TQB2102 is a bispecific epitope antibody-drug conjugate targeting HER2, composed of the antibody Rolditamig and the toxin molecule Deruxtecan-d 2. TQB2102 binds to the ECD2 and ECD4 domains of HER2, promotes its own internalization by HER2-expressing cells, and delivers deuterated DXd payload to inhibit topoisomerase I. TQB2102 induces antibody-dependent cellular cytotoxicity, DNA damage, bystander killing activity, and inhibits cancer cell proliferation. TQB2102 can be used in research related to various cancers including metastatic breast cancer, colorectal cancer, and gastric/gastroesophageal junction adenocarcinoma [1] [2].
In Vivo, TQB2102 (0.5-5.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in the NCI-N87 gastric cancer xenograft model[2]. TQB2102 (0.5-5.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in BT-474 breast cancer xenografts[2]. TQB2102 (1.0-10.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in the COLO 205 colorectal cancer xenograft model[2]. TQB2102 (3.0-30.0 mg/kg; intravenous injection; once every 2 weeks; 3 or 7 doses) is well tolerated in cynomolgus monkeys. No significant pulmonary toxicity or organ system damage is observed at the highest dose of 30.0 mg/kg administered once every 2 weeks[2].
In Vitro, TQB2102 (6 h) induces antibody-dependent cell-mediated cytotoxicity (ADCC) in human gastric cancer cell line NCI-N87, with an EC50 of 2.33 ng/mL[2]. TQB2102 (144 h) exhibits bystander killing activity against HER2-negative MDA-MB-468 cells when co-cultured with HER2-positive KPL-4 cells[2]. TQB2102 (44 h) potently inhibits the proliferation of NCI-N87 cells with high HER2 expression, Trastuzumab emtansine -resistant NCI-N87/16-8 cells, and BT-474 cells with moderate HER2 expression, with IC50 values of 66.7 ng/mL, 74.3 ng/mL, and 116.2 ng/mL, respectively, but exerts no inhibitory effect on JIMT-1 cells with low HER2 expression[2]. TQB2102 induces DNA damage, an effect detected by increased phosphorylation levels of γ-H2AX, and this phenomenon occurs in human cancer cell lines NCI-N87 and JIMT-1[2].
References:
[1]. Zhang, et al. Antibody drug conjugate. WO2022033578.
[2]. Ruan DY, et al. Preclinical characterization and phase I results of TQB2102, a first-in-class HER2 biparatopic antibody-drug conjugate, in patients with advanced solid tumors. Annals of oncology: official journal of the European Society for Medical Oncology. 2026 May 15.
In Vivo, TQB2102 (0.5-5.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in the NCI-N87 gastric cancer xenograft model[2]. TQB2102 (0.5-5.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in BT-474 breast cancer xenografts[2]. TQB2102 (1.0-10.0 mg/kg; intravenous injection; single administration) achieves dose-dependent tumor growth inhibition in the COLO 205 colorectal cancer xenograft model[2]. TQB2102 (3.0-30.0 mg/kg; intravenous injection; once every 2 weeks; 3 or 7 doses) is well tolerated in cynomolgus monkeys. No significant pulmonary toxicity or organ system damage is observed at the highest dose of 30.0 mg/kg administered once every 2 weeks[2].
In Vitro, TQB2102 (6 h) induces antibody-dependent cell-mediated cytotoxicity (ADCC) in human gastric cancer cell line NCI-N87, with an EC50 of 2.33 ng/mL[2]. TQB2102 (144 h) exhibits bystander killing activity against HER2-negative MDA-MB-468 cells when co-cultured with HER2-positive KPL-4 cells[2]. TQB2102 (44 h) potently inhibits the proliferation of NCI-N87 cells with high HER2 expression, Trastuzumab emtansine -resistant NCI-N87/16-8 cells, and BT-474 cells with moderate HER2 expression, with IC50 values of 66.7 ng/mL, 74.3 ng/mL, and 116.2 ng/mL, respectively, but exerts no inhibitory effect on JIMT-1 cells with low HER2 expression[2]. TQB2102 induces DNA damage, an effect detected by increased phosphorylation levels of γ-H2AX, and this phenomenon occurs in human cancer cell lines NCI-N87 and JIMT-1[2].
References:
[1]. Zhang, et al. Antibody drug conjugate. WO2022033578.
[2]. Ruan DY, et al. Preclinical characterization and phase I results of TQB2102, a first-in-class HER2 biparatopic antibody-drug conjugate, in patients with advanced solid tumors. Annals of oncology: official journal of the European Society for Medical Oncology. 2026 May 15.