Macc1-inhibitor for Targeted Therapy of Macc1-Induced Metastasis

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This patent describes novel small molecule inhibitors of MACC1 (Metastasis-Associated in Colon Cancer 1), a gene shown to promote cancer cell proliferation, migration, and especially metastasis in numerous solid tumors. The inhibitors, including a lead compound and several analogues, were discovered through high-throughput screening and are shown to reduce MACC1 expression at the transcriptional level, thus preventing or reducing tumor growth and spread in vitro and in animal models. These molecules are intended for use as targeted medications to treat patients with cancers exhibiting elevated MACC1 levels, particularly those at risk of metastasis or at early disease stages (such as stage I/II colorectal or pancreatic cancer).

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• Targeted therapy for early-stage colorectal, pancreatic, breast, gastric, lung, and other solid cancers with high MACC1 expression to prevent metastasis.
• Treatment of patients with already metastasized tumors driven by MACC1 overexpression to reduce further disease spread.
• Prophylactic therapy (prevention) for cancer patients identified as high-risk for metastasis due to elevated MACC1, especially after initial tumor removal.
• Adjunct treatment in combination with conventional chemotherapeutics or anti-angiogenic drugs to improve outcomes.
• Personalized medicine: patient stratification and monitoring based on MACC1 levels to select those most likely to benefit from therapy.
• Reduction of tumor angiogenesis (formation of new blood vessels) that supports tumor growth and metastasis.

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• First targeted approach to treat and prevent metastasis in cancers with elevated MACC1, filling an unmet medical need.
• Reduces cancer cell migration, invasion, and proliferation, directly targeting the underlying cause of metastasis.
• Enables earlier intervention in high-risk patients, potentially preventing lethal metastatic disease and improving survival rates.
• Improves patient selection for treatment by focusing on those with high MACC1, increasing therapy effectiveness and cost-efficiency.
• Shown to be effective in both laboratory cell models and animal models, indicating strong translational potential.
• Favorable safety and toxicity profile in animal studies, supporting further clinical development.
• Versatility for use as monotherapy or in combination with other anti-cancer drugs.
• Potential application across a wide range of solid tumor types due to MACC1's role in multiple cancers.
• Novel mechanism of action (transcriptional inhibition of MACC1), offering a new tool in cancer therapy.

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Patent Abstract

The invention relates to MACC1 inhibitors for use as a medicament in the treatment of cancer. The general formula 1 provided by the invention shows beneficial effects in inhibiting the formation of metastasis, cell proliferation and cancer progression. The invention further relates to the MACC1 inhibitors of the invention for the treatment of a subject with elevated MACC1 levels and wherein said treatment inhibits MACC1 expression in said subject. The invention further relates to the MACC1 inhibitors of the invention in the treatment of subjects with a solid cancer at early stages of cancer progression such as stage I or II for colorectal or pancreatic cancer or metastatic cancer, and/or for the prevention of developing metastases.