BigHat Biosciences, a clinical-stage, AI-driven protein therapeutics platform company, today announced that the first patient has been dosed in its Phase 1 clinical trial evaluating BHB810, a novel, potentially best-in-class Cadherin-17 (CDH17)-directed VHH-Fc antibody-drug conjugate (ADC) for the treatment of gastric cancer and other advanced gastrointestinal (GI) malignancies. BHB810 was engineered using BigHat’s AI-powered antibody design platform to combine potent antitumor activity against CDH17-expressing tumors with a differentiated safety profile and favorable manufacturability.

“The treatment of the first patient with BHB810 marks an important step forward in our mission to enable transformative AI-designed therapeutics and comes during a period of steady momentum for BigHat, as we continue to advance both our pipeline of novel therapeutics and AI platform,” says Peyton Greenside, Co-founder and CEO of BigHat. “This is the first program we’ve taken from AI-generated design into human studies, validating the ability of our platform to identify and develop promising antibodies into clinic-ready therapeutics. BHB810 could offer a differentiated approach to address a target that has been difficult to drug well, and we are excited by the potential to offer a much-needed new treatment option for patients living with GI cancers.”

The first-in-human, Phase 1 dose escalation trial will evaluate the safety, tolerability, pharmacokinetics, and preliminary antitumor activity of BHB810. The trial will initially enroll patients with advanced gastric and gastroesophageal (GEJ) tumors.

“Despite recent advances, patients with advanced gastric cancers and other GI malignancies continue to face substantial unmet medical needs,” says Principal Investigator Alexander Spira, MD, PhD, Chief Executive Officer and Chief Scientific Officer of NEXT Oncology-Virginia and Co-Director of the Virginia Cancer Specialists Research Institute. “We are excited to help advance BHB810, a potentially best-in-class CDH17-targeted antibody-drug conjugate developed using BigHat’s AI-driven antibody engineering platform, as a potential new treatment option for patients.”

Across a preclinical program spanning nearly 30 patient- and cell-derived tumor models, including gastric cancers with low and heterogeneous CDH17 expression, BHB810 drove complete or near-complete tumor clearance. Its compact antibody format and highly stable payload technology also translated into a favorable safety profile in preclinical studies.

Beyond BHB810, BigHat is developing a portfolio of investigational therapeutics. BHB299, an avidity-driven TCE targeting CEACAM6 for the treatment of solid tumors, is expected to enter the clinic in 2027. BigHat has also designed multiple antibody therapeutics with Merck and Johnson & Johnson, in addition to multiple active collaborations, including Eli Lilly to design antibodies with enhanced functionality for patients with chronic disease.

For more information, visit www.bighatbio.com.