ROCKVILLE, Md. and SUZHOU, China — February 5, 2026 — Leads & Copy —
Ascentage Pharma Group International (NASDAQ: AAPG; HKEX: 6855) announced that its novel next-generation Bruton’s tyrosine kinase (BTK)-targeted protein degrader, APG-3288, has received investigational new drug (IND) application clearance from the China Center for Drug Evaluation (CDE) and is poised to enter a clinical study in patients with relapsed/refractory hematologic malignancies.
The IND clearance from the China CDE came shortly after the IND was cleared by the U.S. Food and Drug Administration (FDA). The clearance ushers in a new phase in the multicenter clinical development of APG-3288 and highlights Ascentage Pharma’s global development capabilities in the field of targeted protein degradation.
Ascentage Pharma will conduct a multicenter, open-label Phase I study to evaluate the safety, tolerability, pharmacokinetic (PK) profile, and preliminary efficacy of APG-3288 in patients with relapsed/refractory hematologic malignancies.
BTK is a key kinase in the B-cell receptor (BCR) signaling pathway and plays a central role in the activation, proliferation, and survival of B-cells. Aberrant BTK activation is associated with the initiation and progression of multiple B-cell malignancies such as B-cell lymphoma, chronic lymphocytic leukemia (CLL), and Waldenström’s macroglobulinemia (WM). BTK inhibitors have drastically improved treatment outcomes for patients with B-cell malignancies.
BTK mutations and remodeling of signaling pathways often lead to acquired resistance during prolonged treatment. There remains an urgent clinical need for new drugs promising novel mechanisms of action.
APG-3288 is a potent and selective BTK degrader developed utilizing Ascentage Pharma’s proteolysis-targeting chimera (PROTAC) technology platform. The candidate induces the formation of a ternary complex consisting of the BTK target, the PROTAC, and the Cereblon E3 ubiquitin ligase, leading to proteasome-mediated degradation of the BTK target.
APG-3288 is designed to act through degradation rather than inhibition, inducing rapid, potent, selective, and sustained degradation of both wild-type BTK and multiple BTK mutants associated with resistance to existing BTK inhibitors. This approach blocks the BCR-BTK signaling axis at its source, overcoming resistance to BTK inhibitors and potentially providing a therapeutic strategy for BTK-targeted treatment.
Ascentage Pharma has dedicated many years to building a presence in the field of hematologic malignancies with a portfolio that includes Olverembatinib and Lisaftoclax, two products approved in China. The IND clearance for APG-3288 in China will further strengthen the Company’s pipeline in hematologic malignancies and lay a foundation for potential combinations with other assets within the pipeline.
Yifan Zhai, M.D., Ph.D., Chief Medical Officer of Ascentage Pharma, said the IND clearances for APG-3288 from the U.S. FDA and the China CDE mark a milestone in the field of targeted protein degradation. Zhai said there is considerable unmet clinical need in patients with hematologic malignancies, particularly drug-resistant patients who lack treatment options. Ascentage Pharma will advance the global clinical development program for APG-3288 and explore its combinatory potential in efforts to bring this therapeutic to patients in China and around the world.
APG-3288 is currently under investigation and has not been approved by the U.S. FDA.
Ascentage Pharma Group International (NASDAQ: AAPG; HKEX: 6855) is a global, commercial stage, integrated biopharmaceutical company engaged in the discovery, development and commercialization of therapies to address unmet medical needs in cancer. The Company has built a pipeline of drug products and candidates that includes inhibitors targeting key proteins in the apoptotic pathway, next-generation kinase inhibitors, as well as protein degraders.
The lead asset, Olverembatinib, is the first third-generation BCR-ABL1 inhibitor approved in China for the treatment of patients with CML in chronic phase (CML-CP) with T315I mutations, CML in accelerated phase (CML-AP) with T315I mutations, and CML-CP that is resistant or intolerant to first and second-generation TKIs. All indications are covered by the China National Reimbursement Drug List (NRDL). The Company is conducting an FDA-cleared, global registrational Phase III trial, or POLARIS-2, of Olverembatinib for CML, as well as global registrational Phase III trials for patients with newly diagnosed Ph+ ALL and SDH-deficient GIST patients.
The Company’s second approved product, Lisaftoclax, is a novel Bcl-2 inhibitor for the treatment of hematologic malignancies. Lisaftoclax is being commercialized in China following National Medical Products Administration (NMPA) approval for the treatment of adult patients with chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) who have previously received at least one systemic therapy including BTK inhibitors. The Company is conducting four global registrational Phase III trials: the FDA-cleared GLORA study of Lisaftoclax in combination with BTK inhibitors in patients with CLL/SLL previously treated with BTK inhibitors for more than 12 months with suboptimal response; the GLORA-2 study in patients with newly diagnosed CLL/SLL; the GLORA-3 study in newly diagnosed, elderly and unfit patients with acute myeloid leukemia (AML); and the GLORA-4 study in patients with newly diagnosed higher-risk myelodysplastic syndrome (HR MDS), a study that was simultaneously cleared by the U.S. FDA, the EMA of the EU, and China CDE.
Ascentage Pharma has built a portfolio of global intellectual property rights and entered into global partnerships and other relationships with biotechnology and pharmaceutical companies, such as Takeda, AstraZeneca, Merck, Pfizer, and Innovent, in addition to research and development relationships with research institutions, such as Dana-Farber Cancer Institute, Mayo Clinic, National Cancer Institute and the University of Michigan.
Source: Ascentage Pharma
