# Bazedoxifene Inhibits Cell Viability, Colony‐Forming Activity, and Cell Migration in Human Non–Small Cell Lung Cancer Cells and Improves the Treatment Efficacy of Paclitaxel and Gemcitabine

**Authors:** Yaochen Huang, Jiayuh Lin, Xiangning Fu, Lequn Li, Shenging Fu

PMC · DOI: 10.1111/crj.13822 · The Clinical Respiratory Journal · 2024-08-17

## TL;DR

Bazedoxifene, an FDA-approved drug, shows antitumor effects in lung cancer cells and enhances the effectiveness of existing cancer drugs.

## Contribution

Demonstrates bazedoxifene's antitumor activity and synergy with paclitaxel and gemcitabine in non–small cell lung cancer.

## Key findings

- Bazedoxifene inhibits cell viability, colony formation, and migration in a dose-dependent manner.
- Bazedoxifene synergizes with paclitaxel and gemcitabine to enhance antitumor effects.
- The drug shows potential as an adjunct therapy for non–small cell lung cancer.

## Abstract

Bazedoxifene is a third‐generation selective estrogen receptor modulator that inhibits the IL6/IL6R/GP130 signaling pathway by inhibiting IL6‐induced homodimerization of GP130. Considering that the IL6/IL6R/GP130 signaling pathway is important in tumorigenesis and metastasis, bazedoxifene is thought to have an antitumor effect, which has been proven preliminarily in breast cancer and pancreatic cancer but has not yet been studied in non–small cell lung cancer (NSCLC). This study is aimed at evaluating the antitumor effect of bazedoxifene in NSCLC.

A549 and H1299 NSCLC cell lines were employed and exposed to various concentrations of bazedoxifene, paclitaxel, gemcitabine, and their combinations for cell viability, colony formation, and wound healing assays to demonstrate the antitumor effect of bazedoxifene with or without paclitaxel or gemcitabine.

MTT cell viability, colony formation, and wound healing assays showed that bazedoxifene was capable of inhibiting cell viability, colony formation, and cell migration in a dose‐dependent manner. In addition, bazedoxifene was capable of working with paclitaxel or gemcitabine synergistically to inhibit cell viability, colony formation, and cell migration.

This study demonstrated the potential antitumor effect of bazedoxifene and its ability to improve the treatment efficacy of paclitaxel and gemcitabine.

Our study showed that bazedoxifene, an FDA‐approved drug, was capable of inhibiting cell viability, colony formation, and cell migration in a dose‐dependent manner and was capable of working with paclitaxel or gemcitabine synergistically. These results demonstrated the potential antitumor effect of bazedoxifene.

## Linked entities

- **Proteins:** IL6 (interleukin 6), IL6R (interleukin 6 receptor), IL6ST (interleukin 6 cytokine family signal transducer)
- **Chemicals:** bazedoxifene (PubChem CID 154257), paclitaxel (PubChem CID 36314), gemcitabine (PubChem CID 60750)
- **Diseases:** non–small cell lung cancer (MONDO:0005233), breast cancer (MONDO:0004989), pancreatic cancer (MONDO:0005192)

## Full-text entities

- **Genes:** IL6R (interleukin 6 receptor) [NCBI Gene 3570] {aka CD126, HIES5, IL-1Ra, IL-6R, IL-6R-1, IL-6RA}, IL6ST (interleukin 6 cytokine family signal transducer) [NCBI Gene 3572] {aka CD130, CDW130, GP130, HIES4, HIES4A, HIES4B}, ESR1 (estrogen receptor 1) [NCBI Gene 2099] {aka ER, ESR, ESRA, ESTRR, Era, NR3A1}, IL6 (interleukin 6) [NCBI Gene 3569] {aka BSF-2, BSF2, CDF, HGF, HSF, IFN-beta-2}
- **Diseases:** metastasis (MESH:D009362), tumorigenesis (MESH:D063646), pancreatic cancer (MESH:D010190), NSCLC (MESH:D002289), breast cancer (MESH:D001943)
- **Species:** Homo sapiens (human, species) [taxon 9606]
- **Cell lines:** H1299 — Homo sapiens (Human), Lung large cell carcinoma, Cancer cell line (CVCL_0060), A549 — Homo sapiens (Human), Lung adenocarcinoma, Cancer cell line (CVCL_0023)

## Full text

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## Figures

5 figures with captions in the complete paper: https://tomesphere.com/paper/PMC11329873/full.md

## References

29 references — full list in the complete paper: https://tomesphere.com/paper/PMC11329873/full.md

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Source: https://tomesphere.com/paper/PMC11329873