Drug intelligence / Profile preview

carboplatin + exisulind + gemcitabine

Development stage
Phase 2
Lead developer
Astellas Pharma
Modality
Targeted Protein Degraders (TPDs) → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Prodrugs/Conditional Activator Small Molecules → Small Molecules, Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Intravenous (carboplatin, Gemcitabine), Oral (exisulind)
01

Overview

This is a combination regimen consisting of three agents: - **Carboplatin** is a platinum-based chemotherapeutic that forms DNA crosslinks, leading to apoptosis in rapidly dividing cells. - **Gemcitabine** is a nucleoside analog (antimetabolite) that inhibits DNA synthesis, resulting in cell death. - **Exisulind** (also known as Aptosyn) is an oral proapoptotic agent and sulfone derivative of sulindac. It acts primarily by inhibiting cyclic guanosine monophosphate phosphodiesterase (cGMP-PDE), leading to increased cGMP levels and activation of protein kinase G, which induces apoptosis selectively in precancerous and cancerous cells with minimal effects on normal tissue. This combination has been investigated primarily for advanced non-small cell lung cancer (NSCLC). Clinical trials have shown the regimen to be generally well tolerated, with hematologic toxicity being most common. The addition of exisulind was intended to enhance proapoptotic effects beyond standard chemotherapy[1][7][9].

02

Targets

DNAPDE5 (Phosphodiesterase 5A)RRM1

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