[Translation] A randomized, double-blind, placebo-controlled Phase I clinical study to evaluate the pharmacokinetic characteristics, safety and tolerability of single and multiple intravenous infusions of Nacubactam in healthy Chinese male subjects

主要目的：评价中国健康男性受试者单次和多次静脉输注后，Nacubactam及代谢产物的药代动力学（血浆和尿液）特征。次要目的：评价中国健康男性受试者单次和多次静脉输注Nacubactam的安全性和耐受性。

[Translation]

Primary objective: To evaluate the pharmacokinetic (plasma and urine) characteristics of Nacubactam and its metabolites after single and multiple intravenous infusions in healthy Chinese male subjects. Secondary objective: To evaluate the safety and tolerability of single and multiple intravenous infusions of Nacubactam in healthy Chinese male subjects.

Start Date05 Dec 2023

Sponsor / Collaborator

Shanghai Fosun Pharmaceutical Industrial Development Co., Ltd.

NCT05905055

/ RecruitingPhase 3

A Phase 3, Multi-Center, Randomized, Single-Blind Study to Assess the Efficacy and Safety of Cefepime/Nacubactam and Aztreonam/Nacubactam Versus Best Available Therapy in Adults With Complicated Urinary Tract Infection, Acute Uncomplicated Pyelonephritis, Hospital-Acquired Bacterial Pneumonia, Ventilator Associated Bacterial Pneumonia, and Complicated Intra-Abdominal Infection Due to Carbapenem Resistant Enterobacterales

This study is a multi-center, randomized, single-blind, parallel-group study to assess the efficacy and safety, when nacubactam is coadministered with cefepime or aztreonam, compared with best available therapy (BAT), in the treatment of patients with cUTI, AP, HABP, VABP, and cIAI, due to Carbapenem Resistant Enterobacterales.

Start Date22 Sep 2023

Sponsor / Collaborator

Meiji Seika Pharma Co., Ltd.

JPRN-jRCT2031230076

/ RecruitingPhase 3IIT

A Phase 3, Multi-Center, Randomized, Single-Blind Study to assess the Efficacy and Safety of Cefepime/Nacubactam and Aztreonam/Nacubactam Versus Best Available Therapy in Adults With Complicated Urinary Tract Infection, Acute Uncomplicated Pyelonephritis, Hospital-Acquired Bacterial Pneumonia, Ventilator-Associated Bacterial Pneumonia, and Complicated Intra-Abdominal Infection due to Carbapenem Resistant Enterobacterales - Integral-2

Start Date29 May 2023

Sponsor / Collaborator-

100 Clinical Results associated with Nacubactam

100 Translational Medicine associated with Nacubactam

100 Patents (Medical) associated with Nacubactam

Literatures (Medical) associated with Nacubactam

01 May 2025·Journal of Global Antimicrobial Resistance

Combined dual β-lactams and diazabicyclooctane β-lactamase inhibitor is highly effective against Mycobacterium abscessus species in vitro

Article

Author: Misawa, Kana ; Kashimura, Shoko ; Nishimura, Tomoyasu ; Enoki, Yuki ; Shimamura, Rina ; Yoshikawa, Maiko ; Taguchi, Kazuaki ; Hasegawa, Naoki ; Matsumoto, Kazuaki

OBJECTIVE:

Mycobacterium abscessus pulmonary disease is a refractory infectious disease. Developing an effective treatment is urgent as the number of patients infected with M. abscessus species (MABS) is increasing worldwide. We previously reported that nacubactam, a diazabicyclooctane (DBO) β-lactamase inhibitor, could inhibit MABS β-lactamase. Few reports have indicated that dual β-lactams are effective with a DBO β-lactamase inhibitor against MABS. The objective of this study was to determine which dual β-lactams have high antibacterial activity against MABS in the presence and absence of nacubactam.

