SYN004

Autoradiography and NanoSPECT/CT confirmed the sustained retention of I-LR004 at the tumor site in xenograft mice. These findings demonstrated the adequate tumor targeting capabilities of I-LR004 in EGFR-positive tumors, which may improve dosing strategies and future drug development.

P1b/2a, N=36, Recruiting, Theriva Biologics, Inc. | Trial completion date: Dec 2024 --> Dec 2025 | Trial primary completion date: Dec 2023 --> Dec 2024

P1, N=22, Active, not recruiting, Synermore Biologics Co., Ltd. | Recruiting --> Active, not recruiting | N=36 --> 22 | Trial completion date: May 2022 --> Sep 2023 | Trial primary completion date: Feb 2022 --> Jul 2023

By harnessing the payload DM1 and a monoclonal antibody LR004 through a noncleavable linker succinimidyl-4-(N-maleimidomethyl)-cyclohexane-1-carboxylate, we designed and evaluated an antibody-drug conjugate LR-DM1 with an appropriate drug-antibody ratio of 3.6...Moreover, LR-DM1 possessed a relatively broad therapeutic index with a half-lethal dose above 300 mg/kg, which was over 15-fold higher than the highest administration dosage of 20 mg/kg. This initial study on LR-DM1 holds promise for further development of a new antibody drug conjugate that is transformative for treatment of patients concerned.

LR004-VC-MMAE showed effective antitumor activity by inhibiting the activation of EGFR signaling and the expression of cancer stemness marker genes. It might be a promising therapeutic candidate and provides a potential therapeutic avenue for the treatment of EGFR-positive TNBC.

P1, N=36, Recruiting, Synermore Biologics Co., Ltd. | Trial completion date: Dec 2021 --> May 2022 | Trial primary completion date: Sep 2021 --> Feb 2022