutions. The company will continue to actively advance the development of MRX-5 and MRX-8, aiming to bring these innovative drugs to market as soon as possible, bringing hope to patients worldwide. For more information, please contact: MicuRx Pharmaceuticals, Inc. Website: About MicuRx Pharmaceuticals MicuRx Pharmaceuticals is a biopharmaceutical company focused on the discovery, development, and commercialization of innovative antibiotics for the treatment of multidrug-resistant infections. With a mission to address significant unmet medical needs, MicuRx is advancing a portfolio of drug candidates targeting difficult-to-treat infections. SOURCE MicuRx Pharmaceuticals WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

2024-09-03

·GBIHealth

Y24H1财报速读：盟科药业态势稳定，营收增长44%至6074万元

近日，多家药企陆续公布了2024年上半年财务业绩。盟科药业上半年态势稳定，营收增长向好，主要商业化产品市场进一步扩大；营收增长44%至6074万元 2024年9月3日，上海盟科药业股份有限公司（盟科药业，688373.SH）披露2024年上半年度（2024H1）报告。报告期内，公司实现营业收入6,073.82万元，同比增长44.24%；归母净亏损2.01亿元，相比上年同期（亏损1.25亿元）进一步扩大。公司期内研发投入达16,616.74万元，同比增长72.91%；研发投入占营业收入273.58%，较上年同期增长45.37个百分点。公司目前仅有一款商业化产品——新一代噁唑烷酮类抗菌药康替唑胺片。该产品可用于治疗多重耐药革兰阳性菌引起的感染，目前已覆盖了全国533家医院，在143家医院实现了正式准入及批量临采。在研管线中，康替唑胺片水溶性前药MRX-4正在推进Ⅲ期临床试验进程，用于治疗多重耐药革兰阴性菌感染的MRX-8已完成中国Ⅰ期临床试验并达到预期目标，抗非结核分枝杆菌感染（NTM）的MRX-5预计年内完成澳洲Ⅰ期临床试验。全球医疗情报领导者解锁隐藏在数据中的商业潜力关于 G B I ” 自从2002年成立以来，GBI始终以技术为驱动，为药企、器械及行业相关服务商提供贯穿生命周期的全球药品市场竞争数据、全球行业资讯、HCPs洞察、全国医疗器械数据等商业信息与洞察，助力企业在进行战略布局和决策时，脱颖而出。历经20余年的深耕细作GBI已成为95%以上跨国药企、国内头部药企、咨询与投资机构等医疗圈灯塔用户值得信赖的长期合作伙伴。联系我们投稿 | 发稿 | 媒体合作 ▶ zhangxinyue13@baidu.com 数据库 | 咨询服务 | 资讯追踪 ▶ 点击左下“阅读原文”完成表单填写点击阅读原文，解锁完整双语新闻

财报临床3期

2024-07-18

·PRNewswire

MicuRx Presents Innovative Antibiotic Research Results at the 7th World Bronchiectasis Conference

