The primary purpose of this study is to assess the effect of renal impairment on the PK of afabicin desphosphono after a single oral 80 milligrams (mg) or intravenous (IV) 55 mg dose of afabicin.

Start Date01 Aug 2026

Sponsor / Collaborator

Debiopharm International SA

NCT03723551

/ TerminatedPhase 2

Randomized Open-label Active-controlled Study to Assess the Safety, Tolerability, and Efficacy of Afabicin IV/Oral in the Treatment of Patients With Bone or Joint Infection Due to Staphylococcus

This is a randomized, active-controlled, open-label study to assess the safety, tolerability and efficacy of Afabicin in the treatment of participants with bone or joint infection due to Staphylococcus aureus [both methicillin-susceptible S. aureus (MSSA) and methicillin-resistant S. aureus (MRSA)] and/or coagulase-negative staphylococci (CoNS) and to compare it to standard of care (SOC).

Start Date20 Feb 2019

Sponsor / Collaborator

Debiopharm International SA

NCT03209648

/ CompletedPhase 1

A Phase 1, Open-Label, Fixed Sequence Study to Investigate the Effect of Itraconazole on the Pharmacokinetics of Debio 1450 in Healthy Subjects

Debio 1450 is metabolised mainly by CYP3A4, therefore inhibitors of CYP3A4 have the potential to raise Debio 1450 plasma concentrations. Hence, it is important to determine the effect of CYP3A4 inhibition by itraconazole on the Pharmacokinetics of Debio 1450.

Start Date14 Jun 2017

Sponsor / Collaborator

Debiopharm International SA

100 Clinical Results associated with Afabicin diolamine

100 Translational Medicine associated with Afabicin diolamine

100 Patents (Medical) associated with Afabicin diolamine

Literatures (Medical) associated with Afabicin diolamine

01 Apr 2026·ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Model-based quantification of immune response and anti-staphylococcal activity of afabicin in immunocompetent mouse thigh infections to enable predictions of clinical efficacy

Article

Author: Nicolas-Métral, Valérie ; Nielsen, Elisabet I. ; Cameron, David R. ; Menetrey, Annick ; Friberg, Lena E. ; Saporta, Raphaël

ABSTRACT:

This study aimed to describe the immune response and activity of the novel antibiotic afabicin against Staphylococcus aureus in an immunocompetent mouse thigh infection model using PKPD modeling and to predict the clinical efficacy of different afabicin dosing regimens in Staphylococcus -infected immunocompetent patients. Bacterial counts of five Staphylococcus aureus strains were determined over 74 h in an immunocompetent mouse thigh infection model. Afabicin doses of 0.011–150 mg/kg were administered intraperitoneally every 6 h. A PKPD model was developed to describe immune response and afabicin desphosphono (active moiety) activity. The model was used jointly with a human population PK model for afabicin to predict the efficacy of different clinical dosing regimens (intravenous 55 to 160 mg twice-daily or oral 80 to 240 mg twice-daily) in immunocompetent patients. The developed model included a saturable neutrophil-mediated phagocytosis process of bacteria. The afabicin desphosphono effect was characterized using a model structure previously developed based on in vitro time-kill and neutropenic mouse thigh infection data. A lower maximum killing rate constant (0.24 h −1 ) and an 82% lower EC 50 were estimated for immunocompetent animals compared to in vitro . Predictions indicated that all tested afabicin regimens would achieve bacterial killing in immunocompetent patients infected with S. aureus . Afabicin activity against five S. aureus strains was adequately quantified in immunocompetent animals by the developed PKPD model. Predictions supported the efficacy of afabicin 55 mg intravenously twice daily, followed by an 80 mg oral twice-daily regimen in humans, which is currently tested in a clinical trial in bone and joint infections.

