Drug intelligence / Profile preview

BMS-986158 + nivolumab

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

Overview

**BMS-986158 + nivolumab** is a **combination therapy** investigated in clinical trials for advanced solid tumors and hematologic malignancies[1][2][5][7]. BMS-986158 is a small molecule inhibitor of the bromodomain and extra-terminal (BET) proteins (especially BRD2, BRD3, BRD4), acting as an epigenetic modulator that disrupts transcription of cancer-promoting genes such as MYC[3][9]. Nivolumab is a monoclonal antibody targeting the programmed death-1 (PD-1) receptor, functioning as a checkpoint inhibitor to enhance anti-tumor immune response[1][6]. The rationale for the combination is to pair BET inhibition’s anti-proliferative and transcriptional regulatory effects with nivolumab’s immunotherapy, potentially improving outcomes in cancers resistant to monotherapy[1][5].

Brand names
Opdivo
Other names
BET inhibitor + nivolumabBMS-986158 + Opdivo
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)BRD4 (Bromodomain-containing protein 4)BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)

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