Pegylated lapatinib, injection and preparation method thereof

2015 
The present invention provides a pegylated lapatinib, an injection and a preparation method thereof, wherein the general formula of the pegylated lapatinib is defined in the specification, A is selected from a single-arm or multi-arm polyethylene glycol or poly ethylene glycol derivative, X is selected from the formula defined in the specification, Y and M are independently and respectively selected from double carboxylic acids having amino or corresponding acyl substituents, N is selected from an amino acid or peptide, LPT is lapatinib, a is 0 or 1, b is 0 or 1, c is 1 or 2, d is 1 or 2, and e is equal to the arm number of X. According to the present invention, the pegylated drug of lapatinib is synthesized, such that the lapatinib toxicity is reduced, the water solubility and the biological stability are improved, the drug resistance of cancer cells and cancer stem cells are avoided, the targeting property is enhanced, and the anticancer treatment effect is significantly improved.
    • Correction
    • Source
    • Cite
    • Save
    • Machine Reading By IdeaReader
    0
    References
    0
    Citations
    NaN
    KQI
    []