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Tumor Discovery A comprehensive review of bexarotene

hypopituitarism may have the potential for treating antiviral drugs, such as remdesivir. In addition to the
Cushing’s disease . Moreover, combination therapy with FDA-approved drugs, bexarotene has shown encouraging
[41]
bexarotene and lapatinib has shown synergistic inhibition results in a two-tier screening study that included a SARS-
of pituitary adenoma cell growth, leading to a deceleration CoV-2 enzyme-linked immunosorbent assay and cell
of tumor progression . viability assay. In this study, bexarotene demonstrated
[42]
the ability to inhibit in vitro replication of SARS-CoV-2,
5.7. Alopecia areata (AA) with an EC value (the concentration at which the drug
50
AA is a hair loss disorder that leads to spot baldness, exhibits half of the maximum effect) of 2.01 μM. After
2
resulting in unpredictable patchy hair loss. Bexarotene an oral administration of 300 mg/m , the peak serum
has shown tremendous effects in treating AA. In a study concentration (C max ) of bexarotene was found to be 3.39 μM.
conducted on a half-head trial, 1% bexarotene gel was Moreover, the ratio of C max to EC for SARS-CoV-2 with
50
applied to the affected areas twice daily for 6 months, bexarotene was calculated to be 1.69. In addition, the time
leading to noticeable improvements in patients’ hair growth required to achieve C max (T ) with a standard oral dose
max
and condition . Despite not affecting organ systems, AA of bexarotene is 2.5 h, which could be advantageous for
[43]
[49]
can cause significant discomfort for those experiencing COVID patients .
it. Unfortunately, treatment options for AA are limited, Bexarotene has shown notable results as a potential
making it challenging to treat AA. treatment option for COVID-19 in an in silico study using
5.8. Central nervous system (CNS) disorders molecular docking. This anti-neoplastic retinoid has a
high binding affinity toward the angiotensin-converting
Bexarotene has shown promising defensive effects in CNS enzyme-2 (ACE2) receptor, thereby inhibiting the binding
disorders. Traumatic brain injury is sudden brain damage of SARS-CoV-2 with the ACE2 receptor. As a result,
that results in temporary or permanent dysfunction. In the conjugation of bexarotene with the ACE2 receptor
the mice model of traumatic brain injury, bexarotene leads to the inhibition of viral entry into the host cell.
demonstrated the augmentation of spatial memory by Bexarotene forms stable complexes with ACE2 receptors,
suppressing cell apoptosis. This treatment decreased the and these complexes exhibit negative free energy values,
expression of nuclear factor kappa B (NF-κB) (an apoptotic suggesting strong binding affinity. Moreover, bexarotene
protein) and induced oxidative stress through inhibition has demonstrated more potency than other drugs, such as
of microtubule-associated protein, resulting in the high remdesivir, which showed higher values of free energy .
[50]
therapeutic efficacy of bexarotene . Although bexarotene has shown high potential as a
[44]
Bexarotene facilitated erythrophagocytosis, limiting treatment option for COVID-19 in these studies, further
the harmful effects of erythrocyte metabolites. Hence, investigation is necessary to investigate its systemic effects.
bexarotene promoted brain recovery by improving Ex vivo studies, animal models, and clinical trials should be
hematoma clearance and reducing pro-inflammatory conducted to assess the drug’s full potential in combating
responses in mouse models of intracerebral hemorrhage . the disease.
[45]
In cases of subarachnoid hemorrhage, bexarotene 5.10. Ovarian cancer
promotes recovery by minimizing brain infarct damage,
blood–brain barrier leakage, and neurological inadequacy Research demonstrated that bexarotene, at clinical
through the activation of dimerization of PPARγ, which concentrations, can inhibit cell proliferation and induce
is a type of PPAR known for its anti-inflammatory and p21, a well-known factor associated with cell death,
neuroprotective properties . In addition, bexarotene potentially through pyroptosis, in ovarian cancer cell lines.
[46]
improved depression-like behavior in mice by reducing These findings suggest that bexarotene holds promise as an
neuroinflammation and protecting against synaptic anticancer drug for ovarian cancer. However, despite these
damage . These studies indicate that bexarotene holds promising results, the study was unable to fully uncover
[47]
promise as a prospective drug for treating various CNS the specific mechanisms underlying bexarotene-induced
disorders. pyroptosis in ovarian cancer cells. Therefore, further
investigations are needed to gain a deeper understanding
5.9. COVID-19 of how bexarotene induces pyroptosis and to better
[51]
The COVID-19 pandemic has proven to be a global comprehend its pharmacological action .
disturbance, causing millions of deaths worldwide. With
the rapid evolution of the deadly SARS-CoV-2 virus, 6. Conventional formulations of bexarotene
finding a drug that can eliminate this disease remains Bexarotene, also known as LGD1069, has emerged as
an exigent task . There are only few clinically approved a promising antineoplastic agent, particularly for the
[48]

Volume 2 Issue 2 (2023) 6 https://doi.org/10.36922/td.0436