SUZHOU, China, and ROCKVILLE, Md., June 1, 2024 /PRNewswire/ — Ascentage Pharma (6855.HK), a worldwide biopharmaceutical firm engaged in growing novel therapies for most cancers, continual hepatitis B (CHB), and age-related ailments, introduced at present that it has launched up to date information of its novel drug candidate AGP-2449, a FAK/ALK/ROS1 tyrosine kinase inhibitor (TKI), in sufferers with non-small-cell lung most cancers (NSCLC) in a poster presentation on the sixtieth American Society of Medical Oncology (ASCO) Annual Assembly going down in Chicago, IL. That is the third consecutive yr by which scientific information from this examine of APG-2449 have been chosen for shows on the ASCO Annual Assembly.

The ASCO Annual Assembly showcases essentially the most cutting-edge research in scientific oncology and state-of-the-art superior most cancers therapies and is the world’s most influential and outstanding scientific gathering of the scientific oncology neighborhood. Presenting scientific growth progress on the ASCO Annual Assembly for the seventh consecutive yr, Ascentage had 4 scientific research of three of the corporate’s proprietary drug candidates chosen for shows, together with an oral report, at ASCO 2024.

Outcomes introduced this yr reaffirmed the therapeutic potential of APG-2449 in NSCLC, with information demonstrating preliminary efficacy in sufferers with NSCLC who have been TKI naïve and immune to second-generation ALK TKIs, in addition to early antitumor exercise in mind metastases. Biomarker analysis confirmed that, in sufferers with NSCLC immune to second-generation ALK TKIs, phosphorylated FAK (pFAK) expression ranges in tumor tissue at baseline and discount in pFAK ranges in peripheral blood mononuclear cells (PBMCs) have been correlated with responses to APG-2449.

“APG-2449 is an effective multitargeted inhibitor that acts on FAK/ALK/ROS1. Compared to the data released at last year’s ASCO Annual Meeting, the latest results presented this year continued to show manageable safety and favorable antitumor activity in patients with NSCLC,” stated Prof. Li Zhang, the principal investigator of this examine from Solar Yat-sen College Most cancers Middle. “We are very encouraged by the preliminary efficacy observed in patients with resistance to second-generation ALK TKIs, as it suggests that multitargeted inhibition on FAK and ALK may offer a new strategy for the management of patients with NSCLC resistant to second-generation ALK TKIs. We hope that Ascentage Pharma will conduct further studies on APG-2449 and allow more patients to benefit from this novel therapeutic agent as soon as possible.”

“These data of APG-2449 in patients with NSCLC revealed a connection between resistance to ALK inhibitors and the FAK pathway, thus suggesting that the multitargeted FAK/ALK/ROS1 TKI APG-2449 may bring renewed hope to patients with NSCLC who are resistant to second-generation ALK inhibitors. This finding is indeed very encouraging,” stated Dr. Yifan Zhai, Chief Medical Officer of Ascentage Pharma. “Remaining committed to the mission of addressing unmet clinical needs in China and around the world, we will press forward with this clinical development program in order to bring a safe and effective new treatment option to patients in need.”

Highlights of those information introduced at ASCO 2024 are as follows:

Up to date examine outcomes of novel FAK/ALK/ROS1 inhibitor APG-2449 in sufferers (pts) with non-small-cell lung most cancers (NSCLC) immune to second-generation ALK inhibitors.

Summary#:  3124

Session Developmental Therapeutics”Molecularly Focused Brokers and Tumor Biology

Date and Time:  June 1, 2024, Saturday, 9:00 AM “ 12:00 PM (Central Time)

First Creator:  Yuxiang Ma, MD, PhD, Solar Yat-sen College Most cancers Middle, Guangzhou, Guangdong, China.

Highlights:

Background: ALK inhibitors improve FAK pathway gene expression in ALK⁺ NSCLC cell traces, with the best induced expression in drug-tolerant persister cells. This implies that FAK pathway activation is concerned within the mechanism that results in ALK TKI resistance in ALK⁺ NSCLC. APG-2449 is an orally energetic FAK inhibitor and a third-generation ALK/ROS1 TKI that has proven potent antitumor exercise in preclinical fashions. This poster experiences additional security and efficacy information of APG-2449.

Affected person enrollment and strategies:

• This examine contains dose-escalation and dose-expansion parts. 1,200 mg each day (QD) was decided because the RP2D. There have been two cohorts within the dose-expansion portion: Cohort 1 included sufferers with NSCLC who have been immune to second-generation ALK TKIs; Cohort 2 included sufferers with NSCLC who have been ALK or ROS1 TKI naïve.
• As of April 2, 2024, a complete of 144 sufferers with NSCLC, mesothelioma, or ovarian most cancers have been handled with APG-2449 at doses starting from 150 “ 1,500 mg. The median (vary) age of sufferers was 53 (21-78) years, and 53.5% have been feminine.