02 Dec 2024·JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Model-based translation of results from in vitro to in vivo experiments for afabicin activity against Staphylococcus aureus

Article

Author: Nielsen, Elisabet I ; Friberg, Lena E ; Menetrey, Annick ; Nicolas-Metral, Valérie ; Cameron, David R ; Saporta, Raphaël

Abstract:

Background:

Translation of experimental data on antibiotic activity typically relies on pharmacokinetic/pharmacodynamic (PK/PD) indices. Model-based approaches, considering the full antibiotic killing time course, could be an alternative.

Objectives:

To develop a mechanism-based modelling framework to assess the in vitro and in vivo activity of the FabI inhibitor antibiotic afabicin, and explore the ability of a model built on in vitro data to predict in vivo outcome.

Methods:

A PK/PD model was built to describe bacterial counts from 162 static in vitro time–kill curves evaluating the effect of afabicin desphosphono, the active moiety of the prodrug afabicin, against 21 Staphylococcus aureus strains. Combined with a mouse PK model, outcomes of afabicin doses of 0.011–190 mg/kg q6h against nine S. aureus strains in a murine thigh infection model were predicted, and thereafter refined by estimating PD parameters.

Results:

A sigmoid Emax model, with EC50 scaled by the MIC described the afabicin desphosphono killing in vitro. This model predicted, without parameter re-estimation, the in vivo bacterial counts at 24 h within a ±1 log margin for most dosing groups. When parameters were allowed to be estimated, EC50 was 38%–45% lower in vivo, compared with in vitro, within the studied MIC range.

Conclusions:

The developed PK/PD model described the time course of afabicin activity across experimental conditions and bacterial strains. This model showed translational capacity as parameters estimated on in vitro time–kill data could well predict the in vivo outcome for a wide variety of doses in a mouse thigh infection model.

02 Aug 2023·The Journal of antimicrobial chemotherapy

Evaluation of the microbiota-sparing properties of the anti-staphylococcal antibiotic afabicin

Article

Author: Kühn, J ; Nicolas-Metral, V ; Le Vacon, F ; Nowakowska, J ; Wittke, F ; Le Fresne-Languille, S ; Vuagniaux, G ; Amouzou, Y ; Carton, T ; De Martino, A ; Leuillet, S ; Chaves, R L ; Cameron, D R

Abstract:

Background:

Antibiotic use is associated with collateral damage to the healthy microbiota. Afabicin is a first-in-class prodrug inhibitor of the FabI enzyme that, when converted to the pharmacologically active agent afabicin desphosphono, demonstrates a staphylococcal-specific spectrum of activity. An expected benefit of highly targeted antibiotics such as afabicin is microbiome preservation.

Objectives:

To compare the effects of oral treatment with afabicin and standard-of-care antibiotics upon the murine gut microbiota, and to assess the effects of oral afabicin treatment on the human gut microbiota.

Methods:

Gut microbiota effects of a 10 day oral course of afabicin treatment were monitored in mice and compared with clindamycin, linezolid and moxifloxacin at human-equivalent dose levels using 16S rDNA sequencing. Further, the gut microbiota of healthy volunteers was longitudinally assessed across 20 days of oral treatment with afabicin 240 mg twice daily.

Results:

Afabicin treatment did not significantly alter gut microbiota diversity (Shannon H index) or richness (rarefied Chao1) in mice. Only limited changes to taxonomic abundances were observed in afabicin-treated animals. In contrast, clindamycin, linezolid and moxifloxacin each caused extensive dysbiosis in the murine model. In humans, afabicin treatment was not associated with alterations in Shannon H or rarefied Chao1 indices, nor relative taxonomic abundances, supporting the findings from the animal model.

Conclusions:

Oral treatment with afabicin is associated with preservation of the gut microbiota in mice and healthy subjects.

