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Science

F25 works by selectively inhibiting MCT4, a key transporter that cancer cells use to export lactate produced during high rates of glycolysis. By blocking this lactate efflux, F25 disrupts the tumor’s metabolic balance, leading to intracellular acidification and ultimately triggering cell death. This targeted approach not only weakens cancer cells but also enhances the effectiveness of other treatments when used in combination.

Lactic Acid Metabolism Mode

It is metabolized differently in tumor cells than in normal cells:

  1. Glucose metabolism consists mainly of glycolysis and the tricarboxylic acid (TCA) cycle in the mitochondria. 

  2. Normal cells produce energy mainly through the TCA cycle under well-oxygenated conditions and produce large amounts of lactate under hypoxic conditions. 

  3. Tumor cell glycolysis produces large amounts of lactate, which is transported to the tumor microenvironment (TME) via monocarboxylic acid transport protein 4 (MCT4). 

  4. Lactate can then be transported into oxidative tumor cells using monocarboxylate transporter protein 1 (MCT1) as fuel and generate energy through oxidative phosphorylation. â€‹

What makes FlyNew F25 inhibitor different?

FlyNew F25 MCT4 Inhibitor

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  1. High selectivity: FlyNew F25 exhibits high selectivity with minimal impact on normal cells 

  2. Optimization success: F25 demonstrates an excellent pharmacokinetic profile with improved water solubility and efficient metabolism via hepatic enzymes.

  3. First-in-class MCT4 inhibitor targeting tumor metabolism 

  4. ​May be granted Fast Track Designation (FTD) and Orphan Drug Designation (ODD) Combination by the U.S. FDA

  5. Induces tumor cell death by blocking lactate efflux, reducing the risk of drug resistance 

  6. Particularly effective for cancers with high lactate expression 

  7. Compatible with existing therapies, offering potential for combination treatment​

Other MCT4 Inhibitor 

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  1. Low Selectivity: Most inhibitors act on both MCT1/MCT4

  2. Poor Stability: Rapid metabolism in vivo, short half-life biology

  3. Low Utilization: Limited tissue distribution 

  4. Limited Clinical Development: No approved products on the market yet​

Pioneering Solutions for Cancer Treatment

SUMMARY

  1. MCT4 small molecule inhibitors show remarkable anticancer potential by interfering with tumor metabolism and improving the immune microenvironment. 

  2. FlyNew F25 MCT4 inhibitors are currently in preclinical research and have a promising application in combination therapy. 

  3. Future studies should focus on improving the selectivity and safety of the drugs and exploring their clinical applications in different tumor types to promote the further development of this field. â€‹

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