Compound Development and Early Research

Initial discovery and modeling of ALDH1A3 inhibitors by researchers at Dalhousie University and the University of Pisa.

Details:

• The foundation of Theranib’s innovation began with breakthrough research on ALDH1A3, a protein linked to chemotherapy resistance and metastasis.
• Researchers at Dalhousie University and the University of Pisa collaborated to understand the molecular mechanisms of ALDH1A3’s role in cancer progression.
• Using computational modeling, the team designed and tested multiple small-molecule inhibitors to identify those with the best potential for efficacy and specificity.

Achievements:

• Lead Compound Discovery: The identification of VE3, a first-in-class ALDH1A3 inhibitor, demonstrated nanomolar potency and exceptional specificity without off-target effects.
• Structure-Activity Relationships (SAR): Generated comprehensive SAR data to guide future compound optimization.
• Proof of Concept: Early in vitro studies confirmed VE3’s ability to inhibit tumor growth in breast cancer cell lines, setting the stage for preclinical animal studies.

Strategy:

• Focused on small-molecule drug development to ensure scalability and cost-effectiveness during manufacturing.
• Prioritized specificity to reduce off-target effects and potential toxicity, increasing the likelihood of regulatory approval.
• Leveraged academic partnerships to minimize initial development costs while accessing cutting-edge research facilities and expertise.

Impact:

• Positioned Theranib as the first company to develop a highly specific ALDH1A3-targeted therapy, addressing an unmet need in oncology.
• Built a robust knowledge base for patent filings and further compound development.