METHODS:

Antimicrobial susceptibility tests were conducted through a checkerboard assay of 27 β-lactams using the broth microdilution method for three subspecies-type strains and 20 clinical isolates of MABS. The number of intracellular and extracellular bacteria was measured using human macrophages infected with M. abscessus treated with effective combinations confirmed in susceptibility tests.

RESULTS:

In antimicrobial susceptibility tests, 91 combinations of dual β-lactams with nacubactam exhibited synergistic effects on M. abscessus JCM13569. Among them, the combination of cefazolin, cefotiam, cefoxitin, or cefuroxime with imipenem and nacubactam exhibited highly synergistic effects, resulting in low MICs against MABS clinical isolates. Without nacubactam, the combination of imipenem and cefoxitin showed the lowest MIC. In experiments using human macrophages infected with M. abscessus, these dual β-lactam combinations reduced the number of intracellular and extracellular bacteria compared with those of single β-lactams.

CONCLUSIONS:

The combination of cefazolin, cefotiam, cefoxitin, or cefuroxime with imipenem and nacubactam was highly effective against MABS. Without nacubactam, the combination of cefoxitin and imipenem was effective.

01 May 2025·EUROPEAN JOURNAL OF CLINICAL MICROBIOLOGY & INFECTIOUS DISEASES

In vitro activity and resistance mechanisms of novel antimicrobial agents against metallo-β-lactamase producers

Review

Author: Costa, Cristina ; Cavallo, Rossana ; Broccolo, Francesco ; Bianco, Gabriele ; Gaibani, Paolo ; Boattini, Matteo ; Comini, Sara

Abstract:

The carbapenemase-producing Gram-negative organisms represent an urgent clinical and public health concern, as they have been associated with increased mortality and high dissemination in healthcare settings. Although overall incidence rates of infections sustained by metallo-β-lactamase (MβL)-producers have remained lower than those sustained by other carbapenemase-producers, albeit with substantial geographic differences, a significant increase in the prevalence of MβL-producers has been observed over the last decade. The recent development of new antimicrobials expanded the armamentarium to counter the challenge of metallo-β-lactamase (MβL)-producers. Cefiderocol and aztreonam/avibactam are already clinically available and recommended by international guidelines. In addition, two new classes of β-lactam/ β-lactamase combinations are under clinical evaluation: (i) combination of β-lactam with novel boronic-derived inhibitors (e.g. taniborbactam and xeruborbactam), (ii) combination of β-lactam with last generation diazabicyclooctane β-lactamase inhibitors (e.g. zidebactam and nacubactam), active on most of serine-β-lactamases but also showing strong intrinsic activity on PBP-2. This review aims to provide up-to-date data on the characteristics, activity and emerging resistance mechanisms of the armamentarium of clinically available or soon-to-be introduced drugs for the treatment of MβL-producing Gram-negative organisms.

13 Feb 2025·ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Advancements in the fight against globally distributed OXA-48 carbapenemase: evaluating the new generation of carbapenemase inhibitors

Article

Author: García-Pose, Andrea ; Alonso-Garcia, Isaac ; Guijarro-Sánchez, Paula ; Muras, Andrea ; Bou, German ; Blanco-Martin, Tania ; Outeda-García, Michelle ; Gonzalez-Bello, Concepción ; Rodriguez-Coello, Arianna ; Lence, Emilio ; Rodriguez-Pallares, Salud ; Arca-Suárez, Jorge ; Gonzalez-Pinto, Lucia ; Vázquez-Ucha, Juan Carlos ; Beceiro, Alejandro ; Maceiras, Romina ; Lasarte-Monterrubio, Cristina

ABSTRACT:

