Drug intelligence / Profile preview

tamibarotene + gemcitabine + cisplatin + nivolumab

Development stage
Phase 2
Lead developer
Syros Pharmaceuticals
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral (tamibarotene), Intravenous (gemcitabine, Cisplatin, Nivolumab)
01

Overview

A four-drug combination regimen consisting of **tamibarotene**, **gemcitabine**, **cisplatin**, and **nivolumab**. - **Tamibarotene** is an oral, selective retinoic acid receptor alpha (RARα) agonist, developed primarily for cancers characterized by RARA overexpression. It promotes differentiation of malignant cells[1][3][7]. - **Gemcitabine** is a nucleoside analog (antimetabolite) chemotherapy that inhibits DNA synthesis, leading to cell death. - **Cisplatin** is a platinum-based chemotherapy that forms DNA crosslinks, disrupting DNA function and triggering apoptosis. - **Nivolumab** is a monoclonal antibody targeting the programmed death-1 (PD-1) receptor, blocking its interaction with PD-L1 and PD-L2, thereby enhancing T-cell-mediated anti-tumor immune responses[2][6][8]. This combination brings together **differentiation therapy** (tamibarotene), **cytotoxic chemotherapy** (gemcitabine, cisplatin), and **immune checkpoint inhibition** (nivolumab) for a potential synergistic anti-tumor effect. Current clinical evidence for this specific four-drug regimen is limited, and it may be under investigation in early-phase clinical trials for certain cancers.

Other names
AM80 + gemcitabine + cisplatin + nivolumabMIKE-1 + gemcitabine + cisplatin + nivolumabGRAPE regimen
02

Targets

DNAPDCD1 (Programmed cell death protein 1 receptor)RARA (Retinoic acid receptor alpha)

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