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- DZD8586 demonstrated significant anti-tumor efficacy in heavily pretreated chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) patients with ORR of 84.2%
- DZD6008, a BBB-penetrant 4th generation EGFR TKI, showed encouraging and durable anti-tumor activity with favorable safety and tolerability as a monotherapy in heavily pre-treated non-small cell lung cancer (NSCLC) patients with EGFR-mutations
SHANGHAI, May 26, 2025 /PRNewswire/ — Dizal (SSE:688192), a biopharmaceutical company committed to developing novel medicines for the treatment of cancer and immunological diseases, announced today that it will present latest clinical study results of its investigational drugs DZD8586 and DZD6008 at the 2025 American Society of Clinical Oncology (ASCO) Annual Meeting. The studies focus on B-cell non-Hodgkin lymphomas (B-NHLs) and non-small cell lung cancer (NSCLC) two disease areas Dizal has approved drugs and strong clinical pipeline.
DZD8586: A Potential Novel Therapeutic Option for Patients with B-NHL
A pooled analysis of two phase I/II studies of DZD8586 in CLL/SLL patients after treatment with covalent or non-covalent BTK inhibitors and BTK degraders (Abstract #7010) was selected for an oral presentation:
- An objective response rate (ORR) of 84.2% was achieved. Tumor response was observed in patients previously treated with BTK inhibitors and BCL-2 inhibitors, with response rates of 82.4% and 83.3%, respectively.
- Tumor response was observed irrespective of prior covalent/non-covalent BTK inhibitor, BTK degrader, or BCL-2 inhibitor treatment, and in patients with classic BTK resistance mutations (C481X) as well as other BTK mutations, including kinase-dead mutations.
- Response was durable, with an estimated 9-month duration of response (DOR) rate of 83.3%.
Prof. Jianyong Li, MD, PhD at Jiangsu Province Hospital, and the leading principal investigator of the study, said, “DZD8586 has shown promising antitumor activity in patients with relapsed/refractory CLL/SLL. By targeting both BTK-dependent and -independent signaling pathways, it could overcome resistance driven by target depletion or bypass activation, addressing significant limitations of current BTK inhibitors. We look forward to continued data readout from ongoing clinical studies.”
In addition, a Phase II study of DZD8586 as monotherapy in relapsed or refractory diffuse large B-cell lymphoma (r/r DLBCL) (Abstract # e19050) will also be presented at the conference. Patients recruited in the trial had received 1-4 prior lines of therapy, and all were treated with anthracycline-and CD20-antibody based chemoimmunotherapy. At the doses of 50 mg and 75 mg QD, DZD8586 demonstrated promising antitumor activity and a manageable safety profile. Tumor responses were observed in both germinal center B-cell-like (GCB) and non-GCB subtypes. Updated results from this study will be disclosed at the 2025 European Hematology Association (EHA) Annual Congress.
Prof. Lugui Qiu, MD, PhD at Institute of Hematology & Blood Diseases Hospital, Chinese Academy of Medical Sciences, the leading principal investigator of this study, said, “Treatment resistance in relapsed/refractory DLBCL remains a major clinical challenge. DZD8586, a non-covalent dual LYN/BTK inhibitor, has shown activity in both GCB and non-GCG subtypes, an important feature. With full BBB penetration and a favorable safety profile, it also shows promise in patients with CNS involvement, who typically confront a poor prognosis.”
DZD6008: A 4th generation EGFR TKI Poised to Address Unmet Needs in NSCLC
The presentation at ASCO 2025 will feature promising pre-clinical and early clinical data from an ongoing Phase I/II TIAN-SHAN2 study of DZD6008 in patients with EGFRm NSCLC (Abstract #8616). Preclinical studies showed that DZD6008 was potent against EGFR mutations, including single (L858R/19del), double (T790M and L858R/19del), and triple mutations (C797X, T790M and 19del), with good selectivity (> 50-fold) over wild-type EGFR.
As of March 31, 2025, a total of 12 EGFRm NSCLC patients were enrolled in the study during the dose escalation phase. The median number of prior lines of therapy was 4.5 (range 2-8). DZD6008 monotherapy demonstrated encouraging and durable antitumor activity with good tolerability in this heavily pre-treated population. Ten patients (83.3%) showed target lesion shrinkage with DZD6008 treatment. Partial response (PR) was observed at ≥20 mg. In line with preclinical findings, DZD6008 exhibited excellent BBB penetration, as well as sustained efficacy in patients with brain metastases. The ratio of measured free drug concentrations in CSF over plasma is over 1.0.