Carbapenemase OXA-48 and its variants pose a serious threat to the development of effective treatments for bacterial infections. OXA-48-producing Enterobacterales are the most prevalent carbapenemase-producing bacteria in large parts of the world. Although these bacteria exhibit low-level carbapenem resistance in vitro , the infections they cause are challenging to treat with conventional therapies, owing to their spread and complex detection in clinical settings. However, numerous β-lactamase inhibitors (BLIs) are currently in the pipeline or late clinical stages. To assess the potential of these compounds, this study compared the efficacy against OXA-48 of novel β-lactamase inhibitors, specifically the 1,6-diazabicyclo[3,2,1]octanes (DBOs) avibactam, relebactam, zidebactam, nacubactam, and durlobactam, along with the cyclic and bicyclic boronates vaborbactam, taniborbactam, and xeruborbactam. The extensive kinetics assays identified xeruborbactam, taniborbactam, and durlobactam, together with the already established avibactam, as BLIs with superior biochemical performance. Susceptibility testing further validated these findings but also demonstrated significantly improved bacterial killing by the DBOs zidebactam, nacubactam, and durlobactam. On the other hand, binding studies demonstrated the superior inhibitory capacity of the BLIs durlobactam and xeruborbactam. Combinations, such as cefepime/zidebactam, meropenem/nacubactam, and sulbactam/durlobactam, show promising activity against OXA-48-producing Enterobacterales, while ceftazidime/avibactam, cefepime/taniborbactam, and meropenem/xeruborbactam combinations also appear highly active, largely due to the excellent kinetics of these new inhibitors. Overall, this comprehensive analysis provides important insights into the effectiveness of new BLIs against OXA-48-producing Enterobacterales, highlighting xeruborbactam, durlobactam, and avibactam as leading candidates. Additionally, BLIs like zidebactam, nacubactam, and taniborbactam also showed potential in addressing the clinical challenges posed by OXA-48-mediated antimicrobial resistance.

