Drug intelligence / Profile preview

Carboplatin + Gemcitabine + Zileuton

Development stage
Unknown
Lead developer
Johnson Matthey
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

The combination of carboplatin, gemcitabine, and zileuton appears to be an investigational treatment regimen that has been studied for advanced non-small cell lung cancer (NSCLC). This combination was evaluated in clinical trials, specifically in a completed Phase 2 trial[1][3]. ## Drug Information Carboplatin and gemcitabine form a chemotherapy combination known as GemCarbo, which is used to treat various cancer types[4]. Zileuton is an FDA-approved 5-lipoxygenase inhibitor primarily used for asthma treatment[7][10]. When combined, these three medications appear to have been investigated for potential synergistic effects in cancer treatment. The clinical trial mentioned in the search results combined carboplatin/gemcitabine with zileuton, celecoxib, or both zileuton and celecoxib for treating advanced non-small cell lung cancer[5]. ## Mechanism of Action Each component of this combination has a distinct mechanism: - **Carboplatin**: A platinum-based chemotherapy drug that destroys quickly dividing cells, such as cancer cells[4]. - **Gemcitabine**: A chemotherapy drug that has demonstrated single-agent activity in advanced non-small cell lung cancer, with response rates of ≥20%[2]. - **Zileuton**: A 5-lipoxygenase inhibitor that suppresses leukotriene production. It inhibits leukotriene LTB4, LTC4, LTD4, and LTE4 formation[10]. While primarily used for asthma, research suggests it may have anti-cancer properties by reducing inflammation associated with cancer development[5]. ## Administration The GemCarbo (gemcitabine and carboplatin) portion is typically administered as follows: - Gemcitabine as a drip into the bloodstream over 30 minutes on days 1 and 8 - Carboplatin as a drip into the bloodstream over 30 to 60 minutes on day 1 - Treatment cycles typically last 21 days (3 weeks)[4] ## Clinical Trials A Phase 2 clinical trial investigated carboplatin and gemcitabine combined with zileuton, celecoxib, or both zileuton and celecoxib in treating patients with advanced non-small cell lung cancer. However, according to the limited information available, the study failed to demonstrate significant benefits from the addition of zileuton[5]. ## Side Effects and Interactions The combination may present various side effects: - **Carboplatin and gemcitabine**: Common side effects include thrombocytopenia, neutropenia, and anemia. When administered together, there may be increased severity of thrombocytopenia, particularly if carboplatin is given immediately after gemcitabine[8][9]. - **Zileuton**: Side effects may include upset stomach, diarrhea, nausea, muscle aches, headache, and in rare cases, liver problems[7]. This combination represents an investigational approach to cancer treatment that combines traditional chemotherapy agents with an anti-inflammatory medication to potentially enhance efficacy through multiple mechanisms.

02

Targets

ALOX12 (Arachidonate 12-lipoxygenase, 12S type)DNA

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