BLB-101 / Asieris - LARVOL DELTA

The KIF18A Inhibitor ATX020 Induces Mitotic Arrest and DNA Damage in Chromosomally Instable High-Grade Serous Ovarian Cancer Cells. (PubMed, Cells) - "Mechanistically, ATX020 blocks KIF18A's plus-end movement on spindle fibers, increasing spindle length, resulting in chromosomal mis-segregation, aneuploidy, and DNA damage. Our findings suggest that ATX020 inhibits CIN+ HGSOC cells mainly by inducing mitotic arrest and DNA damage, disrupting KIF18A's function crucial for mitosis."

Journal • High Grade Serous Ovarian Cancer • Oncology • Ovarian Cancer • Solid Tumor • KIF18A • TP53

Discovery of Kinesin KIF18A Inhibitor ATX020: Tactical Application of Silicon Atom Replacement. (PubMed, ACS Med Chem Lett) - "ATX020 is a potent KIF18A inhibitor with a high degree of kinesin selectivity, favorable in vitro and in vivo ADME properties, and robust efficacy in the OVCAR-3 cell-derived xenograft (CDX) model. A high-resolution crystal structure of the KIF18A-tubulin complex and an experimentally guided model of ATX020 bound to the complex are provided, supporting future structure-based drug design of KIF18A inhibitors."

Journal • Oncology • KIF18A

Focusing on strategic expansion in key areas and fast-tracking high-impact R&D initiatives (PRNewswire) - "Progress on APL-2501 (CLDN6/9 ADC) is also on track, with its preclinical research and unique linker platform selected for a poster presentation at the 2025 American Association for Cancer Research Annual Meeting (AACR 2025)...APL-2401 — a dual FGFR2/3 small molecule inhibitor — has entered IND-enabling studies, with its findings selected for a poster presentation at AACR 2025."

Preclinical • Oncology

Preclinical evaluation of BLB-101, a topoisomerase-inhibitor-based anti-CLDN6/9 antibody-drug conjugate featuring a proprietary hydrophilic linker (Asieris Pharma Press Release) - "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."

Preclinical • Solid Tumor

A linker platform for antibody drug conjugates (ADCs): expanding the therapeutic window (AACR 2025) - "Additionally, BLB-101 ADC, featuring the same linker, was well tolerated in non-human primates following repeated administration. In conclusion, our novel linker designs offer significant advantages, with features that could expand the therapeutic window of current ADCs by improving their stability, reducing off-target effects, increasing bystander activity, and maintaining efficacy. We are also expanding the utility of this class of linkers to enable ubiquitous design of dual-payload-ADC Degrader-Antibody-Conjugates."

Oncology

Baylink Biosciences To Highlight New Preclinical Data At The American Association For Cancer Research (AACR) Annual Meeting (ACCESSWIRE) - "Baylink Biosciences today announced that new preclinical data from its portfolio will be presented at the American Association for Cancer Research (AACR) Annual Meeting....Preclinical data from Baylink's most advanced candidate (BLB-101) will be presented....Data generated to support the rationale for Baylink's innovative linker platform will also be presented. Baylink's linker platform is designed to reduce non-specific uptake into healthy tissues and cells while enhancing potency by improving ADC's homogeneity, stability, PK, and efficacy."

Preclinical • Solid Tumor

Preclinical evaluation of BLB-101, a topoisomerase-inhibitor-based anti-CLDN6/9 antibody-drug conjugate featuring a proprietary hydrophilic linker (AACR 2025) - "Additionally, repeated administration of BLB-101 was well tolerated in both mice and in non-human primates. Together, these findings provide strong support for the continued development of BLB-101directed against CLDN6/CLDN9 positive tumors."

Preclinical • Endometrial Cancer • Oncology • Ovarian Cancer • Solid Tumor • CLDN6