News (Medical) associated with Nacubactam

28 Aug 2024

·www.prnewswire.com

Fosun Pharma Announces 2024 Interim Results

Breakthroughs for Innovative Products Going Overseas with Global Operation Capabilities Continuing to Strengthen SHANGHAI, Aug. 28, 2024 /PRNewswire/ -- On August 27, Shanghai Fosun Pharmaceutical (Group) Co., Ltd. ("Fosun Pharma" or "the Group"; Stock Code: 600196.SH; 02196.HK), announced its operating performance for the first half of 2024 (the "Reporting Period"). During the Reporting Period, Fosun Pharma achieved revenue of RMB20.46 billion, an increase of 5.31% YoY after excluding COVID-related products. The net profit attributable to owners of the parent of the Group after deducting extraordinary gain or loss amounted to RMB1.3 billion. In the second quarter of 2024, the net profit attributable to owners of the parent of the Group after deducting extraordinary gain or loss was RMB646 million, a quarter-on-quarter increase of RMB37 million. As a global innovation-driven pharmaceutical and healthcare industry group, Fosun Pharma continuously advance its innovation transformation and the development and commercialization of innovative products. In the first half of 2024, Fosun Pharma's revenue from key innovative products in pharmaceuticals business grew steadily, exceeding RMB3.7 billion. In 2024, Fosun Pharma continued to boost operational efficiency and profitability, laying the foundation for long-term sustainable development. During the Reporting Period, the gross margin minus the selling and distribution expense ratio increased by 1.72 percentage points YoY; excluding the impact of newly acquired companies, the management expense decreased by about RMB0.2 billion. During the Reporting Period, Fosun Pharma ensured stable free cash flow through measures including optimizing operating cash flow, supply chain management, and controlling capital expenditures, achieving operating cash flow of RMB1.9 billion, a period-on-period increase of 5.36%, exceeding the growth of operating profit. In addition, the Group continued to optimize asset structure and improve asset efficiency. Since 2024, the cash inflow from asset disposals and the expected cash inflow from contracts signed by Fosun Pharma exceeded RMB2 billion in aggregate. Revenue from innovative products maintains steady growth, with a further focus on innovative drugs and high-value devices In the first half of 2024, Fosun Pharma further focused on innovative drugs and high-value devices. Four key innovative products with a total of 9 indications, independently developed and licensed-in by the Group, were approved for launch domestically and internationally. In addition to the key innovative products, Fosun Pharma also had 38 generic drug varieties approved for launch domestically and internationally. In the first half of 2024, Fosun Pharma's pharmaceutical manufacturing segment achieved revenue of RMB14.7 billion. The innovative drug business achieved breakthroughs in core therapeutic areas such as solid tumors, hematologic tumors and immunity inflammation, and realized multiple innovative achievements in hematologic tumors, breast cancer and lung cancer, benefiting patients worldwide. Han Si Zhuang (serplulimab injection), Fosun Pharma's first self-developed biopharmaceutical innovative drug, as well as the world's first anti-PD-1 monoclonal antibody (mAb) approved for the first-line treatment of small cell lung cancer (SCLC), was commercialized in the domestic market in March 2022. Up to now, it has been approved for 4 indications, broadly covering high-incidence tumours including lung cancer and gastrointestinal cancer, benefiting over 75,000 patients globally. Additionally, the 5th NDA of Han Si Zhuang for the first-line treatment of non-squamous non-small cell lung cancer (nsNSCLC) has been accepted by the National Medical Products Administration (NMPA) in China. During the Reporting Period, Fosun Pharma's self-developed biosimilar Han Da Yuan (adalimumab injection) received 4 new indications approval from the NMPA. It has now been approved for eight indications in China, covering all indications of originator adalimumab in China, providing more treatment options for adult and pediatric patients with autoimmune diseases. Fosun Pharma adheres to an open innovation strategy, and actively expands its pipelines through BD in addition to independent R&D. In June 2024, Su Ke Xin (avatrombopag malate tablets), which is exclusively commercialized by Fosun Pharma, received approval in Chinese mainland for a second indication for the treatment of adult patients with chronic primary immune thrombocytopenia (ITP) who have shown poor response to prior treatment, further benefiting ITP patients in China. Additionally, certain domestic innovative drugs licensed-in by the Group such as Bei Wen (keverprazan hydrochloride tablets) and Pei Jin (telpegfilgrastim injection), were officially included in the National Medical Drugs Catalogue in January 2024. This significantly enhanced the accessibility of drugs for relevant diseases within Chinese mainland and practically reduced the burdens of drugs on patients, aiming to improve the living and life quality of patients