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Tumor Discovery

REVIEW ARTICLE
An evidence-based review on bexarotene

Ayushi Mahajan, Lovepreet Singh, Gurjeet Singh, Ravi Kumar Dhawan,
Manjeet Kaur, Pritpal Kaur Malhi, Komal Thakur, and Lakhvir Kaur*
Department of Pharmaceutics, Khalsa College of Pharmacy, Amritsar, Punjab, India

Abstract
Bexarotene is a selective retinoid X receptor agonist of utmost clinical importance.
The United States Food and Drug Administration has approved this drug for its
effects on cutaneous T-cell lymphoma. Bexarotene has shown great potential,
demonstrating enhanced therapeutic activity against a plethora of tumor types, both
as a single agent and as an adjuvant with other targeted agents. Despite its potential,
bexarotene has turned out to be a nostrum, and formulation-related studies that
explore its use have not received much emphasis. Poor aqueous solubility and
low bioavailability are challenges in developing an appropriate formulation of this
drug. In this review, we aim to provide insights into recent research conducted on
formulation development, recent pharmacological findings, patents, and future
research requisites of bexarotene, based on the literature gathered from authentic
web resources and research articles. Bexarotene is a diamond in the rough, as
many researchers have not yet recognized its multipotentiality. The incorporation
of bexarotene into nanoformulations can surmount the current drawbacks and
efficiently enhance its anticancer activity. In conclusion, this drug is a potentially
effective and broad-spectrum anticancer drug for treating malignancies; therefore,
extensive research is required to confirm its potential.

*Corresponding author:
Lakhvir Kaur Keywords: Bexarotene; Cutaneous T-cell lymphoma; Anticancer drug; Retinoid X
(lakhvir86@gmail.com) receptor; Apoptosis
Citation: Mahajan A, Singh L,
Singh G, et al., 2023, An evidence-
based review on bexarotene. Tumor
Discov, 2(2): 0436. 1. Introduction
https://doi.org/10.36922/td.0436
Received: April 13, 2023 Bexarotene is a newly engineered retinoid drug that has exhibited potent activity against
Accepted: July 18, 2023 various myelogenous diseases, particularly cutaneous T-cell lymphoma (CTCL). It was
Published Online: August 3, 2023 approved by the United States Food and Drug Administration (FDA) as a treatment
Copyright: © 2023 Author(s). option for CTCL in 1999. Bexarotene is a retinoid analog with a specific affinity for the
This is an Open Access article retinoid X receptor (RXR) . Retinoids are potent biological modulators employed in the
[1]
distributed under the terms of the
Creative Commons Attribution treatment and management of cancer. They are active biological derivatives of Vitamin
License, permitting distribution, and A, playing a key role in regulating cell differentiation, multiplication, and apoptosis.
reproduction in any medium, which Retinoids function in two forms: RXRs and retinoic acid receptors (RARs) .
[2]
provided that the original work is
properly cited. The RXRs are ligand-activated transcription factors that can form homodimers
Publisher’s Note: AccScience or heterodimers with RARs, thereby modulating cell growth, apoptosis, and
Publishing remains neutral with differentiation . RXRs can act as normal heterodimerization partners and also
[3]
regard to jurisdictional claims in
published maps and institutional function as transcriptional suppressors, competing with other transcription factors for
affiliations. co-activator molecules of other nuclear hormone receptors such as Vitamin D receptor,

Volume 2 Issue 2 (2023) 1 https://doi.org/10.36922/td.0436