Qpex Biopharma to Provide First Public Presentations of Preclinical Data on the Novel Ultra-Broad-Spectrum Beta-lactamase Inhibitor QPX7728 for IV and Oral Products at 2019 ASM Microbe Meeting

SAN DIEGO, June 13, 2019 /PRNewswire/ -- Qpex Biopharma today announced that preclinical data on its investigational beta-lactamase inhibitor QPX7728 will be featured in several presentations at the 2019 ASM Microbe Meeting to be held June 20-24 in San Francisco, CA.

"We are pleased to be making the first public presentations on our next generation beta-lactamase inhibitor QPX7728 that exceeds the profile of other agents recently approved or in clinical development." said Michael Dudley, PharmD, President and CEO of Qpex Biopharma. "QPX7728's potent inhibition of major beta-lactamases, including metallo enzymes, and activity in multi-drug resistant Acinetobacter as well as Enterobacteriaceae and Pseudomonas aeruginosa represents a major advance in the field. QPX7728 has the potential for use in combination with multiple beta-lactam antibiotics, including oral agents."

Eight presentations on the discovery, microbiological properties, and preclinical pharmacology of the clinical candidate beta-lactamase inhibitor QPX7728 will be provided by Qpex scientists and external collaborators. Data show that QPX7728 has potent inhibition of clinically important beta-lactamases from Classes A, B, C, and D that are often present in multi-drug resistant (MDR) bacteria. Notably, QPX7728 activity is minimally affected by resistance mechanisms that impede entry of antibiotics or other beta-lactamase inhibitors into bacteria. In preclinical species, QPX7728 has excellent pharmacokinetic properties, including oral bioavailability. Of note, the company will summarize data on QPX7728 in an oral presentation session that showcases important new antimicrobial agents in early development.

In addition to QPX7728 presentations, Qpex will present a summary of its pipeline, including QPX7728 and the company's next generation polymyxin program that are part of its BARDA portfolio collaboration, in a separate oral presentation session.

The American Society for Microbiology's ASM Microbe 2019 showcases the best microbial sciences in the world, and provides a one-of-a-kind forum to explore the complete spectrum of microbiology from basic science to clinical trials.

The Qpex Biopharma presentations are listed below; additional information may be found at the ASM Microbe 2019 website at https://www.asm.org. All times listed below are in Pacific Daylight Time.

Date: Friday, June 21, 2019
Presentation Title: Broad-Spectrum Orally Bioavailable Beta-lactamase Inhibitor QPX7728
Presenter: Olga Lomovskaya, PhD, Qpex Biopharma
Oral Session: S020- New Agents Discovery Summary Session: Early New Antimicrobial Agents
Time: 9:10am-9:30am
Place: 207/208 South
Summary: The discovery and microbiological properties of QPX7728, an ultra-broad-spectrum beta-lactamase inhibitor with inhibitory activity against clinically important enzymes in Classes A-D in drug-resistant Enterobacteriaceae, Pseudomonas, and Acinetobacter spp. will be reviewed.

Date: Saturday, June 22, 2019
Presentation Title: Qpex Biopharma Pipeline
Presenter: David Griffith, Qpex Biopharma
Oral Session: Pharma Pipeline Updates: Part 2
Time: 11:33am-11:44am
Place: AAR Track Hub (Booth 5053) - Learn - Exhibit and Poster Hall
Summary: A corporate overview of Qpex Biopharma and its development pipeline will be reviewed.

Date: Sunday, June 23, 2019
Poster Session: P588 - AAR08 - New Antimicrobial Agents (pre-Phase 2): Early Beta-Lactams and Beta-Lactamase Inhibitor Combinations
Time: 10:30am-4:00pm
Place: Exhibit and Poster Hall
Presentation Titles (abstract numbers), authors, and summary:

Discovery of QPX7728, an Ultra-Broad-Spectrum Inhibitor of Serine and Metallo Beta-lactamases (AAR706)
Scott J. Hecker, K. Raja Reddy, Olga Lomovskaya, David C. Griffith, Debora Rubio-Aparicio, Kirk Nelson, Ruslan Tsivkovski, Dongxu Sun, Mojgan Sabet, Ziad Tarazi, Maxim Totrov, Orville Pemberton, Yu Chen, and Michael N. Dudley
The path to discovery of the ultra-broad-spectrum beta-lactamase inhibitor QPX7728, including an overview of microbiology and structural biology, will be described.

