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ALS-4 is a first-in-class, orally administered small molecule anti-virulence drug being developed by Aptorum Group Limited for the treatment of infections caused by Staphylococcus aureus, including methicillin-resistant Staphylococcus aureus (MRSA). Unlike traditional bactericidal antibiotics, ALS-4 employs a novel mechanism by inhibiting dehydrosqualene desaturase (CrtM), an enzyme essential for the biosynthesis of staphyloxanthin. Staphyloxanthin is a golden carotenoid pigment that protects the bacteria from oxidative stress and host immune responses, such as reactive oxygen species (ROS) produced by neutrophils. By blocking the production of this pigment, ALS-4 renders the bacteria colorless and significantly more vulnerable to clearance by the host innate immune system. The drug has completed Phase I clinical trials in healthy volunteers, demonstrating safety and favorable pharmacokinetics, and is being advanced for the treatment of acute bacterial skin and skin structure infections (ABSSSI).
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