Shanghai, China, April 27, 2025 – Asieris Pharmaceuticals (www.asieris.cn, 688176.SH), a global biopharmaceutical company focused on developing innovative therapies for genitourinary tumors and women’s health with significant unmet medical needs, and its subsidiary Baylink Biosciences Inc. (www.baylinkbio.com), announced today that findings from three preclinical studies have been presented in poster format at the 2025 American Association for Cancer Research (AACR) Annual Meeting. The meeting, which took place from April 25th to 30th in Chicago, USA, featured the following posters:
ASN-7350, a highly selective FGFR2/3 dual inhibitor, for FGFR2/FGFR3 driven solid tumors
- Poster number：3014
- Session Date and Time: April 28, 2025, 2:00 PM – 5:00 PM
- Introduction: Currently, first-generation pan-FGFR inhibitors have achieved clinical breakthroughs in treating specific solid tumors: Erdafitinib is approved for FGFR-altered advanced/metastatic urothelial carcinoma, while Pemigatinib and Futibatinib are authorized for FGFR2-aberrant intrahepatic cholangiocarcinoma. However, These drugs also face dual challenges: 1) off-target toxicity (including hyperphosphatemia and other dose-limiting adverse events) caused by non-selective inhibition of FGFR1/FGFR4 subtypes; 2) frequent acquired resistance mutations in FGFR2/3 kinase domains (e.g., FGFR2 N549K and FGFR3 V555M) during treatment, which substantially compromise long-term efficacy. To address these unmet clinical needs, our research team has successfully developed ASN-7350 – a differentiated FGFR2/3 dual-target small molecule inhibitor.
- Conclusions: Addressing the issues of FGFR1/4-related toxicities and acquired resistance associated with existing pan-FGFR inhibitors, ASN-7350 achieves selective inhibition through a non-covalent binding mechanism. In preclinical studies, it has demonstrated superior broad-spectrum anti-tumor activity compared to peer candidates (e.g., RLY-4008, TYRA-300). This compound effectively overcomes FGFR2/3 resistance mutations while exhibiting a significantly widened therapeutic window, making it applicable for various FGFR2/3-driven solid tumors including bladder cancer, endometrial cancer, and gastric cancer. The project has entered the IND-enabling study and is targeting regulatory approval by the end of 2025.
A linker platform for antibody drug conjugates (ADCs): expanding the therapeutic window
- Poster number: 7463
- Session Date and Time: April 30, 2025, 9:00 AM – 12:00 PM
- Introduction: Although antibody-drug conjugates (ADCs) have demonstrated great clinical potential, their therapeutic window remains narrow due to the complexity of this drug format, which limits their clinical development. The hydrophobicity of the payload and the instability of ADC molecules are key factors. A well-designed linker can improve the hydrophilicity of ADC molecules, enhance their stability, reduce side effects, and expand the therapeutic window.
- Conclusions: We have developed a set of novel linkers that expand the therapeutic window of current ADCs by enhancing their hydrophilicity and stability, reducing off-target effects, and maintaining efficacy. The advantages of these linkers have been demonstrated in multiple projects, with the leading project (CLDN6/9 ADC) expected to complete IND filing in 2026. Additionally, we are further exploring the application of this class of linkers to enable innovative designs of dual-payload ADCs and Degrader–Antibody–Conjugates (DACs).
Preclinical evaluation of BLB-101, a topoisomerase-inhibitor-based anti-CLDN6/9 antibody-drug conjugate featuring a proprietary hydrophilic linker
- Poster number: 1578
- Session Date and Time: April 28, 2025, 9:00 AM – 12:00 PM
- Introduction: Claudin 6 (CLDN6) is a tight junction protein that is highly expressed in various human cancers, including ovarian cancer, endometrial cancer, and non-small cell lung cancer (NSCLC), but is absent in normal adult tissues. Claudin 9 (CLDN9), which shares high homology with CLDN6, exhibits a similar expression pattern—being nearly undetectable in normal tissues but upregulated in ovarian and endometrial cancers. We propose to simultaneously target both CLDN6 and CLDN9 with antibody-drug-conjugate (ADC) to enhance anti-tumor efficacy and provide treatment options for a broader patient population.
- Conclusions: We successfully identified a high-affinity antibody that specifically binds to CLDN6 and CLDN9 while avoiding interaction with other Claudin family members. BLB-101 is an antibody-drug conjugate (ADC) candidate that incorporates 2D5S (CLDN6/9 Ab) and the topoisomerase I inhibitor, exatecan as payload, along with our proprietary hydrophilic linker, BL001. BLB-101 demonstrates excellent biological activity, favorable in vivo pharmacokinetics (PK), and excellent developability. It exhibits strong cytotoxic effects across multiple antigen-positive cancer cell lines. In xenograft models expressing CLDN6 or CLDN9, BLB-101 achieved tumor elimination at low doses. Additionally, BLB-101 was well tolerated in non-human primates. Collectively, these findings provide strong support for the continued clinical development of BLB-101.
As shown in the above reports of two drug products in development and a technology platform, Asieris Pharmaceuticals and its ADC-focused subsidiary Baylink Biosciences Inc. have demonstrated their impressive new drug development ability. These products have potential in dramatically improving the lives of cancer patients.
About Asieris
Asieris Pharmaceuticals(688176.SH), founded in March 2010, is a global biopharma company specializing in discovering, developing and commercializing innovative drugs for the treatment of genitourinary tumors and other related diseases. We strive to improve human health to preserve patient’s dignity. We aim to become a global pharma leader that integrates R&D, manufacturing and commercialization in our areas of focus, as we provide best-in-class integrated diagnosis and treatment solutions for patients in China and worldwide.
The company has been developing its proprietary R&D platform and core technologies, exploring new mechanisms of action, and efficiently screening and evaluating drug candidates. With a well-established in-house R&D system and expertise in global drug development, Asieris is committed to launching first-in-class drugs and other innovative products to address huge unmet needs in its areas of focus.
Asieris is also enhancing its pipeline for genitourinary diseases via proprietary R&D and strategic partnerships, while closely following cutting-edge technologies and therapeutics. The company strives to discover and identify unmet clinical needs, and adopts a forward-looking approach in product planning and life-cycle management. We aim to establish an outstanding portfolio that covers diagnosis and treatment in a bid to benefit more patients in China and globally.
