Methods and compositions for administration of 3-halopyruvate and related compounds for the treatment of cancer

摘要

The present disclosure relates to the discovery that compounds of the invention, particularly 3-bromopyruvate and related compounds, can be safely administered at concentrations effective for the treatment of cancer when formulated with an acidity of greater than or equal to pH of 2 and less than or equal to a pH of 6. Disclosed herein are novel and improved methods and compositions for the treatment of cancer using 3-halopyruvate and related compounds.

主权项

1. A method of treating cancer in a subject, wherein the cancer is selected from the group consisting of: liver cancer, pancreatic cancer, lung cancer and breast cancer, comprising orally administering to the subject an effective amount of a pharmaceutical composition comprising a pharmaceutical agent represented by the general formula:wherein, independently of each occurrence:
X represents a halide; R1 represents OR, H, N(R″)2, C1-C6 alkyl, C6-C12 aryl, C1-C6 heteroalkyl, or C6-C12 heteroaryl; R″ represents H, C1-C6 alkyl, or C6-C12 aryl; R represents H, alkali metal, C1-C6 alkyl, C6-C12 aryl or C(O)R′; and R′ represents H, C1-C20 alkyl or C6-C12 aryl;wherein the pharmaceutical composition has an acidity of greater than or equal to about pH 2 and less than pH 5; andwherein the pharmaceutical composition further comprises NaHCO3.