Prof. Mengzhao Wang, MD, PhD at Peking Union Medical College Hospital, the leading principal investigator of the study said, “DZD6008 is a novel, highly selective, full-BBB penetrant EGFR TKI with broad-spectrum of activity against different EGFR mutations. The clinical data revealed at ASCO 2025 suggested that DZD6008 has good antitumor activity and tolerability in EGFRm NSCLC patients who were resistant to EGFR TKIs, especially their durable remission effect on metastatic brain lesions. The ongoing TIAN-SHAN2 study aims to further validate these findings in a broader patient population.”
“The clinical data on DZD8586 and DZD6008 presented at this year’s ASCO further highlight our strong R&D capabilities and competitive edge in tackling difficult-to-treat hematologic malignancies and lung cancer. The significant efficacy data and encouraging safety profile give us confidence to push forward to accelerate its clinical development programs,” said Xiaolin Zhang, PhD, CEO of Dizal.
About DZD8586
DZD8586 is a first-in-class, non-covalent, LYN/BTK dual inhibitor with full blood-brain barrier (BBB) penetration, designed as a potential treatment option for B-cell non-Hodgkin lymphoma (B-NHL).
While Bruton’s Tyrosine Kinase (BTK) inhibitors have been approved for the treatment of B-NHL, resistance can arise through two major mechanisms: the BTK C481X mutation and BTK-independent BCR signaling pathway activation. Currently, there is no targeted therapy available to address both resistance mechanisms, posing an urgent clinical challenge. Although BTK degraders have shown encouraging efficacy in early clinical studies, mutation-related resistance has been reported, and degrader-related toxicities may affect long-term clinical application.
DZD8586 has high selectivity against other TEC family kinases (TEC, ITK, TXK and BMX). By targeting BTK and LYN, it blocks both BTK-dependent and -independent BCR-signaling pathways, effectively inhibiting tumor growth of B-NHLs in cell lines and in animal models. Phase I clinical trial suggests that DZD8586 exhibits favorable PK properties, good central nervous system (CNS) permeability, complete blockade of BCR signaling, and encouraging anti-tumor efficacy with good safety and tolerability in patients with B-NHL.
About DZD6008
DZD6008 is a novel, highly selective, full-BBB penetrant EGFR TKI, designed as a potential treatment option for advanced EGFR mutation positive (EGFRm) NSCLC.
Non-small cell lung cancer is the leading cause of cancer death in the world. Epidermal growth factor receptor (EGFR) gene is one of the most common driver genes for NSCLC. Multiple agents can be used to treat patients with EGFR mutated NSCLC who develop resistance to EGFR tyrosine kinase inhibitors (TKIs), but the clinical outcome was not satisfactory. Brain metastases (BM) are a leading cause of death and disease progression for NSCLC. Approximately 23%-30% of NSCLC patients are synchronous BM at their initial diagnosis. Previous studies reported that the 3-year cumulative rate of BMs ranges from 29.4% to 60.3% in patients with mutated EGFR.
Currently, the clinical benefits of existing treatments for third-generation EGFR TKI-resistant NSCLC are limited and DZD6008 is expected to fill the unmet medical needs. DZD6008 effectively inhibits EGFR-mutated tumor growth in cell lines and in animal models. Previous clinical studies have validated the design concept of the molecule and suggest that DZD6008 demonstrates good safety and efficacy in NSCLC patients with brain metastases who had failed third-generation EGFR TKI therapy or multiple lines of pre-treatments.
About Dizal
Dizal is a biopharmaceutical company, dedicated to the discovery, development and commercialization of differentiated therapeutics for the treatment of cancer and immunological diseases. The company aims to develop first-in-class and groundbreaking new medicines, and further address unmet medical needs worldwide. Deeply rooted in translational science and molecular design, it has established an internationally competitive portfolio with two leading assets in global pivotal studies, both of which have already been launched in China.
To learn more about Dizal, please visit www.dizalpharma.com, or follow us on Linkedin or X.
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