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FGX15-147-trastuzumab ADC is an antibody-drug conjugate (ADC) developed by Femtogenix, consisting of the HER2-targeting monoclonal antibody trastuzumab conjugated to a novel pyridinobenzodiazepine (PDD) payload, FGX15-147. The payload is a sequence-selective DNA mono-alkylating agent that binds to the minor groove of DNA, specifically targeting regions with two guanines spaced 2-4 base pairs apart. Beyond DNA alkylation, the drug is designed to inhibit the binding of oncogenic transcription factors, such as Hypoxia Inducible Factor (HIF), to their DNA binding sites. In preclinical studies, the ADC demonstrated significant efficacy in low-HER2-expressing pancreatic cancer models and showed a favorable tolerability profile.
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