Country for PR: China
Contributor: PR Newswire Asia (China)
Thursday, November 26 2020 - 17:42
Approval of Phase I/II Clinical Trial of ATG-016 (Eltanexor), a Second Generation Selective Inhibitor of Nuclear Export (SINE), in Mainland China for the Treatment of Myelodysplastic Syndrome
SHANGHAI and HONG KONG, Nov. 26, 2020 /PRNewswire-AsiaNet/ --

Antengene Corporation Limited ("Antengene", HKSE stock code: 6996.HK), a 
leading innovative biopharmaceutical company dedicated to discovering, 
developing and commercializing global first-in-class and/or best-inclass 
therapeutics in hematology and oncology, announced that the National Medical 
Products Administration (NMPA) has approved the clinical trial of ATG-016 
(eltanexor) in patients with intermediate and higher risk myelodysplastic 
syndrome (MDS) according to the Revised International Prognostic Scoring System 
(IPSS-R) after the failure of hypomethylating agents (HMA) based therapy. The 
trial is a Phase I/II, single-arm, open-label clinical study, aiming to 
evaluate the pharmacokinetics, safety and efficacy of ATG-016 (eltanexor) 

MDS is a heterogeneous group of clonal disorders of the bone marrow 
hematopoietic stem cells (HPSCs), characterized by ineffective hematopoiesis 
with peripheral blood cytopenia and a higher risk for developing acute myeloid 
leukemia (AML). Patients with high-risk MDS refractory to hypomethylating 
agents have a median overall survival (OS) of only 4 to 6 months with limited 
options for follow-up treatment. Pre-clinical studies have demonstrated that 
selective inhibitor of nuclear export (SINE) compounds are able to block the 
nuclear export of many tumor suppressor proteins (e.g. p53, IkB, p21) leading 
to their accumulation and activation in the nucleus thereby exerting anti-tumor 
effects. In addition, SINE compounds can also reduce the nuclear export and 
translation of many oncogenic mRNA (c-Myc, Bcl-2, Bcl-6, cyclin D) which are 
bound to elF4E and result in selective apoptosis of tumor cells. ATG-016 is a 
member of the latest-generation of SINE compounds. Compared to the 
first-generation nuclear export inhibitor, ATG-016 demonstrates minimal 
blood-brain barrier permeability and a broader therapeutic window. It has shown 
preliminary anti-cancer activity in high-risk MDS patients.

Dr. Jay Mei, the Founder, Chairman and CEO of Antengene expressed, "The 
approval of the ATG-016 clinical trial demonstrates the efficient execution of 
the Antengene R&D team and is also the first clinical trial approval obtained 
by Antengene in mainland China after its listing." He also mentioned, 
"Selinexor, the first-generation selective inhibitor of nuclear export, has 
shown extensive activity against hematological malignancies and solid tumors, 
and has been approved by the FDA for relapsed/refractory multiple myeloma and 
diffuse large B-cell lymphoma. As a second-generation orally available SINE 
compound, ATG-016 can reduce the blood-brain barrier penetration, thereby 
representing a broader therapeutic window with potentially less adverse events 
and better drug tolerability."

About ATG-016

ATG-016 (eltanexor) is a second-generation selective inhibitor of nuclear 
export compound. Compared to the first-generation SINE compound, ATG-016 has 
lower blood-brain barrier penetration and broader therapeutic window which 
allows more frequent dosing and a longer period of exposure at higher levels 
with better tolerability. Therefore, ATG-016 may be used to target a wider 
range of indications. We plan to conduct phase I/II clinical studies for MDS in 
China, and plan to further develop ATG-016 for cancers with high prevalence in 
the Asia-Pacific region (such as KRAS-mutant solid tumors) and virus infection 
related malignancies (such as nasopharyngeal carcinoma).

About Antengene

Antengene Corporation Limited ("Antengene", SEHK: 6996.HK) is a leading 
clinical-stage Asia-Pacific biopharmaceutical company focused on innovative 
oncology medicines. Antengene aims to provide the most advanced anti-cancer 
drugs to patients in China, the Asia Pacific Region and around the world. Since 
its establishment, Antengene has built a pipeline of 12 clinical and 
pre-clinical stage assets, obtained 10 investigational new drug (IND) approvals 
and has 9 ongoing cross-regional clinical trials in Asia Pacific. At Antengene, 
we focus on developing drug candidates with novel mechanisms of action (MoAs) 
and first-in-class/best-in-class potential to address significant unmet medical 
needs. The vision of Antengene is to "Treat Patients Beyond Borders" through 
research, development and commercialization of first-in-class/best-in-class 

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SOURCE  Antengene Corporation Limited