Research Progress on the Antitumor Mechanism of Penfluridol

Abstract

Background:
Penfluridol is a long-acting oral antipsychotic drug originally used to treat schizophrenia and other severe mental illnesses. Due to its favorable pharmacokinetic profile and ability to penetrate the blood-brain barrier, recent studies have evaluated its potential in oncology, particularly its anti-tumor properties.

Objective:
To explore the pharmacological basis, molecular mechanisms, and therapeutic implications of repurposing penfluridol as an anti-cancer agent across various tumor types.

Methods:
This review synthesizes data from preclinical studies that investigated the anti-tumor activity of penfluridol. The mechanisms discussed include pharmacology, toxicology, resistance development, and synergy with other therapeutic agents. Particular attention is given to its impact on tumor metabolism, immune modulation, cell cycle arrest, apoptosis induction, and its efficacy across cancer models such as glioblastoma, breast, lung, pancreatic, colon, bladder cancers, leukemia, and inflammatory autoimmune diseases.

Results:
Penfluridol exerts broad anti-tumor effects via multiple mechanisms including:

• Inducing cell cycle arrest and apoptosis

• Inhibiting angiogenesis and tumor metastasis

• Modulating immune responses in the tumor microenvironment

• Disrupting glycolysis and cholesterol homeostasis

• Enhancing efficacy when combined with chemotherapy, immune checkpoint inhibitors, and targeted drugs.
  In vitro and in vivo studies confirm its efficacy in reducing tumor growth and improving survival in animal models.

Conclusion:
Penfluridol demonstrates promising potential as a repurposed anti-cancer agent. Its multifaceted molecular targets make it a strong candidate for integrated cancer therapy. Further clinical trials and pharmacokinetic optimizations are essential to validate its therapeutic value and translate preclinical findings into clinical applications.