Macrocycle Therapeutics to Treat Life-threatening Diseases

Area of Science:

• Drug discovery and development
• Antibacterial agents
• Oncology therapeutics

Background:

• Gram-negative bacteria pose significant therapeutic challenges.
• Targeting outer membrane proteins offers a novel strategy against these pathogens.
• Neutrophil elastase and CXCR4 are implicated in various diseases.

Purpose of the Study:

• To highlight the capabilities of Polyphor's macrocycle platform.
• To introduce novel antibiotics targeting Gram-negative bacteria.
• To present POL6014 (neutrophil elastase inhibitor) and balixafortide (CXCR4 inhibitor).
• To report on the clinical development of balixafortide in combination therapy.

Main Methods:

• Leveraging a macrocycle drug discovery platform.
• Identifying and developing small molecule inhibitors.
• Conducting preclinical and clinical trials for drug candidates.

Main Results:

• Discovery of novel antibiotics effective against Gram-negative bacteria.
• Development of POL6014 and balixafortide.
• Balixafortide in combination with eribulin is in Phase III clinical trials for advanced metastatic HER2-negative breast cancer.

Conclusions:

• Polyphor's platform is effective for discovering diverse therapeutic agents.
• The platform yields novel antibiotics and inhibitors for significant unmet medical needs.
• Balixafortide represents a promising therapeutic candidate in oncology.