Akeso Announces First ADC Drug Clinical Trial, Marking a New Era for "IO 2.0 + ADC" Strategy

HONG KONG, Feb. 27, 2025 /PRNewswire/ -- Akeso, Inc. (9926.HK) announced the first patient has been enrolled in the Phase I clinical trial of AK138 D1 for the treatment of advanced malignancies in Australia. AK138D1,  a self-developed and differentiated HER3-targeting ADC (antibody-drug conjugate),  is Akeso's first ADC drug to enter clinical studies.

Akeso is dedicated to transforming the global oncology treatment landscape by establishing new standards of care for cancer patients worldwide. A key element of this mission is the company's "IO 2.0 + ADC" strategy. Akeso's self-developed, first-in-class bispecific antibodies, cadonilimab (PD-1/CTLA-4) and ivonescimab (PD-1/VEGF), have both received regulatory approval and are now available to patients in China. Akeso is the only global biopharmaceutical company with two approved bispecific checkpoint antibodies for cancer immunotherapy.

The continued development of differentiated ADC therapies, such as AK138D1, further extend Akeso's ability to explore the full clinical potential of its innovative in-house pipeline and to create synergistic new combination treatment options includes that multiple checkpoints and tumor targets.

Dr. Xia Yu, Founder, Chairwoman, President and CEO of Akeso said,

"The initiation of the clinical study for AK138D1 in Australia marks a pivotal moment in Akeso's strategic advancement into next-generation ADC therapies. Building on our global prominence in bispecific antibodies and a robust pipeline of high-potential drug candidates, the development of AK138D1 and subsequent ADCs/bispecific ADCs will significantly bolster our product offering. This is part of Akeso's continued effort to redefine standard of care in cancer treatment.

Following our achievements in bispecific antibody development, ADC therapies have emerged as a strategic priority for Akeso. Based on our extensive experience in bispecific antibody development, we are excited by the potential of our proprietary ADCs and bispecific ADCs.  Our goal is to enhance drug efficacy while minimizing ADC toxicity, offering transformative treatment alternatives for patients worldwide.

Moreover, Akeso has established cutting-edge ADC research, pilot production, and manufacturing facilities.  These investments position us for high-quality clinical development and for global market expansion of our ADC portfolio."

HER3 has emerged as an active target in cancer drug development and is the focus of ongoing research. Although experimental drugs targeting HER3 have not shown satisfactory antitumor effects over the past 30 years, studies indicate that HER3 is expressed or overexpressed in various malignancies, including breast cancer, ovarian cancer, lung cancer, colorectal cancer, melanoma, head and neck cancers, cervical cancer, and prostate cancer. Additionally, upregulation of HER3 and its synergistic interactions with other receptors contribute to tumor initiation, metastasis, and resistance to certain anticancer treatments, such as resistance to EGFR-targeted therapies, endocrine therapy in breast cancer, HER2-targeted therapies, and chemotherapy.

About AK138D1

Injectable AK138D1 is a HER3-targeted antibody-drug conjugate (ADC), with a fully humanized anti-HER3 IgG1 antibody, patritumab. It is conjugated to the topoisomerase I inhibitor DXd through a cleavable linker, MC-AAA (maleimide-alanine-alanine-alanine). After binding to HER3 on tumor cells, the ADC is internalized into the tumor cells, where the linker is cleaved, releasing the membrane-permeable DXd. This leads to DNA damage and subsequent cell apoptosis. Currently, Akeso has initiated patient enrollment for a Phase I dose-escalation and expansion clinical study in Australia. This study will investigate the safety, tolerability, pharmacokinetics, and preliminary efficacy of AK138D1 for the treatment of advanced malignancies.

About Akeso
Akeso (HKEX: 9926.HK) is a leading biopharmaceutical company committed to the research, development, manufacturing and commercialization of the world's first or best-in-class innovative biological medicines. Founded in 2012, the company has created a unique integrated R&D innovation system with the comprehensive end-to-end drug development platform (ACE Platform) and bi-specific antibody drug development technology (Tetrabody) as the core, a GMP-compliant manufacturing system and a commercialization system with an advanced operation mode, and has gradually developed into a globally competitive biopharmaceutical company focused on innovative solutions. With fully integrated multi-functional platform, Akeso is internally working on a robust pipeline of over 50 innovative assets in the fields of cancer, autoimmune disease, inflammation, metabolic disease and other major diseases. Among them, 23 candidates have entered clinical trials (including 11 bispecific/multispecific antibodies and bispecific antibody-drug conjugates). Additionally, 5 new drugs are commercially available, and 5 new drugs across 7 indications are currently under regulatory review for approval. Through efficient and breakthrough R&D innovation, Akeso always integrates superior global resources, develops the first-in-class and best-in-class new drugs, provides affordable therapeutic antibodies for patients worldwide, and continuously creates more commercial and social values to become a global leading biopharmaceutical enterprise.

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SOURCE Akeso, Inc.