TSRL, Inc. Awarded $3 Million NIH Grant to Develop a First-in-Class Oral Antibiotic

April 25, 2023, ANN ARBOR, MICHIGAN — TSRL, Inc., a privately held preclinical accelerator, announced today that the company was awarded a Phase IIB Small Business Technology Transfer (SBIR) grant from the National Institute of Allergy and Infectious Diseases (NIAID) of the National Institute of Health (NIH).

TSRL and its collaborators from the University of Washington were awarded $3 million over the next three years to conduct a successful development program that will be the foundation for an Investigational New Drug (IND) application for MRS-2541 (the lead candidate emerging from research conducted under our previous Phase II SBIR grant).

Acute bacterial skin and skin structure infections (ABSSSIs) pose a significant healthcare challenge in the United States, with over 14 million visits to ambulatory and hospital institutions each year. Considering this alarming statistic, our previous research has unveiled a novel antibiotic, MRS-2541, which exhibits a unique mechanism of action (MOA) and the potential for oral administration and would represent a major breakthrough in the treatment of Gram+ infections.

Traditionally, vancomycin has been the preferred treatment for hospitalized patients with ABSSSIs. However, rates of resistance or intermediate resistance to Staphylococcus aureus (SA) strains, which have now surpassed 5% and continue to climb, have now shed light on the urgent need for alternative therapeutic options.

Our extensive research has resulted in the revelation of MRS-2541, a novel small-molecule antibiotic. MRS-2541 exhibits a unique MOA by inhibiting the bacterial methionyl-tRNA synthetase enzyme (MRS), which is necessary for protein synthesis. Therefore, additional lead characterization studies will still be required to advance the lead candidate toward an IND application. This research holds the potential to revolutionize the treatment landscape for ABSSSIs, offering patients and healthcare professionals a much-needed alternative to addressing these complex infections.

About TSRL, Inc.:

TSRL, Inc. is a preclinical biotech accelerator. We collaborate with partners in academia and industry to develop early-stage therapeutics and drug delivery technologies. In these collaborations, we provide infrastructure, drug development expertise, and access to non-dilutive funding. Our portfolio holds promising lead-stage therapeutics. We are actively looking for new technologies and strategic partnerships. More information about TSRL, Inc. and portfolio technologies are available at http://www.tsrlinc.com or can be requested by contacting Elke Lipka, CEO, elipka@tsrlinc.com

TSRL, Inc. awarded NIH Grant to Discover Novel, Safe, Efficacious Heparin Reversal Therapy

Ann Arbor, Michigan, December 8th, 2022 – TSRL, Inc., a privately-held preclinical accelerator, announced that in September the company was awarded a Phase I Small Business Innovation Research (SBIR) grant from the National Heart, Lung, and Blood Institute (NHLBI) of the National Institute of Health (NIH).

TSRL and its collaborators from the University of Michigan and the University of British Columbia were awarded close to $400,000 to generate critical in vivo proof-of-concept data over the next year to de-risk their lead, second-generation, heparin-reversal therapeutic toward clinical development.

“We are excited to work with this world-class team on the development of a completely novel dendrimer-based therapy approach to rapidly restore blood clotting function when needed in a variety of conditions that require temporary or chronic heparin therapy.”

— TSRL’s CEO, Elke Lipka, PhD, MBA

Anticoagulants and their reversal agents are crucial for managing unwarranted blood clotting (i.e. thrombosis). Heparin is used for thrombosis prevention in multiple clinical indications, including procedures such as catheter ablation and cardiopulmonary bypass, after which heparin’s anticoagulant activity requires prompt neutralization.

Protamine sulfate, the only FDA-approved reversal agent for heparin, is a 60-year-old drug with a Black Box Warning. Its clinical use is constrained by two major limitations:

1. Requirement of titration because of its very narrow therapeutic safety window.

2. Potentially life-threatening hypersensitivity reactions or anaphylaxis manifesting as severe hypotension, cardiovascular collapse, pulmonary edema, pulmonary vasoconstriction, and pulmonary hypertension.

Thus, there is a large unmet medical need to discover and develop novel heparin reversal agents with a wider therapeutic window and better safety profile.

“Jay Kizhakkedathu, Ph.D. and colleagues at the University of British Columbia have developed a novel, safe drug platform that allows for safely blocking the action of all types of heparin – even low molecular weight heparins that currently lack an effective reversal agent. It is exciting to work with them and TSRL scientists to bring this promising drug candidate closer to the clinic.”

— James H. Morrisey, Ph.D. TSRL’s collaborator PI at the Univeristy of Michigan

About TSRL, Inc.:

TSRL, Inc. is a preclinical biotech accelerator. We collaborate with partners in academia and industry to develop early-stage therapeutics and drug delivery technologies. In these collaborations, we provide infrastructure, drug development expertise, and access to non-dilutive funding. Our portfolio holds promising lead-stage therapeutics. We are actively looking for new technologies and strategic partnerships. More information about TSRL, Inc. and portfolio technologies are available at http://www.tsrlinc.com or can be requested by contacting Elke Lipka, CEO, elipka@tsrlinc.com