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Repurposing Tranexamic Acid as an Anticancer Agent.

Mary E Law¹, Bradley J Davis¹, Amanda F Ghilardi²

¹Department of Pharmacology and Therapeutics, University of Florida, Gainesville, FL, United States.

Frontiers in Pharmacology

|January 31, 2022

Summary

Tranexamic Acid (TA), an antifibrinolytic, shows anticancer potential by blocking plasmin formation and inhibiting cancer cell viability. It also affects intracellular pathways and amino acid uptake, suggesting new therapeutic strategies.

Keywords:

CDCP1 MYC S6K1 STAT3 acetylation cancer protein synthesis tranexamic acid

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Area of Science:

Biochemistry
Oncology
Pharmacology

Background:

Tranexamic Acid (TA) is an antifibrinolytic agent that inhibits plasminogen activation.
Previous research suggests TA may possess anticancer properties by blocking extracellular plasmin formation.
Plasmin-mediated cleavage of CDCP1 protein is implicated in promoting oncogenic functions.

Purpose of the Study:

To investigate the anticancer effects of Tranexamic Acid (TA).
To explore TA's mechanism of action in cancer, including its effects on CDCP1 and intracellular signaling.
To evaluate TA's potential as a lead compound for novel anticancer agents.

Main Methods:

In vitro studies assessing cancer cell viability.
In vivo breast tumor growth studies.
Analysis of intracellular signaling pathways, protein synthesis, and amino acid uptake.

Main Results:

TA blocks plasmin-mediated cleavage of the oncoprotein CDCP1.
TA reduces the viability of diverse human and murine cancer cell lines in vitro.
TA inhibits breast tumor growth in vivo, suppresses protein synthesis, STAT3/S6K1 phosphorylation, MYC expression, and lysine acetylation, while inhibiting lysine and arginine uptake.

Conclusions:

Tranexamic Acid (TA) demonstrates significant anticancer activity through multiple mechanisms, including inhibition of extracellular plasmin formation and intracellular signaling.
TA's ability to mimic lysine and arginine suggests potential for developing new anticancer agents targeting these amino acid pathways.
TA and its analogs represent promising lead compounds for novel cancer therapies.