News (Medical) associated with Afabicin diolamine

15 Oct 2024

·www.debiopharm.com

Debiopharm to Showcase Research Results of Their First-In-Class Anti-Staphylococcal Program at IDWeek 2024 in Los Angeles

Share Debiopharm to present at the Rapid Fire session on Challenging Bacterial Infections, the latest data for afabicin, first-in-class, pathogen-specific FabI inhibitor antibiotic with clinically demonstrated activity against antibiotic-resistant staphylococcus infections and microbiome sparing potential. Lausanne, Switzerland – Debiopharm (www.debiopharm.com), a privately-owned, Swiss-based biopharmaceutical company aiming to establish tomorrow’s standard-of-care to cure cancer and infectious diseases, today announced preclinical and clinical data releases for the afabicin (Debio 1450) antibiotic program during the 2024 IDWeek summit in Los Angeles, California. “With the global demographic shift, healthcare practitioners are likely to experience more and more patients with bone and joint infections (BJIs), particularly involving prosthetic devices. Staphylococcus aureus is the most prevalent microorganism involved in BJIs and is notorious for its ability to become resistant to widely used antibiotics, including newer agents. With the phase 2 results I will be presenting, physicians may question themselves further on whether it’s still a smart choice to use wide-spectrum antibiotics.” – Dr. Alireza Shamaei-Tousi, Principal Clinical Scientist at Debiopharm Thu, October 17th Poster display: 12:15-12:45pm Rapid Fire Session: Challenging Bacterial Infections Results from A Phase 2 Clinical Trial for Treatment of Bone And Joint Infections with Afabicin, A First-in-Class Selective Anti-Staphylococcal Antibiotic Alireza Shamaei-Tousi, Principal Clinical Scientist Fri, October 18th Poster display: 12:15-1:30pm Poster Session: PK/PD Studies Assessment of Pharmacokinetic-Pharmacodynamic (PK-PD) Target Attainment for the Anti-Staphylococcal Antibiotic Afabicin David Cameron, Senior Scientist, Translational Pharmacology Sat, October 19th Poster display: 12:15-1:30pm Poster Session: Basic Science and Translational Studies The First-in-Class Anti-Staphylococcal Antibiotic Afabicin Desphosphono is Not Associated With Clostridioides difficile Infection in an in vitro Human Gut Model David Cameron, Senior Scientist, Translational Pharmacology Bone and joint infections are a group of diseases that include osteomyelitis, septic arthritis and prosthetic joint infections affecting over 30,000 people per year within the US, UK, France, Germany, Spain and Italy combined. These conditions are associated with significant global morbidity, and in certain circumstances, mortality. Staphylococci are the most common causative bacteria, identified in 30 to 70% of the cases. Debiopharm aims to develop innovative therapies that target high unmet medical needs in oncology and bacterial infections. Bridging the gap between disruptive discovery products and real-world patient reach, we identify high-potential compounds and technologies for in-licensing, clinically demonstrate their safety and efficacy, and then select large pharmaceutical commercialization partners to maximize patient access globally. For more information, please visit www.debiopharm.com We are on X. Follow us @DebiopharmNews at http://twitter.com/DebiopharmNews or on LinkedIn

Phase 2Clinical ResultQualified Infectious Disease Product

27 Aug 2024

·www.businesswire.com

Debiopharm Underlines Commitment to Eradicating Antimicrobial Resistance by Sponsoring the 8th Annual World AMR Conference

