TEC

DZD8586 study results in B-cell non-Hodgkin lymphomas (B-NHLs) were selected for oral and poster presentations. The analysis in chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) after covalent or non-covalent BTK inhibitors and BTK degraders was selected for oral presentation Dizal will also present results from the ongoing Phase I/II study of DZD6008, a 4th generation EGFR TKI with full BBB penetration, in advanced EGFR mutation positive (EGFRm) non-small cell lung cancer (NSCLC) SHANGHAI, April 24, 2025 /PRNewswire/ -- Dizal (SSE:688192), a biopharmaceutical company committed to developing novel medicines for the treatment of cancer and immunological diseases, announced today that the 2025 American Society of Clinical Oncology (ASCO) Annual Meeting will feature the latest study results from the company's investigational drugs DZD8586 and DZD6008 in B-cell non-Hodgkin lymphomas (B-NHLs) and non-small cell lung cancer (NSCLC). The oral presentation includes results in B-NHLs from a pooled safety and efficacy analysis of two phase I/Ⅱ studies of DZD8586 in chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) patients with prior treatment of covalent and/or non-covalent BTK Inhibitors as well as BTK degraders. While early clinical data showed encouraging anti-tumor activities from BTK degraders in CLL/SLL patients, resistance mutations to both BTK inhibitors and degraders have already been reported, and degrader-related toxicities may affect long-term clinical application. Data from Phase I/II studies of DZD8586 in CLL/SLL, presented at the 66th American Society of Hematology (ASH) Annual Meeting, showed that 94.4% of patients achieved tumor shrinkage at ≥50 mg QD. Significant tumor responses were also observed in other B-NHLs, including diffuse large B-cell lymphoma (DLBCL). Preliminary results from the ongoing phase Ⅱ study of DZD8586 monotherapy in patients with relapsed/refractory DLBCL will be presented at this ASCO meeting. Dizal will also present Phase I/II data of DZD6008, a 4th generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with full blood–brain barrier (BBB) penetration, in advanced EGFR mutation positive (EGFRm) NSCLC patients who failed prior 3rd generation EGFR TKI treatment. Lung cancer is a leading cause of brain metastases (BMs), with 10-20% of patients with NSCLC presenting with BMs at diagnosis and 25-50% developing them over the course of their disease. NSCLC patients whose disease progressed after 3rd generation EGFR TKI treatment often develop CNS metastasis and exhibit acquired EGFR resistance mutations. Preclinical data shows that DZD6008 demonstrates good safety and efficacy in NSCLC patients with brain metastases who had failed 3rd generation EGFR TKI therapy or multiple lines of pre-treatments. "We are honored that our study results have been selected for oral presentations at ASCO for three consecutive years. Our presence at this congress highlights our commitment to addressing global unmet medical needs in hematological malignancies and lung cancer," said Xiaolin Zhang, PhD, CEO of Dizal. "We look forward to sharing positive clinical data of our novel medicines, which have the potential to bring clinical benefit to patients with limited treatment options." Dizal presentation details during ASCO 2025 ： 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 , or follow us on Linkedin or X. 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 turnout to be incorrect. Contacts Investor Relations: [email protected] Business Development: [email protected] Media Contact: [email protected] SOURCE Dizal Pharmaceutical WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

NANJING, China and GAITHERSBURG, Md., Dec. 10, 2024 /PRNewswire/ -- TransThera Sciences (Nanjing), Inc. (the " TransThera"), a clinical demand-oriented, registrational clinical stage biopharmaceutical company focusing on discovering and developing innovative small molecule therapies for oncology, inflammatory and cardiometabolic diseases, announced the poster presentation at the 2024 American Society of Hematology (ASH) Annual Meeting to discuss the phase I study results of TT-01488, a novel reversible BTK inhibitor for patients with relapsed or refractory B-cell malignancies. Bruton's tyrosine kinase (BTK) plays a critical role in the B-cell receptor signaling pathway, functioning as an important regulator of