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Anne-Marie Ellegaard¹, Christian Dehlendorff², Anna C Vind³

¹Cell Death & Metabolism, Center for Autophagy, Recycling and Disease, Danish Cancer Society Research Center, DK-2100 Copenhagen, Denmark.

|June 23, 2016

Abstract:

Non-small cell lung cancer (NSCLC) is one of the deadliest cancers worldwide. In search for new NSCLC treatment options, we screened a cationic amphiphilic drug (CAD) library for cytotoxicity against NSCLC cells and identified several CAD antihistamines as inducers of lysosomal cell death. We then performed a cohort study on the effect of CAD antihistamine use on mortality of patients diagnosed with non-localized cancer in Denmark between 1995 and 2011. The use of the most commonly prescribed CAD antihistamine, loratadine, was associated with significantly reduced all-cause mortality among patients with non-localized NSCLC or any non-localized cancer when compared with use of non-CAD antihistamines and adjusted for potential confounders. Of the less frequently described CAD antihistamines, astemizole showed a similar significant association with reduced mortality as loratadine among patients with any non-localized cancer, and ebastine use showed a similar tendency. The association between CAD antihistamine use and reduced mortality was stronger among patients with records of concurrent chemotherapy than among those without such records. In line with this, sub-micromolar concentrations of loratadine, astemizole and ebastine sensitized NSCLC cells to chemotherapy and reverted multidrug resistance in NSCLC, breast and prostate cancer cells. Thus, CAD antihistamines may improve the efficacy of cancer chemotherapy.

Insights

Cationic amphiphilic antihistamines, like loratadine, show potential in reducing mortality for non-small cell lung cancer (NSCLC) patients. These drugs may also enhance chemotherapy effectiveness, offering new treatment avenues.

Area of Science:

Oncology
Pharmacology
Cancer Research

Background:

Non-small cell lung cancer (NSCLC) presents a significant global health challenge with limited treatment options.
Cationic amphiphilic drugs (CADs) are being investigated for novel therapeutic applications.
Antihistamines belonging to the CAD class have demonstrated cytotoxic effects on NSCLC cells.

Purpose of the Study:

To investigate the potential of CAD antihistamines in improving survival rates for cancer patients.
To explore the association between the use of specific CAD antihistamines and all-cause mortality in non-localized cancer patients.
To determine if CAD antihistamines can enhance the efficacy of chemotherapy in various cancer types.

Main Methods:

Screening of a cationic amphiphilic drug library for cytotoxicity against NSCLC cells.
A retrospective cohort study analyzing mortality data of Danish cancer patients (1995-2011).
In vitro experiments assessing the sensitization of cancer cells to chemotherapy and reversal of multidrug resistance.

Main Results:

Loratadine, a common CAD antihistamine, was significantly associated with reduced all-cause mortality in patients with non-localized NSCLC and other non-localized cancers.
Other CAD antihistamines, astemizole and ebastine, showed similar trends in reducing mortality.
CAD antihistamine use demonstrated a stronger association with reduced mortality in patients receiving concurrent chemotherapy.
In vitro, loratadine, astemizole, and ebastine sensitized NSCLC, breast, and prostate cancer cells to chemotherapy and overcame multidrug resistance.

Conclusions:

CAD antihistamines, particularly loratadine, are associated with improved survival outcomes in non-localized cancer patients.
These drugs show promise in enhancing the effectiveness of conventional cancer chemotherapy.
CAD antihistamines represent a potential therapeutic strategy to improve cancer treatment efficacy and patient survival.

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