LAUSANNE, Switzerland--( BUSINESS WIRE )--Debiopharm ( www.debiopharm.com ), a Swiss-based, global biopharmaceutical company, aiming to establish tomorrow’s standard-of-care to cure cancer and infectious diseases, announced today their participation in the 2024 World AMR conference from September 5 th -6 th in Philadelphia, Pennsylvania, USA. For the last decade, Debiopharm has been committed to developing new antimicrobials for patients by conducting research on a novel class of antibiotics that target hard-to-treat infections, caused by WHO priority pathogens. Now in its third year of sponsoring World AMR, Debiopharm is proud to support the conference’s mission to unite key decision-makers in AMR from international government bodies, policy organizations, and the healthcare sector to meet, discuss, and formulate initiatives to tackle the emerging threat of AMR effectively. This year, Debiopharm’s Head of Global Value & Access, Jennifer Quinn, will present within the Impact, Policy and Awareness Track and lead a roundtable discussion on how to move the needle on fair reimbursement for antibiotics. Focused on actionable ways to leverage current reimbursement models, Jennifer’s presentation will outline a tangible framework for payer negotiations and discuss evidence needs for products that will reach the market before ‘pull incentives’ become available. “We’re looking forward to open discussions and networking opportunities with public organizations and other infectious disease industry experts to put into place practical solutions to combat the reimbursement challenged that help to fuel AMR.” – Jennifer Quinn, Head of Global Value & Access . World AMR 2023 Session details Congress agenda Speaker Presentation Sept. 5 th 11:20AM EST How can current reimbursement models be leveraged while waiting for 'pull incentives'? Jennifer Quinn, Head of Global Value & Access Roundtable discussion Sept. 5 th 01:30PM EST What data is needed to fit current payer evidence requirements and how can we generate it? Jennifer Quinn, Head of Global Value & Access About afabicin Afabicin (Debio 1450) is Debiopharm’s first-in-class FabI inhibitor , selectively targeting Staphylococcus ’ essential bacterial fatty acid biosynthesis pathway. Afabicin is active against Staphylococcus spp., of which methicillin-resistant Staphylococcus aureus (MRSA) strains are high on the WHO global priority pathogen list and deemed a “serious threat” by the CDC. Afabicin can be administered orally or intravenously. Promising results have been obtained in a comparative double-blind Phase 2 trial with afabicin in acute bacterial skin and skin structure infections. Currently, a global Phase 2 trial in bone and joint infections is being conducted, comparing afabicin to standard antibiotics. About Debio 1453 Analogous to afabicin, the preclinical compound Debio 1453 is a potential first-in-class pathogen-specific drug targeting the essential bacterial fatty acid biosynthesis pathway. Debio 1453 has been developed as an oral drug with activity against. Neisseria gonorrhoeae , the bacteria causing the sexually transmitted disease gonorrhea. Untreated gonorrhea can cause serious and permanent health issues including infertility, ectopic pregnancy, long-term pelvic/abdominal pain, blindness in newborns and in rare cases also have a lethal outcome. Debiopharm’s fight against antimicrobial resistance Debiopharm, an innovation-focused, Swiss biopharmaceutical company is one of the few privately owned companies developing novel class antibiotics to combat hard-to-treat infections. Through their unique partnership-based business model, the company is advancing pathogen-specific antibiotics from early stage through phase II clinical research with afabicin, specifically targeting staphylococci. As a result of high selectivity, FabI inhibitors specifically target selected pathogens, and potentially preserve intestinal microbiota. Debiopharm’s FabI inhibitors meet all four WHO 2020 innovation criteria: new chemical class, new target, new mode of action and no cross-resistance to other antibiotic classes. For more information, please visit www.debiopharm.com We are on X. Follow us @DebiopharmNews at http://twitter.com/DebiopharmNews Sources Antimicrobial Resistance Collaborators. (2022). Global burden of bacterial antimicrobial resistance in 2019: a systematic analysis. The Lancet; 399(10325): P629-655.

Phase 2Qualified Infectious Disease Product

06 Sep 2023

·www.biospace.com

Debiopharm Joins Discussions With International Health Organisations to Fight Anti-Microbial Resistance at the 2023 World AMR Congress