MicuRx showcased the latest research progress on their pipeline products, MRX-5 and MRX-8, at the 7th World Bronchiectasis Conference Three significant study results further support the potential of MRX-5 and MRX-8 in treating Nontuberculous Mycobacteria (NTM) lung disease and Pseudomonas aeruginosa infections DUNDEE, Scotland, July 18, 2024 /PRNewswire/ -- Shanghai MicuRx Pharmaceutical Co., Ltd. ("MicuRx"，688373.SH) presented the latest research progress on their novel antibiotic pipeline products, MRX-5 and MRX-8, at the 7th World Bronchiectasis Conference (WBC) held in Dundee, Scotland, from July 4 to 6, 2024. These research results provide new hope for the future treatment of Nontuberculous Mycobacteria (NTM) lung disease and Pseudomonas aeruginosa infections. Conference Background Continue Reading The World Bronchiectasis Conference is a leading global academic conference focused on the research and treatment of bronchiectasis. This conference brings together top scientists and clinical experts from around the world to discuss the latest research developments, clinical management strategies, and the development of new therapies for bronchiectasis. Research Highlights As a biopharmaceutical company dedicated to developing innovative anti-infective drugs, MicuRx presented three significant research results in poster presentation at the conference. These studies further support the potential of MRX-5 and MRX-8 in the treatment of specific infections： In Vitro and In Vivo Activity of A Novel Leucyl-tRNA Synthetase Inhibitor Against Mycobacterium Abscessus The active drug MRX-6038 was very potent against M. abscessus clinical isolates in vitro with MIC90 0.5 mg/L while the control drug clarithromycin MIC90 was 4 mg/L. MRX-6038 greatly reduced the resistance frequency of standard of care drugs (Ethambutol, Clarithromycin, Rifabutin, Clofazimine, Amikacin, Imipenem, Ciprofloxacin) by more than 10 to 100,000 folds, demonstrating the potential for combination with the background therapy. Oral prodrug MRX-5 was tested in mice with lung infections due to M. abscessus isolates, and efficacy was demonstrated against infections with both clarithromycin-sensitive and clarithromycin non-susceptible isolates. In Vitro Activity of Novel Leucyl-tRNA Synthetase Inhibitor Against Mycobacterium Avium Complex MRX-6038, the major activedrug of MRX-5, has demonstrated potent in vitro activity against Mycobacterium avium clinical isolates including isolates not susceptible to clarithromycin. When MRX-6038 was combined with Clarithromycin, Rifabutin, Amikacin, and Ethambutol, the resistance frequency of these standard of care drugs was greatly reduced to below 6.5×10-11. Further studies are warranted for the evaluation of MRX-6038 for the treatment of Mycobacterium avium pulmonary disease. In Vitro and In Vivo Activity of A Novel Antibiotic In The Polymyxin Class Against Pseudomonas Aeruginosa MRX-8 demonstrated potent in vitro activity against P. aeruginosa including tobramycin and amikacin resistant clinical isolates. In mouse models with P. aeruginosa lung infections of both tobramycin-sensitive and tobramycin-resistant isolates, nebulized MRX-8 treatment significantly decreased bacterial load in the lung tissues, demonstrating bactericidal activity. About MRX-8 MRX-8 is a novel polymyxin antibiotic developed by MicuRx, primarily used to treat severe infections caused by multidrug-resistant Gram-negative bacteria. Traditional polymyxins are limited in clinical use due to nephrotoxicity and neurotoxicity. Through meticulous structural design, MRX-8 not only maintains or enhances therapeutic efficacy but also significantly improves safety by reducing these potential toxic risks. In 2022, MRX-8 completed Phase I clinical trials in the United States. In 2023, it completed Phase I enrollment in China, with primary study results released in June 2024. These trial results indicated that MRX-8 achieved the desired therapeutic levels in the human body at the expected clinical doses for infections caused by Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii. Besides systemic administration, the company plans to explore the development of an inhaled formulation of MRX-8 to uncover its clinical and commercial value in targeted treatment of chronic lung infections. About MRX-5 and NTM MRX-5 is a novel benzoxaborole antibiotic developed by MicuRx for infections caused by NTM. NTM is a common pathogen causing bronchiectasis. In recent years, the incidence of NTM diseases has rapidly increased, becoming a significant public health issue. [1] Among diseases caused by NTM, Mycobacterium avium complex and Mycobacterium abscessus complex account for 70%-95% of NTM diseases. [2] The main clinical symptoms of NTM pulmonary infections include persistent cough, sputum production, chest pain, shortness of breath, fatigue, weight loss, and malaise. [1] Preclinical data indicates that MRX-5 has good antibacterial activity against most common NTM pathogens and has demonstrated good safety in animal studies. Additionally, its characteristics of minimal drug interactions, low resistance potential, and oral availability make it an ideal candidate for the treatment of chronic infections. Currently, MRX-5 is undergoing Phase I clinical trials, offering a promising new treatment option for patients with NTM diseases. About Shanghai MicuRx Pharmaceutical Co., Ltd. MicuRx is a biopharmaceutical company focusing on novel therapeutics for infectious diseases. With global independent intellectual property and competitiveness, we are committed to the discovery, development, and commercialization of innovative drugs for unmet medical needs. Since the company was founded in 2007, MicuRx has adhered to the principle of "Better therapy through superior medicine", focusing on the increasingly serious problem of global antimicrobial resistance. For more information, please visit our website at References： SOURCE MicuRx Pharmaceutical

临床1期临床结果

100 项与 MRX-8 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
革兰氏阴性菌感染	临床1期	中国	MicuRx Pharmaceuticals, Inc. (United States)	2022-01-30
下颌骨发育不良伴A型脂肪代谢障碍	临床1期	美国	MicuRx Pharmaceuticals, Inc.	2020-11-29
季节性情感障碍	临床1期	美国	MicuRx Pharmaceuticals, Inc.	2020-11-29