Teplizumab
Monoclonal antibody
From Wikipedia, the free encyclopedia
Teplizumab, sold under the brand name Tzield among others, is an anti-CD3 humanized monoclonal antibody and the first approved treatment indicated to delay the onset of stage 3 type 1 diabetes in people living with stage 2 type 1 diabetes.[7][8][9]
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Humanized (from mouse) |
| Target | CD3 |
| Clinical data | |
| Trade names | Tzield, others |
| Other names | teplizumab-mzwv, PRV-031,[1] MGA031 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a622077 |
| License data |
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| Routes of administration | Intravenous |
| Drug class | Antidiabetic agent |
| ATC code | |
| Legal status | |
| Legal status | |
| Identifiers | |
| CAS Number | |
| DrugBank | |
| ChemSpider |
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| UNII | |
| KEGG | |
| Chemical and physical data | |
| Formula | C6462H9938N1738O2022S46 |
| Molar mass | 145801.49 g·mol−1 |
Teplizumab's mechanism of action involves binding to CD3 protein complexes (a molecule involved in recognising antigens and activating T cells) on the surface of T-cells and modifying T-cell immune behaviour to reduce cytotoxicity.[10] This appears to involve weak agonistic activity on signaling via the T cell receptor-CD3 complex associated with the development of anergy, unresponsiveness, and/or apoptosis, particularly of unwanted activated T effector cells. In addition, regulatory cytokines are released and regulatory T cells are expanded that may lead to the reestablishment of immune tolerance. [11][12] To avoid overly stimulating cytokine release, the Fc region of this antibody has been engineered to have Fc receptor non-binding (FNB) properties.[10]
Teplizumab was approved for medical use in the United States in November 2022,[7][13] and in the European Union in January 2026.[5][6] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.[14][15]
Medical uses
Teplizumab is indicated to delay the onset of stage 3 type 1 diabetes in persons over age 1 living with stage 2 type 1 diabetes.[4][7] It also now has US FDA approval for persons aged 8 to 17 with recent diagnosis of stage 3 diabetes to slow the decline of c-peptide.[16]
In June 2026, the US Food and Drug Administration expanded the indication for teplizumab to delay the decline of insulin production in people aged 8 years through 17 years of age who have been recently diagnosed with stage 3 type 1 diabetes.[17][18]
History
Teplizumab was developed at the University of Chicago in partnership with Ortho Pharmaceutical, and was then further developed at MacroGenics, Inc.,[19][20] including a collaboration with Eli Lilly to conduct the first phase III clinical trial in early-onset type 1 diabetes.[21] After the initial Phase III trial conducted by Macrogenics failed to meet the primary endpoint,[22] the drug was acquired by Provention Bio, which restarted development based on subset analysis of the original trials.[23][24]
Society and culture
Legal status
Teplizumab was approved for medical use in the United States in November 2022.[7]
In November 2025, the Committee for Medicinal Products for Human Use of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Teizeild, intended for the treatment of type 1 diabetes.[5] The applicant for this medicinal product is Sanofi Winthrop Industrie.[5][25] Teplizumab was authorized for medical use in the European Union in January 2026.[5][6][26]
Research
Teplizumab has been used in clinical trials with the aim of protecting the remaining β-cells in people newly diagnosed with type 1 diabetes.[27] Immunomodulatory agents such as anti-CD3-antibodies may restore normal glucose control if provided in very early stages of the disease, such as stage 2 T1DM, when there are still enough beta cells to maintain euglycemia.[28]
Teplizumab has been evaluated for treatment of renal allograft rejection, for induction therapy in islet transplant recipients, and for psoriatic arthritis.[29]
A phase II study showed that teplizumab could delay the development of diabetes in family members of type 1 diabetics showing signs of progression towards diabetes by about two years after a single treatment, renewing interest in its use as a preventive rather than therapeutic treatment in high-risk patients.[30]
A systematic review and meta-analysis, published in 2024, found that use of teplizumab is associated with better preservation of circulating C-peptide levels.[31]
