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.
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