through regulated therapies. In the field of vaccines, Fosun Pharma has established an independent R&D system centered on two major technical platforms: bacterial vaccines and viral vaccines. In March 2024, the rabies vaccine (Vero cell) for human use (freeze dried), which is independently developed by the Group, has been approved for launch in Chinese mainland. The production line has also passed the GMP compliance inspection. Research progress on various pipelines develops rapidly to secure innovative development To meet the unmet clinical needs, through diversified and multi-level cooperation models such as independent R&D, co-development, license-in and industrial investment, Fosun Pharma continues to enrich its innovative product pipeline and focus on differentiated product R&D with high-tech barriers, to continuously enhance the value of its pipeline. In the first half of 2024, Fosun Pharma's total R&D expenditure amounted to RMB2.7 billion, with R&D expenses totaling RMB1.9 billion. The R&D expenditure in the pharmaceutical manufacturing segment amounted to RMB2.4 billion, accounting for 16.4% of the segment's revenue. In particular, R&D expenses were RMB1.6 billion, accounting for 10.7% of the segment's revenue. In the first half of 2024, 4 innovative drugs/biosimilars with a total of 9 indications independently developed, co-developed and licensed-in by the Group had entered the pre-launch approval/critical clinical stage. The pharmaceutical manufacturing segment of the Group submitted 124 patent applications, including 2 American patents applications, 8 PCT applications, and the Group has obtained 37 licensed invention patents authorization. During the Reporting Period, the New Drug Application (NDA) of self-developed selective MEK1/2 inhibitor (project code: FCN-159) for two indications was accepted by NMPA in May and June 2024, both of which were included in the priority review procedure. The Marketing Authorization Application (MAAs) for five indications of the self-developed denosumab biosimilar HLX14 (recombinant anti-RANKL fully human monoclonal antibody injection) was accepted by the European Medicines Agency (EMA). Additionally, during the Reporting Period, the Phase 3 clinical trials for its self-developed Han Si Zhuang (serplulimab injection), in combination with bevacizumab and chemotherapy for the first-line treatment of metastatic colorectal cancer (mCRC) patients, had commenced in the Chinese mainland. The combination dosing of OP0595 and cefepime or aztreonam, developed by Fosun Pharma in collaboration with Meiji Seika Pharma Co., Ltd., for the treatment of adults infected by aerobic gram-negative bacteria with limited options, had commenced two phase III clinical trials in China. During the Reporting Period, clinical data from multiple pipeline products and marketed products of Fosun Pharma were presented at global industry conferences, including the American Society of Clinical Oncology (ASCO), American Association for Cancer Research (AACR), and the European Hematology Association (EHA), further demonstrating the Group's innovative R&D capabilities on the international stage. In addition to independent R&D, Fosun Pharma actively practices an open R&D model, engaging in the incubation and investment of R&D projects through initiatives such as the establishment and management of industrial funds, ensuring the sustainability of its innovation pipeline. During the reporting period, Fosun Pharma successfully completed the establishment and filing of Shenzhen Biopharma Industrial Fund with fundraising size of RMB5.0 billion Continues to enhance global operation capabilities and gains international recognition for innovative products Fosun Pharma continues to uphold the internationalization strategy in multiple dimensions, such as innovative R&D, two-way license, production and operations as well as commercialization to enhance operational efficiency and strengthen global market layout while covering major overseas markets, including the United States, Europe, Africa, India, and Southeast Asia. As at the end of the Reporting Period, the Group had formed an overseas commercialization team of approximately 1,000 employees. For the first half of 2024, overseas revenue reached RMB5.5 billion, an increase of 15.13% YoY, accounting for 26.93% of total revenue. During the Reporting Period, Fosun Pharma's self-developed Han Qu You (trastuzumab injection, trade name: HERCESSI™ in the U.S., Zercepac® in Europe) received the U.S. FDA approval for three indications covering the treatment of breast cancer and gastric cancer, becoming the first domestic biosimilar approved for launch in China, the EU and the United States. Additionally, through collaboration with global renowned pharmaceutical companies, Fosun Pharma has established a presence in Europe, the United States, Canada, and numerous emerging markets. Up to date, Han Qu You has been approved in 48 countries and regions, benefiting 200,000+ patients, bringing affordable and high-quality treatment options to breast cancer and gastric cancer patients worldwide. Self-developed biopharmaceutical innovative drug of Fosun Pharma, Serplulimab Injection (anti-PD-1 