The rapid growth of antimicrobial resistance (AMR) is staggering, particularly when considering the slow rate at which new antibiotics are being developed and made available to patients1 International health authorities, including the World Health Organization (WHO) and the U.S. Centers for Disease Control and Prevention (CDC), continue to sound the alarm to promote increased preparedness, save human lives and avoid a heavy financial burden on healthcare systems2,3 Debiopharm is one of the main sponsors and panel participants of the 2023 World Antimicrobial Resistance (World AMR) Congress in Philadelphia, Pennsylvania — a conference gathering key AMR stakeholders including international government agencies, policy associations, and healthcare industry professionals LAUSANNE, Switzerland--(BUSINESS WIRE)-- Debiopharm ( ), a privately-owned, Swiss-based, biopharmaceutical company aiming to establish tomorrow’s standard-of-care to cure cancer and infectious diseases, today announced their participation in the keynote panel and antibiotic development track sessions at the 2023 World AMR conference from September 7th – 8th, 2023. Debiopharm’s panelist Morgane Vanbiervliet, Market Intelligence & Business Development Manager, Infectious Diseases, is part of the AMR preparedness keynote panel to be moderated by Bruce Y. Lee from Forbes and involving representatives from the CDC, Menarini Group, IFPMA and the AMR Action Fund. A further Debiopharm-sponsored breakout session, moderated by Dr. Ricardo Chaves, Executive Medical Director, will feature Dr. L. Clifford McDonald, Associate Director for Science in the Division of Healthcare Quality Promotion at the CDC, explaining the relevance of novel microbiome-sparing antibiotics in combating AMR, and the potential need for new regulatory approval and reimbursement pathways.* “It’s important to harness these open dialogues between public organizations and the infectious disease industry experts at World AMR to produce action that can prepare us to face the emerging wave of resistant infections,” explained Morgane Vanbiervliet, Market Intelligence & Business Development Manager, Infectious Diseases, Debiopharm. “We know that uncontrollable infectious diseases are everybody’s business, and that our preparation efforts must involve the reinforcement of prevention measures, better stewardship education, and sustainable market pathways for new effective treatments.” “The CDC recognizes the importance of the human microbiome as it provides key resistance to human colonization with multidrug-resistant pathogens. Along with products that will reduce the degree of colonization (i.e. pathogen reduction), or drugs that will restore the microbiome, we need therapeutic antibiotics that spare the microbiome, by being highly-selective for only specific pathogens.” expressed Dr. L. Clifford McDonald, Associate Director for Science in the Division of Healthcare Quality Promotion, CDC. Last year’s special report from the CDC on the impact of COVID-19 on antimicrobial resistance revealed that 6 of the 18 most alarming bacterial menaces cost the US more that $4.6 billion each year and thousands of human lives.4 The agency’s 18 bacterial and fungal threats include 2 pathogens for which Debiopharm is currently developing new antibiotics: Neisseria gonorrhoeae and methicillin-resistant Staphylococcus aureus. Debiopharm’s FabI inhibitor therapies are part of a new pathogen-specific antibiotic class that is being researched for its capacity to effectively treat a single type of bacteria and thereby preserve the microbiome and avoid subsequent spread of AMR. World AMR 2023 Session details Congress agenda Speakers Keynote panel Sept. 7th 08:35 EST How can we push AMR to the forefront of preparedness? Morgane Vanbiervliet, Market Intelligence & Business Development Manager, Infectious Diseases, Debiopharm + other invited speakers Panel discussion Sept. 7th 11:00–11:30 EST Antibiotic Development stream The public health case for microbiome-sparing antibiotics: Potential need for new pathways in regulatory approval and reimbursement Moderator: Dr. Ricardo Chaves Executive Medical Director Debiopharm Speaker: Dr.L. Clifford McDonald, Associate Director for Science in the Division of Healthcare Quality Promotion, CDC About afabicin Afabicin (Debio 1450) is Debiopharm’s first-in-class FabI inhibitor against Staphylococcus spp., whose methicillin-resistant Staphylococcus aureus (MRSA) strains are high on the WHO global priority pathogen list and deemed a “serious threat” by the CDC. Afabicin can be administered orally or IV and selectively targets Staphylococcus’ essential bacterial fatty acid biosynthesis. Promising results have been obtained in a comparative double-blind Phase 2 trial with afabicin in acute bacterial skin and skin structure infections. Currently, a Phase 2 trial in bone and joint infections is being conducted in several countries comparing afabicin to standard antibiotics. About Debio 1453 Analogous to afabicin, the preclinical compound Debio 1453 is a potential first in class pathogen-specific drug targeting the essential bacterial fatty acid biosynthesis pathway. Debio 1453 is administered orally to treat Neisseria gonorrhoeae, the bacteria causing the sexually transmitted disease gonorrhea, a cause of serious and permanent health issues including infertility, ectopic pregnancy, cardiovascular and neurological problems. Debiopharm’s fight against antimicrobial resistance Debiopharm, an innovation-focused, Swiss biopharmaceutical company is one of the few privately owned companies developing novel class antibiotics to combat hard-to-treat infections. Through their unique partnership-based business model, the company is advancing pathogen-specific antibiotics from early stage through phase II clinical research with afabicin, specifically targeting staphylococci, being the most clinically advanced for the treatment of bone and joint infections. As a result of high selectivity, FabI inhibitors specifically target selected pathogens while preserving intestinal microbiota and meet all four WHO 2020 innovation criteria: new chemical class, new target, new mode of action and no cross-resistance to other antibiotic classes. For more information, please visit We are on Twitter. Follow us @DebiopharmNews at References [1] Morrison L, Zembower TR. Antimicrobial resistance. Gastrointest Endosc Clin N Am. 2020 Oct;30(4):619-635. [2] Antimicrobial resistance surveillance in Europe 2023–2021 data. [3] CDC Antibiotic resistance threats in the United States, 2019. [4] COVID-19 U.S. Impact on Antimicrobial Resistance. Disclosures * Speaker disclosures: Dr. McDonald has no relevant financial or non-financial relationships to disclose. The findings and conclusions of this presentation are those of the author and do not necessarily represent the official position of the Centers for Disease Control and Prevention or the U.S. Department of Health and Human Services. Any use of trade names and commercial sources is for identification only and does not imply endorsement by the Centers for Disease Control and Prevention or the U.S. Department of Health and Human Services. View source version on businesswire.com: Contacts Debiopharm Contact Dawn Bonine Head of Communication dawn.bonine@debiopharm.com Tel: +41 (0)21 321 01 11 Source: Debiopharm View this news release online at:

