Dizal Announces Positive Phase I Clinical Trial Results for DZD1516 in Treating HER2 Breast Cancer at 2022 ESMO

PARIS,Sept. 5,2022 -- Dizal reported the promising safety and pharmacokinetic data from the global Phase I study of DZD1516 in patients with HER2 positive metastatic breast cancer (HER2+ MBC) who relapsed from multiple prior treatments at the 2022 European Society for Medical Oncology Annual Meeting.

Nearly 60% of patients with advanced HER2-positive breast cancer develop brain metastasis and the prognosis is extremely poor. DZD1516 is an oral,full blood-brain barrier (BBB) penetrant selective HER2 inhibitor for the treatment of HER2-positive metastatic breast cancer.

The Phase I study is enrolling HER2+ MBC patients who relapsed from or were intolerant to the standard of care (SoC). The primary objective is to evaluate the safety of DZD1516 and to define maximum tolerated dose (MTD). As of February 20,2022,DZD1516 was explored in 22 HER2+ MBC patients from the USA and China,among whom nearly 70% had CNS metastases at baseline. Key findings are as follows:

DZD1516 was well tolerated at doses ≤ 250 mg,and in consistent with its high selectivity,no wild-type EGFR-related AEs have been reported. Thus,250 mg was defined as MTD.

In patients,mean Kpuu,CSF was 2.1 for DZD1516 across the dose range,indicating full penetration of DZD1516 through human BBB.

18 patients had completed ≥ 1 post treatment RECIST assessment. With a median of 7 lines of prior systemic treatment (86% treated with HER2 TKI),the best antitumor efficacy in intracranial,extracranial and overall lesions was stable disease.

"Patients with HER2 positive breast cancer and brain metastasis have poor outcomes due to the limited therapies," said Dr. Xiaolin Zhang,CEO of Dizal,"Based on these promising findings,we will further explore the potential of DZD1516 as a new treatment option forthis underserved patient population."

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,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.

About ESMO

The European Society for Medical Oncology (ESMO) is the leading professional organization for medical oncology. With more than 25,000 members representing oncology professionals from over 160 countries worldwide,ESMO is the society of reference for oncology education and information. Found in 1975,ESMO's core mission is to improve the quality of cancer care,from prevention and diagnosis all the way to palliative care and patient follow-up. And it is to promote equal access to optimal cancer care for all patients. The 2022 annual ESMO Congress will be held in Paris,France,online and offline from 9-13 September. The congress presents the latest scientific developments in basic,translational and clinical cancer research and contextualizes new findings for practical implementation in everyday patient care.

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