Antengene Corporation Limited ("Antengene", SEHK: 6996.HK), a leading innovative biopharmaceutical company dedicated to discovering, developing and commercializing global first-in-class and/or best-in-class therapeutics in hematology and oncology, announced that China's National Medical Products Administration (NMPA) has approved the initiation of a Phase Ib/II open-label, multicenter, dose-escalation study of eltanexor (ATG-016) in patients with advanced solid tumors (the REACH study).

This study aims to assess the safety and efficacy of eltanexor monotherapy in patients with advanced solid tumors. The Phase Ib part of the study will be carried out in patients with advanced solid tumors, including those with KRAS-mutant, p53 wild-type, human papillomavirus (HPV)-associated, Epstein–Barr virus (EBV)-positive and other solid tumors; and the Phase II part of the study will enroll patients with recurrent or metastatic penile squamous cell carcinoma, and patients with recurrent or metastatic nasopharyngeal carcinoma.

Eltanexor is a next-generation selective inhibitor of nuclear export (SINE) compound which exerts antitumor effects by inhibiting the nuclear export protein XPO1 leading to the accumulation and activation of tumor suppressor proteins in the nucleus, while simultaneously blocking the expression and translation of oncogenic proteins. For cancer patients, high XPO1 expression is commonly associated with a poor prognosis and resistance to chemotherapies. Pre-clinical data showed that eltanexor has potent pro-apoptotic activity in a broad spectrum of tumor cells without affecting normal cells. Moreover, eltanexor has also showed potent antitumor activity in animal models with multiple solid tumors including hepatocellular carcinoma, prostate cancer, pancreatic cancer, colon cancer and breast cancer.

"This IND approval marks an important step for Antengene's clinical development of eltanexor, one that we hope will ultimately allow patients with solid tumors to benefit from eltanexor's novel mechanism of action," said Dr. Jay Mei, founder, chairman and CEO of Antengene. "Based on the compelling pre-clinical and clinical data, eltanexor monotherapy has the potential of bringing renewed hope and higher quality of life to patients with advanced solid tumors in China."