A biparatopic CXCR4-targeted bispecific antibody-drug conjugate (ADC) represents a novel therapeutic strategy in cancer treatment, particularly for tumors that express the CXCR4 receptor. This innovative approach utilizes a bispecific antibody engineered to simultaneously bind two distinct epitopes on the CXCR4 receptor, enhancing binding specificity and therapeutic efficacy. The biparatopic design improves the targeting precision of the ADC, ensuring that the cytotoxic drug payload is delivered predominantly to cancer cells, thereby minimizing off-target effects and reducing toxicity. By focusing on CXCR4, a receptor commonly associated with tumor progression and metastasis, this bispecific ADC holds great promise for treating a variety of cancers that rely on CXCR4 signaling for growth and dissemination. As research advances, biparatopic CXCR4-targeted bispecific ADCs could become key players in precision oncology, providing patients with more effective and targeted cancer therapies.