| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Human |
| Target | CTLA-4 |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 745013-59-6 |
| ATC code | None |
| UNII | QEN1X95CIX |
| Chemical data | |
| Formula | C65000H9974N1726O2026S52 |
| Mol. mass | 146.4 kDa |
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Tremelimumab (formerly ticilimumab, CP-675,206) is a fully human IgG2 monoclonal antibody produced by Pfizer. It binds to the protein CTLA-4, which is expressed on the surface of activated T lymphocytes. Tremelimumab blocks the binding of the antigen-presenting cell ligands B7.1 and B7.2 to CTLA-4, resulting in inhibition of B7-CTLA-4-mediated downregulation of T-cell activation; subsequently, B7.1 or B7.2 may interact with another T-cell surface receptor protein, CD28, resulting in a B7-CD28-mediated T-cell activation unopposed by B7-CTLA-4-mediated inhibition.
Tremelimumab is thought to stimulate patients’ immune systems to attack their tumors. It has been shown to induce durable tumor responses in patients with metastatic melanoma in Phase 1 and Phase 2 clinical studies.[1]
On April 2, 2008, Pfizer announced that it has discontinued a Phase III clinical trial for patients with advanced melanoma after the review of interim data showed that the trial would not demonstrate superiority to standard chemotherapy.[2] Studies for other tumors are planned as of October 2009[update], namely for prostate cancer[3] and bladder cancer.[4]
On October 4, 2011, MedImmune LLC gained worldwide rights on Tremelimumab to develop and commercialize the drug for treatment of cancer, while Pfizer retains all rights for combination therapies.
As of October 2009[update], there are two fully human anti CTLA-4 monoclonal antibodies in advanced clinical trials, tremelimumab and ipilimumab (from Medarex and Bristol-Myers Squibb).[5]
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