Efficacy outcomes:

• The ORRs of APG-2449 in sufferers with ROS1+ and ALK+ TKI-naïve NSCLC (n=36) have been 68.2% (15/22) and 78.6% (11/14), respectively. Of the 22 sufferers with NSCLC immune to second-generation ALK inhibitors and with out targetable bypass gene mutations (e.g., KRAS G12C, BRAF V600E), 10 achieved PRs (10/22; 45.5%). Among the many sufferers handled at RP2D, 12 had mind metastasis at baseline, 9 of whom achieved intracranial PR, leading to an intracranial ORR of 75.0%.
• Biomarker analysis discovered that, in sufferers with NSCLC that was immune to second-generation ALK TKIs, responses to APG-2449 have been correlated with pFAK ranges in tumor tissues at baseline and reductions in pFAK ranges in PBMCs.

Security outcomes: A complete of 129 (89.6%) sufferers had therapy‘associated hostile occasions (TRAEs), essentially the most frequent ( ‰¥10%) of which have been elevated serum creatinine (49.3%), improve in alanine aminotransferase (42.4%), improve in aspartate aminotransferase (36.1%); nausea (28.5%); vomiting (23.6%); diarrhea (22.9%); decreased leukocyte depend (22.2%), decreased neutrophil depend (17.4%) and rash (13.2%). In all, 20 (13.9%) TRAEs have been grade ‰¥ 3.

Conclusions: APG-2449 demonstrated preliminary efficacy in sufferers with NSCLC whose illness was TKI naïve and immune to second-generation ALK inhibitors, particularly in mind metastases. Biomarker analysis confirmed that, in sufferers with NSCLC immune to second-generation ALK TKIs, responses to APG-2449 PFS have been correlated with pFAK ranges in tumor tissues at baseline and reductions in pFAK ranges in PBMCs.

APG-2449 is an investigational drug that has not been permitted in any nation and area.

Appendix: The 4 scientific research of Ascentage Pharma’s three drug candidates, together with lisaftoclax, introduced at this yr’s ASCO Annual Assembly.

About Ascentage Pharma
Ascentage Pharma (6855.HK) is a globally centered biopharmaceutical firm engaged in growing novel therapies for cancers, continual hepatitis B, and age-related ailments. On October 28, 2019, Ascentage Pharma was listed on the Most important Board of the Inventory Change of Hong Kong Restricted with the inventory code 6855.HK.

Ascentage Pharma focuses on growing therapeutics that inhibit protein-protein interactions to revive apoptosis, or programmed cell dying. The corporate has constructed a pipeline of 9 scientific drug candidates, together with novel, extremely potent Bcl-2, and twin Bcl-2/Bcl-xL inhibitors, in addition to candidates aimed toward IAP and MDM2-p53 pathways, and next-generation tyrosine kinase inhibitors (TKIs). Ascentage Pharma can also be the one firm on this planet with energetic scientific packages focusing on all three recognized courses of key apoptosis regulators. The corporate is conducting greater than 40 Section I/II scientific trials, together with 5 international registrational section III research, within the US, Australia, Europe, and China. Ascentage Pharma has been designated for a number of Main Nationwide R&D Initiatives, together with 5 Main New Drug Initiatives, one New Drug Incubator standing, 4 Progressive Drug Packages, and one Main Mission for the Prevention and Therapy of Infectious Ailments.

Olverembatinib, the corporate’s core drug candidate developed for the therapy of drug-resistant continual myeloid leukemia (CML) and the corporate’s first permitted product in China, has been granted Precedence Evaluate Designations and Breakthrough Remedy Designations by the Middle for Drug Analysis (CDE) of China Nationwide Medical Merchandise Administration (NMPA). To this point, the drug had been included into the China 2022 Nationwide Reimbursement Drug Checklist (NRDL). Moreover, olverembatinib has been granted an Orphan Drug Designation (ODD) and a Quick Monitor Designation (FTD) by the US FDA, and an Orphan Designation by the EMA of the EU. To this point, Ascentage Pharma has obtained a complete of 16 ODDs from the US FDA and 1 Orphan Designation from the EMA of the EU for 4 of the corporate’s investigational drug candidates.

Leveraging its strong R&D capabilities, Ascentage Pharma has constructed a portfolio of worldwide mental property rights and entered into international partnerships with quite a few famend biotechnology and pharmaceutical corporations and research institutes comparable to UNITY Biotechnology, MD Anderson Most cancers Middle, Mayo Clinic, Dana-Farber Most cancers Institute, MSD, and AstraZeneca (NASDAQ:). The corporate has constructed a gifted staff with international expertise within the discovery and growth of progressive medication and is setting up its world-class business manufacturing and Gross sales & Advertising groups. One pivotal goal of Ascentage Pharma is to repeatedly strengthen its R&D capabilities and speed up its scientific growth packages, with a view to fulfil its mission of addressing unmet scientific wants in China and all over the world for the good thing about extra sufferers.

Ahead-Trying Statements
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