monoclonal antibody, Chinese trade name: Han Si Zhuang) completed the first international shipment in January 2024, making it the first Chinese anti-PD-1 mAb approved for launch in Southeast Asia. The marketing authorization application (MAA) of Han Si Zhuang has been accepted in March 2023 and its head-to-head bridging trial comparing to first-line standard of care with Atezolizumab for extensive-stage small cell lung cancer (ES-SCLC) had entered clinical enrollment stage in the United States. At the same time, Fosun Pharma has established an innovative drug team in the United States to advance the commercialization of Serplulimab Injection. Fosun Pharma actively introduces leading international technologies and products into the Chinese market to benefit more patients. During the Reporting Period, the Headquarters Industrial Base of the joint venture Intuitive Fosun officially opened and was put into operation in Shanghai Zhangjiang International Medical Park. The base integrates R&D, production and training, and its operation will further accelerate the localization process of the Da Vinci Surgical System. As at the end of June 2024, the accumulated total installation volume of the Da Vinci Surgical Robot in Chinese mainland and Hong Kong S.A.R.and Macau S.A.R. was over 380 in more than 300 hospitals. More than 540,000 patients had benefited from the Da Vinci Surgical Robot's precise treatment and returned to normal life. During the Reporting Period, Fosun Pharma's joint venture with Insightec, Fosun Insightec, made steady progress in the commercialization, clinical application and research of magnetic resonance-guided focused ultrasound treatment system for neurological diseases (MRgFus brain therapy system) in Chinese mainland, Hong Kong S.A.R and Macao S.A.R.. As a global pharmaceutical and healthcare industry group, Fosun Pharma continues to promote the building of production system with international quality standard, with its quality management system and production capabilities recognized by leading international certification authorities, laying a solid foundation for the overseas distribution of preparations. As at the end of the Reporting Period, all production lines of the domestic subsidiaries under the pharmaceutical manufacturing segment of the Group obtained domestic GMP certifications and 10 production lines had passed GMP certification in major regulatory markets such as the U.S. and the EU. "Guided by the 4IN strategy (Innovation, Internationalization, Intelligentization, and Integration), Fosun Pharma consistently focuses on unmet clinical needs, prioritizes innovative R&D, adheres to technology-driven and product-driven approach, and strengthens global operation capabilities, ensuring steady and sustainable development." Wu Yifang, Chairman of Fosun Pharma, said, "Looking forward, Fosun Pharma's internal operation will be further improved in quality and efficiency, continuing to enhance its leading position in hematologic tumors, breast cancer, lung cancer and other fields while expanding footprint in immunity inflammation, chronic diseases and central nervous system. We will also intensify industry-university-research strategic cooperation with world-class universities and research institutions to capture innovative products at an early stage. At the same time, we will actively promote the overseas export of high-quality products and promote global simultaneous development, aiming to become the global leading integrator of pharmaceutical and healthcare innovation." About Fosun Pharma Founded in 1994, Shanghai Fosun Pharmaceutical (Group) Co., Ltd.* ("Fosun Pharma"; stock code: 600196.SH, 02196.HK) is a global innovation-driven pharmaceutical and healthcare industry group. Fosun Pharma directly operates businesses including pharmaceuticals, medical devices, medical diagnosis, and healthcare services. As a shareholder of Sinopharm Co., Ltd., Fosun Pharma expands its areas in the pharmaceutical distribution and retail business. Fosun Pharma is patient-centered and unmet clinical needs-oriented. Through diversified and multi-level cooperation models such as independent research and development, cooperative development, license-in, and industrial investment, the company continues to enrich its innovative product pipeline and focus on differentiated product R&D with high-tech barriers, to continuously enhance the value of its pipeline. Fosun Pharma's innovative products focus on core therapeutic areas such as solid tumors, hematologic tumors and immunity inflammation. It also strengthens core technology platforms such as antibodies/ADC, cell therapy, and small molecules. Guided by the 4IN strategy (Innovation, Internationalization, Intelligentization, and Integration), Fosun Pharma adheres to the business philosophy of "Innovation for Good Health", continues to promote innovative transformation, actively deploys internationalization, strengthens business focus by product lines, promotes integrated operations and efficiency improvement, and is dedicated to being the global leading integrator of pharmaceutical and healthcare innovation. For more information, please visit our official website: SOURCE Fosun Pharma

