Drug intelligence / Profile preview

bintrafusp alfa + carboplatin + gemcitabine

Development stage
Discontinued
Lead developer
Merck
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

Bintrafusp alfa + carboplatin + gemcitabine is a combination regimen composed of three agents: - **Bintrafusp alfa** is a first-in-class bifunctional fusion protein, consisting of the extracellular domain of human transforming growth factor beta (TGF-β) receptor II fused to the C-terminus of each heavy chain of a human IgG1 monoclonal antibody targeting programmed death-ligand 1 (PD-L1). It acts as both a PD-L1 checkpoint inhibitor and a TGF-β "trap", targeting two key immunosuppressive mechanisms in the tumor microenvironment. Bintrafusp alfa is under investigation primarily for cancers with poor prognosis, including HPV-associated malignancies, biliary tract cancers, and non-small cell lung cancer[1][2][3]. - **Carboplatin** is a platinum-based cytotoxic chemotherapeutic agent that induces DNA crosslinking and apoptosis. - **Gemcitabine** is a nucleoside analog, acting as an antimetabolite that inhibits DNA synthesis and induces cell death. The combination seeks to exploit potential synergistic antitumor effects by combining checkpoint inhibition, TGF-β sequestration, and DNA-damaging cytotoxic chemotherapy[1].

02

Targets

RNR (Ribonucleotide reductase)CD274 (Programmed cell death protein 1 ligand 1)TGFB (GARP–latent transforming growth factor beta 1 complex)DNA

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