Dizal Announces Pre-clinical and Early Clinical Results of DZD1516 in Breast Cancer Research

Dizal today announced the latest publication of translational science and early clinical results of DZD1516, a potent andselective HER2 tyrosine kinase inhibitor (TKI) with full brain blood barrier (BBB) penetration in Breast Cancer Research (IF: 8.4).   Breast cancer is one of the most common types of cancer worldwide, and around 15%-30% of cases are diagnosed as HER2 positive.Up to 50% of patients with HER2 positive (HER2+) metastatic breast cancer (MBC) develop central nervous system (CNS) metastasis and the prognosis is extremely poor. Currently approved drugs for HER2+ MBC such as antibodies, antibody-drug conjugates (ADCs), and TKIs have limited BBB-penetration ability.   With the goal to address the limitations of existing therapies, Dizal has developed a potent and highly selective HER2TKI, DZD1516. Notably, this TKI exhibits full penetration across the BBB, acrucial accomplishment enabled by Dizal’s unique CNS metastasis research platform. This was validated by a series of cellular and animal models published in the paper.   Key findings from preclinical research areas follows: DZD1516 showed over 300-foldselectivity for HER2 against wild-type EGFR. DZD1516 alone showed profound anti-tumoractivity in brain metastasis (BM) and subcutaneous (SC) models, and when incombination with a HER2 ADC, T-DM1 or T-DXd, its anti-tumor effect was significantly enhanced. DZD1516 demonstrated favorable pharmacokinetic properties, with a dose-dependent increase in plasma exposureand significant pHER2 activity inhibition.   Ina recent global multi-center Phase I study, 23 patients with HER2+ MBC from theUSA and China were treated with DZD1516 monotherapy. Of these patients, 65.2% had baseline brain metastasis. The study results showed:  DZD1516 was well tolerated from 25mg to 250 mg (BID), and in consistent with its high selectivity, no wild-type EGFR-related AEs have been reported up to 250 mg. In patients with CNS metastases, the mean Kpuu,CSF was 2.1 for DZD1516 across thedose range, indicating full penetration of DZD1516 through human BBB. Given these findings, DZD1516 holds significant promise as an improved treatment option for patients with HER2+ MBC.Further clinical studies are currently being planned to explore this potential.   With its promising safety profile,tolerability, and impressive BBB penetration ability, DZD1516 has generated considerable interest in the field of breast cancer. The clinical study resultshave been presented at prestigious international academic conferences, including the 2021 San Antonio Breast Cancer Symposium (SABCS), 2022 AmericanSociety of Clinical Oncology (ASCO), 2022 European Society for Medical Oncology(ESMO), and 2022 SABCS.   About DZD1516 DZD1516 is designed as an oral, potent, reversible, highly selective, and full BBB penetrant HER2 TKI, with over300-fold selectivity for HER2 against wild-type EGFR. It is well tolerated atdoses ≤ 250 mg, twice daily. And in consistent with its high selectivity, nowild-type EGFR-related AEs have been reported up to 250 mg. In patients, the meanKpuu,CSF is 2.1 for DZD1516 across the dose range, indicating fullpenetration 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-rootedin 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. To learn more about Dizal, please visit www.dizalpharma.com, or follow us at Linkedin or Twitter.   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 intendto 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, someof 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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