QPX7728: Spectrum of Beta-Lactamase Inhibition and Impact of Resistance Mechanisms on Activity in Gram-Negative Bacteria (AAR-707)
Olga Lomovskaya, Debora Rubio-Aparicio, Kirk Nelson, Dongxu Sun and Michael Dudley
QPX7728 restores activity of multiple beta-lactam antibiotics in bacteria producing class A, C and D serine BLs, including class D carbapenemases from Acinetobacter, and major class B metallo-beta-lactamases. Excellent activity is observed in pathogens with multiple porin mutations and is not affected by efflux pumps.

QPX7728: Biochemical Characterization of Inhibitory Activity against Serine and Metallo beta-lactamases from Enterobacteriaceae and Acinetobacter (AAR-708)
Ruslan Tsivkovski and Olga Lomovskaya
QPX7728 is a potent reversible inhibitor of serine and metallo-beta-lactamases. It shows slow, tight-binding inhibition of serine beta-lactamases with high enzyme inactivation efficiency and low off-rate with residence times reaching values of several hours for some enzymes.

QPX7728: In Vitro Activity in Combination with Meropenem against Carbapenem-Resistant Enterobacteriaceae (CRE) (AAR-709)
Kirk Nelson, Debora Rubio-Aparicio, and Olga Lomovskaya
QPX7728 restored the potency of meropenem against CRE, with >95% of strains inhibited by QPX7728 + meropenem. Outer membrane porin mutations that restrict entry of many drugs had a lower effect on QPX7728 + meropenem compared to other recently approved beta-lactamase inhibitor combination products.

QPX7728: In Vitro Activity in Combination with Oral Beta-Lactam Antibiotics against Enterobacteriaceae (ENT) (AAR-710)
Debora Rubio-Aparicio, Kirk Nelson, David C. Griffith, Michael N. Dudley, and Olga Lomovskaya
QPX7728 enhanced the potency of the oral beta-lactam antibiotics ceftibuten and tebipenem against Enterobacteriaceae with the ESBL phenotype as well as CRE (including KPC, OXA-48-like, and MBL producing strains).
 

In Vitro Activity of the β-lactamase Inhibitor QPX7728 Combined with Several β-lactams When Tested against Acinetobacter baumannii (AB) and Pseudomonas aeruginosa (PA) (AAR-711)
Mariana Castanheira, Jill Lindley, Kirk Nelson, Debora Rubio-Aparicio, and Olga Lomovskaya
QPX7728 restored the potency of meropenem against carbapenem- resistant Acinetobacter baumannii, with >90% of isolates were inhibited by ≤8 µg/ml of meropenem with QPX7728 (at 4 or 8 µg/ml). In Pseudomonas, QPX7728 combinations showed high potency against a representative panel that reflects current MIC distributions for clinical isolates; in highly meropenem, ceftazidime-avibactam and ceftolozane-tazobactam resistant isolates, QPX7728 combined with meropenem or ceftolozane were the most potent combinations.

In Vivo Activity of QPX7728 in Combination with Meropenem against Carbapenem-resistant K. pneumoniae, A. baumannii, and P. aeruginosa (AAR-712)
Mojgan Sabet, Ziad Tarazi, and David C. Griffith
QPX7728 plus meropenem produces dose-dependent bacterial killing of carbapenem-resistant Enterobacteriaceae (CRE), A. baumannii, and P. aeruginosa in mouse models of infection. 

Pharmacokinetics of QPX7728 following IV Dosing in Non-Clinical Species (AAR-713)
Ziad Tarazi, Mojgan Sabet, Jonathan Parkinson, and David C. Griffith
The pharmacokinetics of QPX7728 following IV dosing in non-clinical species show properties consistent with co-administration with beta-lactam antibiotics.

About Qpex Biopharma, Inc.
Qpex Biopharma (www.qpexbio.com) is a San Diego-based biopharmaceutical company with a pipeline of best-in-class agents addressing critical needs for treatment of infectious diseases in the inpatient and outpatient settings. Qpex was launched in October 2018 with investments from New Enterprise Associates, Adams Street Partners, LYZZ Capital, Hatteras Venture Partners and Stanford University Draper Fund. The company's scientists and clinicians have a record of deep expertise in the discovery and development of anti-infective agents, and an extensive record of working with public-private partnerships, including a previous contract with the Biomedical Advanced Research and Development Authority (BARDA) that led to the first approved antimicrobial drug product under that program in 2017.