Phase 2

100 Deals associated with Afabicin diolamine

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R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Arthritis	Phase 2	United States	Debiopharm International SA	20 Feb 2019
Arthritis	Phase 2	South Africa	Debiopharm International SA	20 Feb 2019
Arthritis	Phase 2	Ukraine	Debiopharm International SA	20 Feb 2019
Bone and joint infections	Phase 2	United States	Debiopharm International SA	20 Feb 2019
Bone and joint infections	Phase 2	South Africa	Debiopharm International SA	20 Feb 2019
Bone and joint infections	Phase 2	Ukraine	Debiopharm International SA	20 Feb 2019
Skin Diseases, Bacterial	Phase 2	United States	Debiopharm International SA	01 May 2015
Skin Diseases, Infectious	Phase 2	-	GSK Plc	-
Soft Tissue Infections	Phase 2	-	GSK Plc	-
Bone Diseases, Infectious	Phase 1	United States	Debiopharm International SA	01 Apr 2016

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02426918 (CTgov)	Phase 2	Skin Diseases, Bacterial	330	Debio 1450 (Debio 1450 80 mg/120 mg BID)	shpshizigl = ogdzuhscid uevlpofmmq (ztahzphtpg, grfspfduxa - oweovgnmtf) View more	-	13 Nov 2019
				Debio 1450 (Debio 1450 160 mg/240 mg BID)	shpshizigl = sbjwbuewxy uevlpofmmq (ztahzphtpg, psvjfygstn - quhmupzmvt) View more

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