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Anticancer Effects of Amlodipine Alone or in Combination With Gefitinib in Non-Small Cell Lung Cancer

Bingjie Fu1, Xiaojing Dou1, Miao Zou1

  • 1Tianjin Key Laboratory of Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Key Laboratory of Immune Microenvironment and Diseases (Ministry of Education), Tianjin Medical University, Tianjin, China.

Frontiers in Pharmacology
|June 20, 2022
PubMed

Insights

Amlodipine, a calcium channel blocker, shows anticancer effects in lung cancer by inhibiting cell proliferation and arresting the cell cycle. It may be a potential therapy for non-small cell lung cancer (NSCLC), especially when combined with gefitinib.

Area of Science:

  • Pharmacology
  • Oncology
  • Molecular Biology

Background:

  • Amlodipine is a widely used calcium channel blocker for cardiovascular conditions.
  • Its potential anticancer effects, particularly in lung cancer, have not been fully elucidated.
  • Non-small cell lung cancer (NSCLC) remains a significant health concern globally.

Purpose of the Study:

  • To investigate the antitumor effects of amlodipine in A549 lung cancer cells.
  • To explore the underlying molecular mechanisms of amlodipine's action.
  • To evaluate the synergistic effect of amlodipine combined with gefitinib in NSCLC.

Main Methods:

  • In vitro studies using A549 lung cancer cells.
  • In vivo studies with A549 lung cancer xenografts.
  • Analysis of cell cycle regulation and key signaling pathways (PI3K/Akt, Raf/MEK/ERK).

Main Results:

  • Amlodipine suppressed A549 cell proliferation by inducing cell cycle arrest.
  • Amlodipine modulated cell cycle proteins (cyclin D1, p-Rb, p27, p21) and attenuated PI3K/Akt and Raf/MEK/ERK pathways via EGFR.
  • Combination therapy with amlodipine and gefitinib demonstrated synergistic inhibition of proliferation and tumor growth.

Conclusions:

  • Amlodipine exhibits significant antitumor activity in NSCLC models.
  • The combination of amlodipine and gefitinib shows enhanced therapeutic efficacy.
  • Amlodipine, alone or with gefitinib, represents a potential therapeutic strategy for NSCLC patients with wild-type EGFR.
Keywords:
amlodipinecell cycle arrestgefitiniblung cancersynergistic anticancer effect

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