Teplizumab
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Humanized (from mouse) |
| Target | CD3 |
| Clinical data | |
| Trade names | Tzield |
| 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 |
| (what is this?) (verify) | |
Teplizumab, sold under the brand name Tzield, is a humanized anti-CD3 monoclonal antibody that is the first approved treatment indicated to delay the onset of stage 3 type 1 diabetes in people with stage 2 type 1 diabetes.[4][5][6]
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.[7] 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. [8][9] To avoid overly stimulating cytokine release, the Fc region of this antibody has been engineered to have Fc receptor non-binding (FNB) properties.[7]
Teplizumab was approved for medical use in the United States in November 2022.[4][10] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.[11][12]
- ^ "Provention Bio Announces PRV-031 (Teplizumab) Granted PRIME Designation by the European Medicines Agency" (Press release). Provention Bio. 24 October 2019. Retrieved 18 November 2022 – via PR Newswire.
- ^ "Summary Basis of Decision for Tzield". Drug and Health Products Portal. 18 June 2025. Retrieved 10 July 2025.
- ^ "Tzield- teplizumab-mzwv injection". DailyMed. 17 November 2022. Retrieved 4 December 2022.
- ^ a b "FDA Approves First Drug That Can Delay Onset of Type 1 Diabetes". U.S. Food and Drug Administration (Press release). 17 November 2022. Retrieved 18 November 2022. This article incorporates text from this source, which is in the public domain.
- ^ American Diabetes Association Professional Practice Committee (1 January 2022). "2. Classification and Diagnosis of Diabetes: Standards of Medical Care in Diabetes—2022". Diabetes Care. 45 (45): S17 – S38. doi:10.2337/dc22-S002. PMID 34964875. S2CID 245451959. Retrieved 17 November 2022.
- ^ "Tzield (teplizumab-mzwv) approved by FDA as the first and only treatment indicated to delay the onset of Stage 3 type 1 diabetes (T1D) in adult and pediatric patients aged 8 years and older with stage 2 T1D" (Press release).
- ^ a b Kissler S, Gaglia J (8 October 2019). "Anti-CD3 Antibody for the Prevention of Type 1 Diabetes: A Story of Perseverance". Biochemistry. 58 (40): 4107–4111. doi:10.1021/acs.biochem.9b00707. ISSN 1520-4995. PMC 6918689. PMID 31523950.
- ^ Belghith M, Bluestone JA, Barriot S, Mégret J, Bach JF, Chatenoud L (September 2003). "TGF-beta-dependent mechanisms mediate restoration of self-tolerance induced by antibodies to CD3 in overt autoimmune diabetes". Nature Medicine. 9 (9): 1202–1208. doi:10.1038/nm924. PMID 12937416. S2CID 26301557.
- ^ Bisikirska B, Colgan J, Luban J, Bluestone JA, Herold KC (October 2005). "TCR stimulation with modified anti-CD3 mAb expands CD8+ T cell population and induces CD8+CD25+ Tregs". The Journal of Clinical Investigation. 115 (10): 2904–2913. doi:10.1172/JCI23961. PMC 1201661. PMID 16167085.
- ^ "Drug Approval Package: Tzield". accessdata.fda.gov. 5 January 2023. Retrieved 23 January 2023.
- ^ "Advancing Health Through Innovation: New Drug Therapy Approvals 2022". U.S. Food and Drug Administration (FDA). 10 January 2023. Archived from the original on 10 January 2023. Retrieved 22 January 2023. This article incorporates text from this source, which is in the public domain.
- ^ New Drug Therapy Approvals 2022 (PDF). U.S. Food and Drug Administration (FDA) (Report). January 2024. Archived from the original on 14 January 2024. Retrieved 14 January 2024. This article incorporates text from this source, which is in the public domain.