Product Name: Motixafortide
Form: TFA salt
CAS No: 664334-36-5
Molar Mass: 2159.52
Chemical Formula: C97H144FN33O19S
Synonyms: BKT140 4-fluorobenzoyl
Storage: Store at -20℃
Sequence: RRXCYXKKPYRXCR
Target: CXCR4
Application:
Motixafortide acetate (CAS: 664334-36-5) is a synthetic peptide drug that acts as a CXCR4 antagonist. CXCR4 is a chemokine receptor involved in cell migration and homing, particularly in hematopoietic stem cells and immune cells. Motixafortide acetate functions by competitively binding to CXCR4 receptors, inhibiting the interaction between CXCR4 and its ligand, CXCL12 (also known as stromal cell-derived factor 1, SDF-1). This blockade disrupts signaling pathways critical for tumor cell migration, invasion, and metastasis, as well as for stem cell mobilization. Motixafortide acetate is being investigated for its potential in the treatment of various cancers, including acute myeloid leukemia (AML), multiple myeloma, and certain solid tumors. In pharmaceutical chemistry, motixafortide acetate's targeted antagonism of CXCR4 represents a promising approach to cancer therapy, offering a specific and effective means of inhibiting tumor progression and metastasis. Ongoing clinical trials aim to further evaluate its safety and efficacy in different cancer types, with the goal of providing a valuable addition to anticancer treatment regimens.
Current Research:
Motixafortide acetate is an investigational synthetic peptide with potential therapeutic applications in oncology and hematology, specifically designed to enhance immune cell trafficking and improve immune response to tumors. It is a potent, selective antagonist of the chemokine receptor CXCR4, which is involved in the regulation of immune cell migration. By inhibiting the interaction between CXCR4 and its ligand, CXCL12, Motixafortide acetate promotes the mobilization of hematopoietic stem cells and enhances the infiltration of immune cells into tumor microenvironments. This novel approach is being explored to boost the effectiveness of immunotherapies and chemotherapy, particularly in cancers such as acute myeloid leukemia (AML), non-Hodgkin lymphoma, and solid tumors.
Mechanism of Action
Motixafortide acetate functions by binding to the CXCR4 receptor, preventing its activation by the endogenous ligand CXCL12. CXCR4 is a G-protein-coupled receptor that plays a crucial role in the trafficking and homing of immune cells, including T cells, dendritic cells, and hematopoietic stem cells. By inhibiting CXCR4, Motixafortide acetate induces the mobilization of immune cells from the bone marrow into peripheral circulation, enhancing their ability to reach and infiltrate tumor sites. This action not only improves the immune response against cancer cells but also may enhance the efficacy of other treatments like chemotherapy and immune checkpoint inhibitors. Motixafortide acetate has demonstrated the ability to reduce the tumor microenvironment's immunosuppressive nature by facilitating immune cell recruitment, potentially reversing tumor resistance mechanisms.
Indications and Uses
Motixafortide acetate is being developed for use in various oncology indications, particularly in combination with other therapies to treat hematological malignancies such as acute myeloid leukemia (AML) and non-Hodgkin lymphoma, as well as certain solid tumors. In AML, it has shown promise in improving the mobilization of hematopoietic stem cells for stem cell transplantation, which is a key therapeutic option for patients with this disease. Moreover, Motixafortide acetate is being explored in combination with chemotherapy and other immunotherapies, including immune checkpoint inhibitors, to enhance anti-tumor immunity and overcome resistance mechanisms that limit treatment efficacy in advanced cancers.
Efficacy and Clinical Benefits
In preclinical and early clinical trials, Motixafortide acetate has demonstrated significant efficacy in improving immune cell mobilization and infiltration into tumors. In patients with AML, it has been shown to improve the outcomes of stem cell transplantation by facilitating better engraftment and recovery of hematopoietic function. In solid tumors, especially when used in combination with chemotherapy, Motixafortide acetate has exhibited the ability to enhance the anti-tumor immune response by increasing the presence of immune cells within the tumor microenvironment. Additionally, clinical studies have shown that the combination of Motixafortide acetate and immune checkpoint inhibitors can improve patient responses by overcoming immune evasion strategies employed by tumors.
Safety and Tolerability
Motixafortide acetate has demonstrated a manageable safety profile in clinical trials, with most adverse effects being mild to moderate in nature. The most common side effects include infusion-related reactions such as fever, chills, and headache, which are typical for therapies that affect immune cell trafficking. Other reported side effects include fatigue, nausea, and mild hematological changes like neutropenia or thrombocytopenia, which are expected in patients undergoing cancer treatment. The drug's tolerability has been well-supported by its use in combination with chemotherapy, with no unexpected toxicity observed in early-phase trials. However, as with all therapies that modify immune responses, there is a risk of increasing the potential for infections, and careful monitoring is required during treatment.
Advantages and Limitations
Motixafortide acetate's main advantage is its ability to enhance the mobilization of immune cells to the tumor site, potentially improving the effectiveness of cancer therapies, including chemotherapy and immune checkpoint inhibitors. This could lead to better treatment outcomes, particularly in patients with advanced, refractory cancers. Moreover, its role in improving stem cell mobilization could make it a valuable adjunct in hematopoietic stem cell transplantation. However, its use is currently limited to clinical trials, and further data is needed to establish its long-term safety and efficacy. As an intravenous agent, it may not be suitable for all patients, especially those requiring more convenient outpatient therapies. Furthermore, while Motixafortide acetate holds promise in enhancing the anti-tumor immune response, the full extent of its impact in combination therapies and its long-term outcomes remain to be fully realized.
Future Directions
The future development of Motixafortide acetate is focused on expanding its use in combination therapies for a variety of cancers, particularly hematological malignancies and solid tumors. Ongoing clinical trials are exploring its role in conjunction with chemotherapy, immune checkpoint inhibitors, and targeted therapies to maximize its therapeutic potential. Further research will help define the optimal patient populations, treatment regimens, and safety profiles for Motixafortide acetate, potentially leading to broader clinical applications. In addition, studies are investigating its use in other immune-modulating roles, such as enhancing immune responses in patients with chronic infections or other immune-related conditions.
Reference:
Get a Quote
LinkPeptide
