2559056-68-5
Chemical Structure
Biological Activity: Xaluritamig (AMG-509) is a bispecific T cell engager and cytolytic agent with a Kd of 27.6 nM for human CD3ε. Xaluritamig binds to CD3ε via an anti-CD3 single-chain variable fragment (scFv) domain, and to STEAP1 via a bispecific anti-STEAP1 antigen-binding fragment (Fab) domain, thereby recruiting and activating T cells and forming a bridge between T cells and STEAP1-expressing cancer cells. Xaluritamig induces T cell-mediated redirected cytotoxicity, tumor cell lysis, cytokine release, CD8+ T cell activation and expansion, as well as tumor stasis or regression. Xaluritamig contains an Fc domain with no effector function, which prolongs serum half-life, exhibits only minimal activity against cells with low STEAP1 expression and normal cells, and shows extremely low target-related off-tumor toxicity in cynomolgus monkeys. Xaluritamig is used in STEAP1×CD3 XmAb 2+1 immunotherapy and in research on metastatic castration-resistant prostate cancer and Ewing sarcoma[1][2][3].
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Xaluritamig | ≥99% | Xaluritamig (AMG-509) is a bispecific T cell engager and cytolytic agent with a Kd of 27.6 nM for human CD3ε. Xaluritamig binds to CD3ε via an anti-CD3 single-chain variable fragment (scFv) domain, and to STEAP1 via a bispecific anti-STEAP1 antigen-binding fragment (Fab) domain, thereby recruiting and activating T cells and forming a bridge between T cells and STEAP1-expressing cancer cells. Xaluritamig induces T cell-mediated redirected cytotoxicity, tumor cell lysis, cytokine release, CD8+ T cell activation and expansion, as well as tumor stasis or regression. Xaluritamig contains an Fc domain with no effector function, which prolongs serum half-life, exhibits only minimal activity against cells with low STEAP1 expression and normal cells, and shows extremely low target-related off-tumor toxicity in cynomolgus monkeys. Xaluritamig is used in STEAP1×CD3 XmAb 2+1 immunotherapy and in research on metastatic castration-resistant prostate cancer and Ewing sarcoma. | ||||||||||||||||||||
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- [1]. Kelly WK, et al. Xaluritamig, a STEAP1 × CD3 XmAb 2+1 Immune Therapy for Metastatic Castration-Resistant Prostate Cancer: Results from Dose Exploration in a First-in-Human Study. Cancer Discov. 2024 Jan 12;14(1):76-89. [Content Brief]
- [2]. Li C, et al. 718 AMG 509, a STEAP1 x CD3 bispecific XmAb® 2+ 1 immune therapy, exhibits avidity-driven binding and preferential killing of high STEAP1-expressing prostate and Ewing sarcoma cancer cells[J]. 2020.
- [3]. Raychaudhuri R, et al. Xaluritamig: A first step towards a new target, new mechanism for metastatic prostate cancer[J]. AME Clinical Trials Review, 2024, 2: 44.
Keywords