• ATG-018, a global rights asset developed by Antengene's internal R&D team, is an orally-bioavailable, small molecule ataxia telangiectasia and Rad3-associated (ATR) kinase inhibitor that targets the DNA damage response (DDR) pathways.
• The Phase I study will evaluate the safety, pharmacology and preliminary efficacy of ATG-018 monotherapy in patients with advanced tumors and hematologic malignancies.

SHANGHAI and HONG KONG, Aug. 16, 2022 /PRNewswire/ -- Antengene Corporation Limited ("Antengene" SEHK: 6996.HK), a leading innovative, commercial-stage global biopharmaceutical company dedicated to discovering, developing and commercializing first-in-class and/or best-in-class therapeutics in hematology and oncology, today announced that the first patient has been dosed in the Phase I ATRIUM trial to evaluate ATG-018 as a monotherapy in patients with advanced solid tumors and hematologic malignancies in Australia.

The ATRIUM trial is a Phase I multi-center, open-label, dose finding study of ATG-018 monotherapy in patients with advanced solid tumors or hematologic malignancies. The primary objective of the study is to evaluate the safety and tolerability of ATG-018 and to determine the maximum tolerated dose (MTD) and/or recommended Phase II dose (RP2D) and/or biologically effective dose of ATG-018 monotherapy and preliminary efficacy, if available. The secondary objective is to characterize the pharmacology of ATG-018.

ATG-018 is an orally-available, potent, selective small molecule ATR inhibitor. ATG-018 inhibits the ATR kinase, which limits cancer cells' ability to repair damaged DNA, in a mechanism also known as synthetic lethality or the DDR.

"In human cells, a variety of repair mechanisms exist to maintain genomic integrity, and defects in these pathways cause genome instability and promote tumorigenesis. Many cancer cells have high level replication stress and rely on their S/G2 checkpoints for survival following DNA damage. This renders tumor cells more susceptible to inhibition of ATR and targeting this may be a novel therapeutic strategy," said Dr Jim Coward, Chair of Icon's Medical Oncology Research Committee and Associate Professor at University of Queensland School of Medicine. "ATG-018, is an oral, potent, and selective inhibitor of ATR. Preclinical studies have demonstrated potent activity against ATR in enzyme inhibition assays and tumor cell lines including both solid tumors and hematological malignancies. We are encouraged by these findings, and eager to further evaluate the therapeutic potential of ATG-018 for patients."

Dr. Jay Mei, Antengene's Founder, Chairman and CEO said, "ATG-018 is a novel in-house discovered and developed drug candidate to enter the clinical stage. I am very proud of the joint efforts from the teams at Antengene and the clinical organizations to bring this compound to the clinical stage. Data on ATG-018 presented at 2022 American Association for Cancer Research (AACR 2022) Annual Meeting showed that ATG-018 has demonstrated promising single-agent activity in a robust preclinical program that includes a wide range of tumor types that rely on DDR and have a need for new treatments. In addition, early work to identify a set of predictive biomarkers could enable ATG-018 to be used as a precision-medicine. We will work closely with our investigators to advance this clinical program and strive to develop a new treatment option for patients around the world."

About ATG-018

Developed by the internal R&D Team at Antengene, ATG-018 is an oral, potent, selective small molecule inhibitor targeting ataxia telangiectasia and Rad3-associated (ATR) kinase. ATR kinase belongs to the phosphoinositide 3 kinase-related family. Inhibiting ATR kinase leads to increased accumulation of single-strand DNA breaks, particularly meaningful for tumor cells which rely on DNA damage repair (DDR). Preclinical studies have demonstrated that ATR inhibitor monotherapy or combination with other drugs (including DDR agents) could be promising therapeutic strategies for solid tumors (including gastric, esophageal, squamous cell carcinoma) and hematologic malignancies (chronic lymphocytic leukemia [CLL], diffuse large B-cell lymphoma [DLBCL] and multiple myeloma [MM]).

According to a preclinical poster presented at 2022 American Association for Cancer Research (AACR 2022) Annual Meeting, ATG-018 has demonstrated potent in vitro and in vivo monotherapy efficacy in solid tumor/hematologic cancer models with certain homologous recombination deficiencies. These data were supported by a series of genetic alterations that correlated with ATG-018 sensitivity and could be potential predictive biomarkers. Taken together, these data suggest that ATG-018 could be a promising therapeutic agent for patients with such homologous recombination deficiencies/genetic alterations.

About Antengene

Antengene Corporation Limited ("Antengene", SEHK: 6996.HK) is a leading commercial-stage R&D-driven global biopharmaceutical company focused on the discovery, development, manufacturing and commercialization of innovative first-in-class/best-in-class therapeutics for the treatment of hematologic malignancies and solid tumors, in realizing its vision of "Treating Patients Beyond Borders".

Since 2017, Antengene has a built broad and expanding pipeline of 15 clinical and preclinical assets, of which 10 are global rights assets, and 5 came with rights for Asia Pacific markets including the Greater China region. To date, Antengene has obtained 24 investigational new drug (IND) approvals in the U.S. and Asia, and submitted 6 new drug applications (NDAs) in multiple Asia Pacific markets, with the NDA for XPOVIO (selinexor) already approved in mainland China, South Korea, Singapore and Australia.

Forward-looking statements

The forward-looking statements made in this press release relate only to the events or information as of the date on which the statements are made in this press release. Except as required by law, we undertake no obligation to update or revise publicly any forward-looking statements, whether as a result of new information, future events or otherwise, after the date on which the statements are made or to reflect the occurrence of unanticipated events. You should read this press release completely and with the understanding that our actual future results or performance may be materially different from what we expect. In this press release, statements of, or references to, our intentions or those of any of our Directors or our Company are made as of the date of this press release. Any of these intentions may alter in light of future development. For a further discussion of these and other factors that could cause future results to differ materially from any forward-looking statement, see the section titled "Risk Factors" in our periodic reports filed with the Hong Kong Stock Exchange and the other risks and uncertainties described in the Company's Annual Report for year-end December 31, 2021, and subsequent filings with the Hong Kong Stock Exchange.

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SOURCE Antengene Corporation Limited