Basiliximab Overview

Introduction to Basiliximab

Basiliximab, commercially known as Simulect®, is a chimeric monoclonal antibody engineered to provide immunosuppressive therapy for kidney cancer particularly. It is a glycoprotein with a molecular weight of approximately 144 kDa, produced through the fermentation of a genetically engineered mouse myeloma cell line. This recombinant chimeric monoclonal antibody (IgG1k) specifically binds to and blocks the interleukin-2 receptor alpha subunit (IL-2R alpha, also known as CD25 antigen) which can be found on the surface of activated T-lymphocytes.

Biological and Chemical Properties of Basiliximab

Protein Structure

Basiliximab is a chimeric monoclonal antibody and is composed of heavy and light chains, both chains with a distinct amino acid sequence. The heavy chain sequence is characterized by a specific string of amino acids, which contributes to its immunosuppressive properties.

Protein Formula

C₆₃₇₈H₉₈₄₄N₁₆₉₈O₁₉₉₇S₄₈

Average Protein Weight

The average weight of the protein is 143801.3 Da.

The Mechanism of Basiliximab Action

Basiliximab exerts its immunosuppressive effect as an IL-2 receptor antagonist. It binds with high specificity to the alpha-subunit (CD25) of the high-affinity IL-2 receptor, thereby inhibiting the binding of IL-2 which plays a critical role in the proliferation and differentiation of T-cells. This action prevents T-cell activation and the subsequent immune response against the transplanted organ. By doing so, basiliximab effectively reduces the incidence of acute organ rejection. Here is a detailed breakdown of its mechanism:

• Binding to CD25: Basiliximab specifically binds to the alpha subunit (Tac antigen or CD25) of the IL-2 receptor on activated T lymphocytes, thereby blocking the binding site for IL-2.
• Blocking IL-2 Interaction: By occupying the IL-2Rα, basiliximab prevents interleukin-2 (IL-2) from binding to its receptor, thus inhibiting the IL-2-mediated signaling pathway.
• Inhibition of T-cell Proliferation: IL-2 is crucial for the proliferation of activated T-lymphocytes. By blocking IL-2 binding, basiliximab effectively suppresses the clonal expansion of these cells, which is essential for the immune response.
• Reduction in Immune Response: This inhibition results in a reduced immune response, thereby decreasing the likelihood of organ rejection in transplant patients.

Figure 1. The mechanism of Basiliximab action (Creative Biolabs Original)

The Clinical Application of Basiliximab

Basiliximab's primary clinical application is in the prophylactic treatment of kidney transplant rejection. It is used in conjunction with other immunosuppressants to prevent acute graft rejection after organ transplantation, including kidney, liver, and other transplants. The drug has been shown to improve outcomes in renal transplantation by reducing the rate of acute rejection episodes. Beyond transplantation, a real-world analysis known as the BRIGHT study evaluated basiliximab's efficacy and safety in treating steroid-refractory acute graft-versus-host disease (SR-aGVHD) in a large-scale, multicenter study in China, demonstrating its potential use beyond its traditional indication.

Basiliximab is primarily utilized in:

1. Renal Transplantation: It is most commonly indicated for the prophylaxis of acute organ rejection in adult and pediatric patients undergoing renal transplantation. It is administered as part of an immunosuppressive regimen that typically includes corticosteroids and cyclosporine or other immunosuppressive agents.
2. Liver Transplantation: Although its primary indication is for renal transplantation, basiliximab has also been investigated and used off-label in liver transplantation to prevent acute rejection episodes.
3. Other Organ Transplantation: Studies and clinical trials have explored its utility in other organ transplants, including heart and lung, though to a lesser extent compared to renal transplants.
4. Autoimmune Diseases: Research has been conducted to explore the use of basiliximab in treating autoimmune diseases due to its ability to modulate the immune system by targeting activated T-cells. However, its primary clinical application remains in transplantation medicine.

Clinical Projects of Basiliximab*

* The table is excerpted from the following website: https://clinicaltrials.gov/search?cond=Basiliximab

Approved Drugs of Basiliximab**

INN (trade name)	Therapeutic area	Dose	Strength	Route	Company	Marketing start	Market
SIMULECT	Chronic Lymphocytic Leukemia(CLL)	Injection	10MG	VIAL; SINGLE-USE	NOVARTIS	05/12/1998

** Information presented in the table is collected from the following website: https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=BasicSearch.process

What We Provide

Basiliximab

Anti-Human CD20 Recombinant Antibody (Basiliximab)

We provide high-quality basiliximab for use in FC, IP, ELISA, Neut, FuncS, IF, WB, and most other immunological methods. The product is for lab research use only, not for diagnostic, therapeutic, or any in vivo human use.

Specification

• Immunogen
• The details of the immunogen for this antibody are not available.

• Host Species
• Mouse

• Derivation
• Chimeric (mouse/human)

• Type
• IgG1 - kappa

• Specificity
• Tested positive against native human antigen

• Species Reactivity
• Human

• Applications
• Suitable for use in FC, IP, ELISA, Neut, FuncS, IF, WB and most other immunological methods.

• Trade name
• simulect

• CAS
• 152923-56-3

• Generic Name
• Basiliximab

• Biological Half-Life
• 7.2 days

• ATC Code
• L04AC02

• DrugBank
• DB00074

• UNII
• 9927MT646M

• ChEMBL
• CHEMBL1201439

• MW
• 143,801.3 g/mol

• Related Disease
• Kidney transplant rejection, acute

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For research use only. Not intended for any clinical use.