Drug ApprovalPhase 3

23 Oct 2020

·www.biospace.com

Could Arixa Pharmaceuticals’ Lead Product Pave the Way for More Efficient Antibiotics?

Photo courtesy of Arixa Pharmaceuticals Arixa Pharmaceuticals announced on Thursday that Pfizer’s hospital business has agreed to acquire the company. Arixa has been developing oral antibiotics for antibiotic-resistant Gram-negative infections. John G. Freund, co-founder and CEO of Arixa, pictured above. Photo courtesy of Arixa Pharmaceuticals. Arixa Pharmaceuticals announced on Thursday that Pfizer ’s hospital business has agreed to acquire the company. Arixa has been developing oral antibiotics for antibiotic-resistant Gram-negative infections. Its technology platform uses prodrug chemistry and existing intravenous-only antimicrobial agents to allow their active ingredients to be orally administered. The financial terms of the acquisition have not been released. “Common Gram-negative infections such as complicated urinary tract infections are becoming a major treatment challenge because of increasing rates of multidrug resistance,” said Jose Vazquez, M.D., Professor, Department of Medicine and Chief of Infectious Diseases at Medical College of Georgia at Augusta University. “There are a progressively larger number of patients who cannot be treated with oral antibiotics and we are forced to treat them with intravenous agents. The option to administer an oral antibiotic containing avibactam to my patients with infections due to pathogens resistant to other oral agents, and thus avoiding intravenous administration and a hospital stay, would always be considered an important advance.” Arixa’s lead compound is ARX-1796, an oral prodrug of avibactam, a beta lactamase inhibitor (BLI). As a result of the company’s patented chemistry, a Phase I study has confirmed that the prodrug of avibactam is 60% to 80% absorbed when administered orally. In contrast, approximately 7% of the prodrug is absorbed when intravenously administered. “We are proud to have created and developed an important new drug candidate in a highly capital efficient manner, and believe Pfizer is the perfect company to take ARX-1796 into subsequent clinical trials and if approved, eventually to patients in need,” said John G. Freund MD MBA, Co-Founder and CEO, Arixa. “We built Arixa as a completely virtual company, with no employees and essentially no overhead - our work was performed by Contract Research Organizations under the supervision of a group of part-time expert consultants. This model has been behind the success of driving the developmental course of ARX-1796.” Annaliesa Anderson, vice president and chief scientific officer of Bacterial Vaccines and Hospital at Pfizer, noted that the company will advance the development program for ARX-1796. The goal is to leverage the potential benefits of the product, and help patients and the overall healthcare system. Arixa was initially granted a broad composition of matter patent by the U.S. Patent and Trademark Office covering use of its prodrug chemistry to develop oral prodrugs of avibactam back in November 2018. The patent also covered relebactam, nacubactam and ETX2514, which share the same chemical scaffold. At the time ARX-1796 was the only BLI in development with an FDA-approved active compound. “The conventional wisdom had been that synthesis of a non-alkylating orally-bioavailable prodrug of avibactam was not possible,” said Daniel H. Rich, Ph.D., Emeritus Ralph F. Hirschmann Professor of Medicinal and Organic Chemistry at the University of Wisconsin-Madison. “The authors of this paper demonstrated that it could be done. This novel orally-available form of a critically important beta-lactamase inhibitor is a stunning accomplishment in prodrug design and synthesis.” Avibactam was originally approved by the U.S. Food and Drug Administration back in 2015 as the BLI in Avycaz, an intravenous combination with a cephalosporin, ceftazidime, for the treatment of a number of indications caused by Gram-negative pathogens. Similar to other BLIs, Avibactam is meant to protect beta-lactam antibiotics, such as penicillin, from being destroyed by beta-lactamase enzymes that bacteria produce to defend themselves.

