Ascentage Pharma Receives IND Clearance for BTK Degrader APG-3288 in China

The novel BTK degrader enters clinical development for relapsed/refractory hematologic malignancies

Feb. 5, 2026 at 9:55pm

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Ascentage Pharma, a global biopharmaceutical company, announced that its BTK-targeted protein degrader APG-3288 has received investigational new drug (IND) application clearance from the China Center for Drug Evaluation (CDE). This clears the way for APG-3288 to enter a clinical study in patients with relapsed/refractory hematologic malignancies. The IND clearance in China comes shortly after the drug received IND clearance from the U.S. FDA, marking a significant milestone in Ascentage Pharma's global development strategy.

Why it matters

BTK is a key kinase involved in the activation, proliferation, and survival of B-cells, making it a crucial target for treating B-cell malignancies. While BTK inhibitors have improved treatment outcomes, resistance often develops over time. APG-3288 is designed to overcome this resistance by inducing rapid and selective degradation of BTK, including mutant forms, potentially providing a novel therapeutic approach for patients with relapsed/refractory hematologic cancers.

The details

APG-3288 is a potent and selective BTK degrader developed using Ascentage Pharma's proprietary proteolysis-targeting chimera (PROTAC) technology. Unlike traditional BTK inhibitors, APG-3288 acts by inducing the degradation of BTK, including wild-type and mutant forms associated with resistance to existing BTK inhibitors. This approach aims to block the BCR-BTK signaling axis at its source, potentially overcoming resistance and providing a differentiated treatment option.

  • On February 5, 2026, Ascentage Pharma announced that APG-3288 received IND clearance from the China CDE.
  • The IND clearance in China came shortly after APG-3288 received IND clearance from the U.S. FDA.

The players

Ascentage Pharma Group International

A global, commercial-stage, integrated biopharmaceutical company engaged in the discovery, development, and commercialization of novel, differentiated therapies to address unmet medical needs in cancer.

China Center for Drug Evaluation (CDE)

The regulatory authority in China responsible for reviewing and approving investigational new drug (IND) applications.

U.S. Food and Drug Administration (FDA)

The regulatory authority in the United States responsible for reviewing and approving investigational new drug (IND) applications.

APG-3288

Ascentage Pharma's novel, next-generation Bruton's tyrosine kinase (BTK)-targeted protein degrader.

Yifan Zhai, M.D., Ph.D.

Chief Medical Officer of Ascentage Pharma.

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What they’re saying

“After receiving IND clearances for APG-3288 from the U.S. FDA and then the China CDE, we have reached a significant milestone in the field of targeted protein degradation, taking another major step forward with our global innovation strategy.”

— Yifan Zhai, Chief Medical Officer of Ascentage Pharma

What’s next

Ascentage Pharma will be conducting 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.

The takeaway

The IND clearance for APG-3288 in China marks a significant milestone for Ascentage Pharma's global development strategy, as the company aims to bring this innovative BTK degrader to patients with relapsed/refractory hematologic cancers who desperately need new treatment options.