Background:

The (6-maleimidocaproyl) hydrazone derivative of doxorubicin (INNO-206), formerly known as DOXO-EMCH, is a prodrug of the anticancer agent doxorubicin which selectively binds to the cys34 of circulating albumin and accumulates in solid tumors due to passive targeting[1]. INNO-206 shows significantly superior antitumor efficacy over free doxorubicin in a spectrum of preclinical tumor models [2].

In vivo: In a murine renal cell carcinoma model and in breast carcinoma xenograft models, INNO-206 has shown superior activity over doxorubicin. INNO-206 has shown more potent antitumor efficacy than free doxorubicin in the tumor models and is thus a promising clinical candidate for treating a broad range of solid tumors [2].

Clinical trials: In a phase I study, INNO-206 showed a good safety profile at doses up to 260 mg/m2 doxorubicin equivalents. INNO-206 was able to induce tumor regressions in breast cancer, small cell lung cancer and sarcoma. [1].

参考文献:
[1]. Kratz F. DOXO-EMCH (INNO-206): the first albumin-binding prodrug of doxorubicin to enter clinical trials[J]. Expert opinion on investigational drugs, 2007, 16(6): 855-866.
[2]. Graeser R, Esser N, Unger H, et al. INNO-206, the (6-maleimidocaproyl hydrazone derivative of doxorubicin), shows superior antitumor efficacy compared to doxorubicin in different tumor xenograft models and in an orthotopic pancreas carcinoma model[J]. Investigational new drugs, 2010, 28(1): 14-19.
[3]. Graeser R, Esser N, Unger H, et al. INNO-206, the (6-maleimidocaproyl hydrazone derivative of doxorubicin), shows superior antitumor efficacy compared to doxorubicin in different tumor xenograft models and in an orthotopic pancreas carcinoma model[J]. Investigational new drugs, 2010, 28(1): 14-19.