New mitochondria-targeted therapeutics will help lung, other cancers

Medical College of Wisconsin inventors have developed novel small molecule therapeutics that will help treat small cell lung cancer, among other cancers. These new compounds, named “mito-honokiols” are selectively designed to accumulate in tumor mitochondria and inhibit OXPHOS via mitochondrial complex 1, which affords cytostatic properties against tumor cells, thereby inhibiting tumor growth and significantly reducing brain metastases.

Historically, mitochondria were thought to be dispensable in tumor cells. However, certain cancers are now known to be highly dependent on mitochondrial metabolism, making OXPHOS an emerging druggable target for cancer therapy. These new “mito-honokiol” compounds were designed with tumor-specific OXPHOS inhibition in mind, and have shown efficacy towards both in vitro cell line and in vivo mouse lung cancer models.

Key Advantages:

• Selective to tumor cells with no toxicity to normal cells—even up to 20x effective dose
• Nanomolar potency
• Significantly reduces brain metastases in addition to inhibiting primary tumor growth

Applications: The “mito-honokiol” cytostatic compounds have significant potential as therapies alone or in combination with cytotoxic agents and/or immunotherapies.