cell proliferation and cell survival in various B-cell malignancies. Currently there are 5 approved irreversible BTK inhibitors (BTKis) in the world. Due to the emergence of acquired mutation in the inhibitor's covalent binding site (C481S), there is a high unmet medical need to develop next-generation BTKi to overcome the resistance. TT-01488 is a next-generation, non-covalent, reversible BTKi which can overcome the acquired resistance to irreversible BTKis. In the preclinical study, TT-01488 potently Inhibits both wildtype and C481S-mutant BTK. The Phase I study of TT-01488 presented at ASH Annual Meeting was an open, multi-center, dose escalation study. As of the data cut-off date on October 2, 2024, 18 patients with pre-treated B-cell malignancies were enrolled, with the median 3 lines of prior therapies. TT-01488 was well-tolerated in all patients. Neither dose limiting toxicity (DLT) occurred nor any bleeding, atrial flutter or atrial fibrillation was reported. In pharmacokinetics and pharmacodynamics study, sustained pBTK C481S-mutant inhibition covering IC­90 was observed at steady state following multiple dosing at both 150 mg (QD) and 100 mg (BID) dose levels. Among 14 efficacy evaluable patients, objective response rate (ORR) was 57% (8/14)，including 3 complete remission (CR) and 5 partial remission (PR). 100% (7/7) of ORR was achieved in mantle cell lymphoma (MCL), Waldenström macroglobulinemia (WM) and marginal zone lymphoma (MZL). Overall, TT-01488 showed encouraging efficacy in B-cell non-Hodgkin lymphoma (B-NHL) patients, regardless of C481S status and with/without prior cBTKi therapy. About TT-01488 TT-01488 is an internally developed, non-covalent, reversible BTK inhibitor to overcome acquired resistance developed from marketed covalent BTK inhibitors in various types of relapsed or refractory hematological malignancies. TT-01488 is highly potent against BTK wild type and mutation with high selectivity over EGFR and Tec, indicating its potential for good efficacy and safety. About TransThera TransThera is a clinical demand-oriented, registrational clinical-stage biopharmaceutical company focusing on discovering and developing innovative small molecule therapies for oncology, inflammatory and cardiometabolic diseases. Further aided by in-depth study of translational medicine and drug design, TransThera aims to develop first-in-class or best-in-class drug candidates strategically positioned to meet urgent clinical needs on a global scale. For more information, please visit Forward-looking statements This news contains forward-looking statements that involve risks, uncertainties, and assumptions. If risks or uncertainties ever materialize or the assumptions prove incorrect, our actual results may differ from those expressed or implied by such forward-looking statements. All statements other than statements of historical facts could be deemed forward-looking, including, but not limited to, any statement of the plans, strategies, and objectives of management for future operations, including but not limited to our clinical development and commercialization plans; any projections of financial information; any statements about historical results that may suggest trends for our business; any statements of expectation or belief regarding future events, potential markets or market size, technology developments, our product pipeline, clinical data, results or practices or the implications thereof, enforceability of our intellectual property rights, competitive strengths or our position within the industry; and any statements of assumptions underlying any of the items mentioned. SOURCE TransThera Sciences (Nanjing) Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

