- DZD6008 demonstrates significant and durable antitumor activity, excellent blood-brain barrier penetration, and a favorable safety profile in patients with NSCLC resistant to third-generation EGFR TKIs
- In treatment-naïve advanced NSCLC patients following chemoimmunotherapy, Gao Ruizhe® combined with an anti-PD-1 antibody shows encouraging and durable antitumor efficacy with good tolerability, with more pronounced benefits observed in patients with high PD-L1 expression
DZD6008: Fourth-Generation EGFR TKI Poised to Overcome Resistance Challenges
Latest data show that DZD6008 demonstrates encouraging and durable antitumor activity with a favorable safety profile in patients with NSCLC resistant to third-generation EGFR TKIs:
- 82.1% of patients experienced tumor shrinkage, with higher response rates expected as treatment duration extends;
- At doses of 40mg and 60mg, the 6-month progression-free survival (PFS) rates were 70.6% and 61.8%, respectively, with median duration of response (mDoR) not yet reached;
- Excellent blood-brain barrier penetration, with intracranial tumor responses observed in patients with baseline brain metastases;
- Favorable safety profile, with high selectivity for wild-type EGFR and low incidence of adverse events.
In the field of EGFR-sensitive mutation NSCLC resistance, the EGFR C797X mutation is one of the most common EGFR pathway-dependent resistance mutations in patients with NSCLC resistant to third-generation EGFR TKIs. DZD6008 is a novel, fully brain-penetrant fourth-generation EGFR TKI with high selectivity for wild-type EGFR. It demonstrates significant antitumor activity and a favorable safety profile across various EGFR mutations, including sensitive mutations (L858R/19del), resistant double mutations (L858R/19del and T790M/C797X), or triple mutations (L858R/19del, T790M, and C797X).
Gao Ruizhe®: JAK1 Combined with Anti-PD-1 Shows Sustained Benefits
The study of Gao Ruizhe® combined with an anti-PD-1 antibody as first-line treatment for NSCLC without driver gene mutations enrolled a total of 47 treatment-naïve advanced NSCLC patients. Following chemoimmunotherapy, Gao Ruizhe® combined with sintilimab demonstrated encouraging and durable antitumor efficacy, with more pronounced benefits in patients with high PD-L1 expression. The combination regimen was well tolerated, with a significant reduction in observed immune-related adverse events (irAEs).
Dr.张小林, Founder, Chairman, and CEO of Dizal Pharmaceutical, stated: “The multiple research results Dizal presented at this year’s ASCO conference demonstrate the company’s ongoing innovative exploration in addressing unmet clinical needs in non-small cell lung cancer (NSCLC). Among these, acquired resistance following third-generation EGFR TKI therapy and central nervous system metastases remain critical recurrence challenges in NSCLC treatment that urgently need to be overcome. DZD6008 was designed precisely based on these key clinical needs. The latest data further validate its molecular design concept, potentially offering patients a safe new oral treatment option. We are extremely encouraged by this clinical progress and look forward to collaborating with global researchers to accelerate the global clinical development of DZD6008.”
Note: References to market position and terms such as “first” or “only” in this article are based on publicly available information as of the publication date of this article.
About Gao Ruizhe® (Golidocitinib)
Gao Ruizhe® is a highly selective Janus kinase 1 (JAK1) inhibitor independently developed by Dizal. It is the world’s first and only approved treatment targeting the JAK/STAT pathway for PTCL with a novel mechanism of action. It received marketing approval from the China National Medical Products Administration (NMPA) in June 2024 for the treatment of adult patients with relapsed or refractory peripheral T-cell lymphoma (r/r PTCL) who have received at least one prior systemic therapy. The approved indication for Gao Ruizhe® has been included in the National Reimbursement Drug List (2024 Edition). In April 2025, Gao Ruizhe® for the treatment of r/r PTCL was included as a Category I recommended regimen in the Chinese Society of Clinical Oncology (CSCO) Guidelines for the Diagnosis and Treatment of Lymphoma (2025 Edition).
AboutDZD6008
DZD6008 is a novel, fully brain-penetrant fourth-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) independently developed by the company. It effectively inhibits the growth of various EGFR mutant cells and tumor animal models. Currently, the mechanisms of resistance to EGFR TKIs in NSCLC are not fully understood, and existing treatments offer limited clinical benefit. Furthermore, brain metastases are a major cause of disease progression and patient mortality, with 23%-30% of EGFR-mutant NSCLC patients having brain metastases at initial diagnosis, and the risk of developing brain metastases within three years of diagnosis potentially increasing to 29.4%-60.3%.
Currently, existing treatments for NSCLC resistant to third-generation EGFR TKIs offer limited clinical benefit. DZD6008 has the potential to fill this unmet clinical need. In completed clinical trials, DZD6008 has fully validated its molecular design concept, demonstrating excellent safety and efficacy in patients resistant to third-generation EGFR TKIs and multiple prior therapies, including those with brain metastases.
About Dizal Pharmaceutical
Dizal Pharmaceutical (Stock Code: 688192.SH) is a global innovative biopharmaceutical company focused on the research, development, and commercialization of novel therapies in oncology and hematological diseases. The company adheres to a concept of source innovation, aiming to introduce first-in-class drugs and treatments with breakthrough potential to fill unmet global clinical needs. Based on its industry-leading translational science and novel drug molecular design and screening technology platforms, the company has established a pipeline of seven globally competitive product candidates. Among these, two leading products whose global pivotal clinical trials have met primary endpoints—舒沃哲® has been approved for marketing in both China and the United States, and Gao Ruizhe® has been approved for marketing in China. For more information, please follow the WeChat public account: 迪哲Dizal, or visit www.dizalpharma.com.
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