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AssigneeQuadriga Biosciences, Inc.
InventorsBernd Jandeleit, Wolf-Nicolas Fischer, Kerry J. Koller
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β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
A method of treating cancer in a patient comprising administering to a patient in need of such treatment a therapeutically effective amount of (3S)-3-amino-4-[5-[bis(2-chloroethyl)amino]-2-methyl-phenyl]butanoic acid (5), or a pharmaceutically acceptable salt thereof, wherein the cancer comprises glioblastoma, triple negative breast cancer, melanoma, prostate cancer, or multiple myeloma.
Dependencies are inferred from the claim text.