DZD8586 demonstrated encouraging anti-tumor activity with manageable safety and favorable pharmacokinetic (PK) characteristics in patients with B-NHL SHANGHAI, Dec. 9, 2024 /PRNewswire/ -- Dizal (SSE:688192), a biopharmaceutical company committed to developing novel medicines for the treatment of cancer and immunological diseases, announced the latest data from a pooled safety and efficacy analysis of DZD8586, a non-covalent blood-brain barrier (BBB) penetrant LYN/BTK dual inhibitor, in B-cell non-Hodgkin lymphoma (B-NHL). The data were presented at the 66th American Society of Hematology (ASH) Annual Meeting. The analysis pooled data from ongoing phase 1/2 clinical studies evaluating DZD8586 in patients with B-NHL who had progressed following, or were intolerant to, prior systemic therapies. As of October 20, 2024, 61 patients were included in the efficacy analysis and 84 patients were included in the safety set. Anti-tumor efficacy: In chronic lymphocytic leukemia (CLL) / small lymphocytic lymphoma (SLL), the overall response rate (ORR) was 57.9% (≥ 50 mg) by data cutoff. Tumor response was observed in patients with prior treatment of covalent and non-covalent BTKi, and Bcl-2i. Tumor responses were observed in patients with classic BTK resistance mutations (C481X) as well as BTK "dead" mutations. Preliminary anti-tumor activity was observed in patients pre-treated by pirtobrutinib, with T474I mutation as well. Significant tumor response was also observed in other B-NHL, including diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), mantle cell lymphoma (MCL), marginal zone B-cell lymphoma (MZL), and central nervous system lymphoma (CNSL). Safety: Dose-dependent thrombocytopenia and neutropenia were the most common ≥grade 3 TEAEs, which could be well managed in the clinic. PK and pharmacodynamic biomarker Dose-proportional PK profile and dose-dependent modulation of pharmacodynamic biomarkers were observed. In patients with CNSL, the Kpuu,CSF at steady state were 1.21 and 0.98, suggesting high CNS penetration of DZD8586 in human. "A significant proportion of B-NHL patients treated with BTK inhibitors will eventually relapse and develop drug-resistant mutations. Two primary types of clinical resistance mutations have been identified: C481X mutation and BTK loss-of-activity mutations," said Xiaolin Zhang, PhD, CEO of Dizal. "DZD8586, as a non-covalent dual inhibitor targeting both BTK-dependent and -independent pathways, has demonstrated promising antitumor activity and safety profile in patients who did not respond to or develop resistance to both covalent and non-covalent BTK inhibitors, including those with CLL/SLL and other B-NHL. With multiple clinical development programs ongoing or under planning, DZD8586 is expected to bring significant clinical benefit to patients with relapsed or refractory B-NHL." Bruton's Tyrosine Kinase (BTK) inhibitors have revolutionized the treatment of B-cell lymphomas. However, resistance can arise through multiple mechanisms, compromising the treatment outcome and posing an urgent clinical challenge. The C481X mutation disrupts covalent BTK inhibitors binding to BTK enzyme and leads to treatment failure. Additionally, BTK-independent resistance mechanism due to loss of or much diminished BTK enzyme activity was also identified in the clinic. Currently, there is no targeted therapy available to address both resistance mechanisms. DZD8586 was designed as a LYN/BTK dual inhibitor with high selectivity against other TEC family kinases (TEC, ITK, TXK and BMX), as well as full BBB penetration. By targeting BTK and LYN, it blocks both BTK-dependent and -independent BCR-signaling pathways, which may potentially overcome resistance to approved covalent and non-covalent BTK inhibitors. About DZD8586 DZD8586 is an oral, highly selective, non-covalent LYN/BTK dual inhibitor to target both BTK-dependent and BTK-independent B-cell receptor (BCR) signaling pathways, with full blood-brain barrier penetration. Pre-clinical research revealed that DZD8586 demonstrated good safety profile and could effectively inhibit the growth of B-NHL cells. A healthy volunteer study of DZD8586 has been completed to investigate the clinical safety and PK/PD correlation. Global phase I/II studies are ongoing to evaluate the safety, tolerability, pharmacokinetics, and anti-tumor efficacy of DZD8586 in patients with r/r B-NHL. Preliminary results from the clinical trials suggest that DZD8586 exhibits favorable PK properties, good safety profile, and preliminary anti-tumor efficacy in patients with B-NHL. 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. Deep-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 , or follow us on 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 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 turnout to be incorrect. Contacts Investor Relations: [email protected] Business Development: [email protected] Media Contact: [email protected] SOURCE Dizal Pharmaceutical WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED