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MiniAp4-trastuzumab conjugate (also known as Tz-MiniAp4) is a preclinical-stage antibody-shuttle conjugate (ASC) developed by Gate2Brain. It consists of the anti-HER2 monoclonal antibody trastuzumab site-specifically conjugated to four molecules of MiniAp-4, a protease-resistant blood-brain barrier (BBB) shuttle peptide. The MiniAp-4 peptide facilitates transcytosis across the BBB and blood-tumor barrier (BTB), enabling the large antibody molecule to access the central nervous system. Once across, trastuzumab binds to human epidermal growth factor receptor 2 (HER2) on tumor cells, inhibiting downstream signaling and preventing the development and growth of HER2-positive brain metastases. This therapeutic candidate is being investigated for the prevention and treatment of HER2-related brain metastasis.
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