tremelimumab   Click here for help

GtoPdb Ligand ID: 8462

Synonyms: CP-675 | CP-675,206 | CP-675206 | Imjudo® | ticilimumab | tremelimumab-actl
Approved drug Immunopharmacology Ligand
tremelimumab is an approved drug (FDA (2022), EMA (2023))
Compound class: Antibody
Comment: Tremelimumab is a fully human investigational monoclonal antibody targeting cytotoxic T-lymphocyte-associated protein 4 (CTLA4, CD152). Tremelimumab was designed as an antineoplastic agent. A BLAST sequence alignment matches tremelimumab to patent US 6682736, and identifies antibody clone 11.2.1 [2].
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
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Summary of Clinical Use Click here for help
Tremelimumab has undergone clinical evaluations in patients with malignant mesothelioma [1] and uveal melanoma [3]. The FDA issued orphan drug (OD) status for the treatment of stage IIb-IV metastatic melanoma in 2006, and in 2015 OD status was granted for the treatment of malignant mesothelioma, a disease that's most commonly caused by exposure to asbestos. EMA OD designation as a treatment for hepatocellular carcinoma (HCC) was issued in December 2020. A combination regimen of tremelimumab + durvalumab (Imfinzi®) that is indicated for unresectable HCC was fully approved by the FDA in October 2022.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Tremelimumab stimulates the immune system to destroy cancer cells [4]. Downregulation of T-cell activation is achieved by the antibody blocking the interaction between CTLA4 on T cells and the B7 proteins (CD80 and CD86) on antigen presenting cells. This leaves the unbound B7 proteins free to bind CD28, another T cell surface receptor. The result is a B7-CD28-mediated T-cell activation unopposed by B7-CTLA4-mediated inhibition.