2022 SABCS| Dizal Announces Updated Results from Phase I Trial Evaluating DZD1516 in Heavily Pretreated Metastatic HER2 Positive Metastatic Breast Cancer

San Antonio-December 9, 2022 – Dizal today announces the presentation of updated results of the first-in-human Phase I WEN-JI1 trial of DZD1516 in treating patients with HER2 positive metastatic breast cancer (HER2+ MBC) who relapsed from the standard of care at the 2022 San Antonio Breast Cancer Symposium.   As of August 29, 2022, 23 patients with HER2+ MBC from the USA and China were enrolled in the Phase I trial for the monotherapy of DZD1516. Key findings are as follows: The mean Kpuu,CSF in patients was 2.1 for DZD1516 across the dose range, indicating full penetration through human BBB. DZD1516 was well tolerated at dose levels from 25 mg to 250 mg, twice daily with oral administration. Consistent with its high selectivity, no wild-type EGFR-related AEs have been reported. Among 21 evaluable patients who completed at least one post-treatment assessment per modified RECIST v1.1 criteria, the best anti-tumor response achieved with the oral HER2-targeted TKI was stable disease in intracranial, extracranial, and overall lesions. Notably, these patients had received a median of 7 prior lines of treatment. Besides, preclinical research showed synergistic anti-tumor activity of DZD1516 in combination with DS-8201a in HER2+ brain metastasis xenograft models.   “Patients with HER2+ breast cancer and CNS metastases have poor prognoses,” said Dr. Xiaolin Zhang, CEO of Dizal, “Based on these promising findings, we will further explore the combination therapy potential of DZD1516 as a new treatment option for this underserved population.”   Nearly 60% of patients with advanced HER2 positive breast cancer develop central nervous system (CNS) metastasis, which is associated with poor prognosis. Recently emerging agents including antibodies, tyrosine kinase inhibitors (TKIs) and antibody–drug conjugates (ADCs) greatly improved the outcomes of HER2+ MBC patients, however, demonstrated poor penetrability through the blood-brain barrier (BBB). To address this unmet clinical need, Dizal designed and developed DZD1516, an oral, potent, reversible, selective, and full blood-brain barrier penetrable HER2 TKI with over 300-fold selectivity over wild-type EGFR.   About 1516 DZD1516 is designed as an oral, potent, reversible, highly selective, and full blood-brain barrier (BBB) penetrant HER2 tyrosine kinase inhibitor (TKI), with more than 300-fold selectivity for HER2 compared to wild-type EGFR. It is well tolerated at doses ≤ 250 mg, twice daily. And in consistent with its high selectivity, no wild-type EGFR-related AEs have been reported. In patients, mean Kpuu,CSF is 2.1 for DZD1516 across the dose range, indicating full penetration of DZD1516 through human BBB.   About Dizal Dizal is a clinical-stage, biopharmaceutical company, dedicated to the discovery and development of differentiated therapeutics for the treatment of cancer and immunological diseases. Deep-rooted in translational science and molecular design, it has established an internationally competitive portfolio of five clinical-stage assets with two leading assets in global pivotal studies.   Forward-Looking Statements This news release may contain certain forward-looking statements that are, by their nature, subject to significant risks and uncertainties. The words "anticipate", "believe", "estimate", "expect", and "intend" and similar expressions, as they relate to Dizal, are intended to identify certain forward-looking statements. Dizal does not intend to update these forward-looking statements regularly. These forward-looking statements are based on the existing beliefs, assumptions, expectations, estimates, projections, and understandings of the management of Dizal with respect to future events at the time these statements are made. These statements are not a guarantee of future developments and are subject to risks, uncertainties, and other factors, some of which are beyond Dizal's control and are difficult to predict. Consequently, actual results may differ materially from information contained in the forward-looking statements as a result of future changes or developments in our business, Dizal's competitive environment, and political, economic, legal, and social conditions. Dizal, the Directors, and the employees of Dizal assume (a) no obligation to correct or update the forward-looking statements contained on this site; and (b) no liability in the event that any of the forward-looking statements does not materialize or turn out to be incorrect.   Contacts Investor Relations: [email protected] Business Development: [email protected]

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