Drug intelligence / Profile preview

ipilimumab + nivolumab + temozolomide

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of two immune checkpoint inhibitors, ipilimumab and nivolumab, plus the alkylating agent temozolomide. Ipilimumab is a monoclonal antibody that blocks cytotoxic T-lymphocyte-associated protein 4 (CTLA-4), enhancing T-cell activation and proliferation. Nivolumab is a monoclonal antibody that inhibits programmed cell death protein 1 (PD-1), preventing tumor cells from evading immune detection. Temozolomide is an oral alkylating chemotherapy agent that induces DNA damage in tumor cells, leading to cell death. This combination has been investigated primarily for the treatment of glioblastoma, gliosarcoma, and metastatic colorectal cancer with specific molecular features such as MGMT promoter methylation or microsatellite stability[1][2][6]. The rationale for combining these agents lies in their complementary mechanisms—temozolomide may increase tumor immunogenicity while dual checkpoint blockade further enhances anti-tumor immune responses.

02

Targets

DNACTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)PDCD1 (Programmed cell death protein 1 receptor)

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