Phase 1AcquisitionDrug Approval

16 Jan 2015

·www.biospace.com

Buying Spree Continues as Roche Picks Up Trophos in $540 Million Deal

January 16, 2015 By Mark Terry , BioSpace.com Breaking News Staff Basel, Switzerland-based Roche announced today that is acquiring Marseille , France-based Trophos for $540 million. There will be an upfront cash payment of 120 million euros and additional contingent payments up to 350 million euros based on milestones. Founded in 1999, Trophos is a privately-held clinical stage pharmaceutical company. Its platform is based on cholesterol-oxime based chemistries and develops mitochondrial targeted compounds. The research is linked to cell death or survival. The company’s olesoxime (TRO19622) is under development for the treatment of SMA, a rare genetic neuromuscular disease most common in children. “SMA is a grievous disease with a huge impact on the daily life of patients and their families, who are currently left only with supportive care,” said Christine Placet , chief executive of Trophos in a statement. “We are proud to see the development of this medicine evolving, with the ultimate goal of a potential first medicine for SMA. This is a tremendous recognition of the work done by Trophos ’s teams and supporters over the past 16 years.” This marks yet another deal by Roche . Earlier this week the company announced a $750 million deal with Japan’s Meiji Seika Pharma and Canada’s Fedora Pharmaceuticals for a beta-lactamase inhibitor OP0595 for antibiotic resistant bacteria. On Jan. 12 Roche entered into a strategic collaboration with Cambridge, Mass.-based Foundation Medicine, Inc. In that deal Roche will fund Foundation ’s research and development for more than $150 million for a minimum of five years. That deal totals about $1.03 billion and gives Roche a 56.3 percent stake in Foundation . “This acquisition highlights Roche ’s commitment to developing medicines for spinal muscular atrophy, a serious disease with no effective treatment,” said CMO and Head of Roche Global Product Development Sandra Horning in a statement. “We will build on the work done by Trophos and the French Muscular Dystrophy Association to advance the development of olesoxime and to bring it to people who live with this devastating condition as quickly as possible.” Olesoxime is designed to protect motor nerve cells. The compound has been granted Orphan Medicinal Product designation for the treatment of SMA by the European Medicines Agency and orphan drug designation by the U.S. Food and Drug Administration . The drug has shown beneficial effect in maintaining neuromuscular function in patients with Type II and non-ambulatory Type III SMA, as well as cutting medical complications. SMA is a rare disease affecting one in 6,000 to 10,000 children. An autosomal recessive genetic disease, a loss of function of the Survival Motor Neuron (SMN) 1 gene is the cause of the loss of function. This decrease in levels of the SMN protein causes progressive deterioration of nerve cells in the spinal cord and loss of motor neurons.

AcquisitionOrphan Drug

100 Deals associated with Nacubactam

External Link

KEGG	Wiki	ATC	Drug Bank
D11329	-	-	DB15353

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Carbapenem Resistant Bacterial Infection	Phase 3	Japan	Meiji Seika Pharma Co., Ltd.	22 Sep 2023
Complicated intra-abdominal infection	Phase 3	Japan	Meiji Seika Pharma Co., Ltd.	22 Sep 2023
Hospital acquired bacterial pneumonia	Phase 3	Japan	Meiji Seika Pharma Co., Ltd.	22 Sep 2023
Ventilator associated bacterial pneumonia	Phase 3	Japan	Meiji Seika Pharma Co., Ltd.	22 Sep 2023
Acute pyelonephritis	Phase 3	Estonia	Meiji Seika Pharma Co., Ltd.	23 May 2023
Complicated urinary tract infection	Phase 3	Georgia	Shanghai Fosun Pharmaceutical Industrial Development Co., Ltd.	22 May 2023
Gram-Negative Bacterial Infections	Phase 3	Georgia	Shanghai Fosun Pharmaceutical Industrial Development Co., Ltd.	22 May 2023
Pyelonephritis	Phase 3	Georgia	Shanghai Fosun Pharmaceutical Industrial Development Co., Ltd.	22 May 2023
Infectious Diseases	Phase 1	Japan	Meiji Seika Pharma Ltd.	30 Jan 2022
Urinary Tract Infections	Phase 1	United States	Hoffmann-La Roche, Inc.	11 Jul 2017

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

AI Agents Built for Biopharma Breakthroughs

Accelerate discovery. Empower decisions. Transform outcomes.

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis