March 23rd, 2015

(The news has been released on bioon.com/ ebiotrade.com)

“Icaritin suppresses multiple myeloma, by inhibiting IL-6/JAK2/STAT3” is published online on Oncotarget ( Link: http://www.impactjournals.com/oncotarget/index.php?journal=oncotarget&page=article&op=view&path%5B%5D=3399&path%5B%5D=7430). The study is completed by Prof. Guangsen Zhang’s lab in the Second Xiangya Hospital, Central South University.

Multiple myeloma (MM) is an incurable B-cell malignancy and the second most frequent hematological tumor. MM treatment is developing rapidly in the last decades but there still remain highly unmet medical needs in refractory or relapsed MM patients. Icaritin is a prenylflavonoid derived from a traditional Chinese medicine Epimedium Genus. It has a wide range of pharmacological and biological activities including cardiovascular function improvement, hormone regulation and antitumor activity.

In this study, Prof. Zhang’s lab found for the first time that, icaritin showed anti-multiple myeloma activities towards MM cell line U266 and primary bone marrow cells (CD 138+ cells). Icaritin induces cell apoptosis without causing general cytotoxic effect. Consistent with in vitro studies, in MM xenograft mouse models, icaritin suppresses tumor growth and decreased serum IL-6 and IgE levels. The underlying mechanisms of icaritin anti-MM activity are mainly involved in the inhibition of IL-6 driven JAK2/STAT3 signaling pathway. The cytokine IL-6 plays a crucial role in immunology, inflammation and carcinogenesis. Effectors in IL-6 mediated pathway become hot targets for anti-tumor drug development not only in MM, but also in various cancers including liver cancer. Prof. Zhang’s study indicates icaritin may provide a novel therapeutic strategy for treatment of refractory MM.

Icaritin is being investigated as a Class 1 TCM/Natural Medicine sponsored by Shenogen Pharma Group. Shenogen possesses robust intellectual property rights around icaritin and got supported from National “Twelfth Five-year Plan” Special Project for “Significant New Drug Development”. Shenogen is funded by top class VCs including IDG, Qiming and Legend Capital. Icaritin treatment in advanced HCC Ph II clinical trial is completing. There’re some positive signals in MOA and biomarker exploratory studies. Shenogen plans to file icaritin as a breakthrough therapy for NDA in June 2015.

Abstract:

Icaritin is an active prenylflavonoid derived from Epimedium genus, a traditionalChinese medicine. Icaritin has a wide range of pharmacological and biologicalactivities, including cardiovascular function improvement, hormone regulationand antitumor activity. Here, we investigated the effect of icaritin on multiplemyeloma (MM) in vitro and in vivo. Icaritin inhibited cell growth of MM cell lineand primary MM cells. In contrast, icaritin had low or no cytotoxic effect on normalhematopoiesis. We also demonstrated that in MM xenograft mouse models, icaritinsuppressed tumor growth and decreased serum IL-6 and IgE levels, but did not showadverse reactions such as body weight loss. The anti-MM activity of icaritin was mainlymediated by inhibiting IL-6/JAK2/STAT3 signaling. We suggest that icaritin can befurther tested in clinical trials in MM.

About Shenogen

ShenogenPharma Group is a drug discovery and development company based in Beijing, China, that dedicated the development of first-in-class therapeutics for cancer treatment. We possess robust intellectual property rights around a novel membrane-bound estrogen receptor, ER-alpha 36, which is related to tumor metastasis. Under the motto of “Better Medicine, Better Life” and a seasoned management team, together with our partners, Shenogen has developed an impressive product pipeline. Our pipeline consists of novel small molecule and antibody therapeutics for cancer treatment which includes liver cancer, breast cancer, other solid tumors and leukemia. Our lead molecule, icaritin, is currently in Ph II clinical trial for treatment of advanced hepatocellular carcinoma.