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Tumor Discovery A comprehensive review of bexarotene

Table 3. The details of various patents on bexarotene
No. Title Application no. Outcome References
1. Bexarotene gel and its preparation method CN100434068C The prepared gel effectively minimized the systemic toxic [67]
effects compared to oral administration of bexarotene by
decreasing the C from 7.56 μg/ml to 0.598 μg/ml.
max
2. Bexarotene soft capsules and preparation CN103181912A The prepared soft capsules depicted better bioavailability, [68]
method thereof safety, and efficacy in contrast to the oral tablets.
3. Topical pharmaceutical compositions EP2612665A1 The prepared topical formulation demonstrated better efficacy [69]
comprising bexarotene and a corticosteroid than the other standard products like Daivobet ointment or
the tazarotene-betamethasone ointment, as the AUC was
reduced to 94.9%.
4. A kind of bexarotene nanosuspension CN104922062A The prepared nanosuspension had a diameter ranging [70]
between 100 and 1000 nm that proficiently reinforced the
drug's solubility and dissolution rate. The drug blood level of
bexarotene was increased to 500 ng/ml from 300 ng/ml, which
enhanced the bioavailability of the drug.
5. Bexarotene soft gel capsule and preparation US20190038566A1 The soft gel bexarotene capsules nullified drug degradation [71]
method thereof and enhanced dose uniformity.
6. Bexarotene and ligustrazine eutectic CN111718257A The eutectic mixture demonstrated better aqueous solubility [72]
compound, preparation method, and dissolution as the dissolution rate was increased by 40%.
composition, and application thereof The concentration of the drug in the blood was enhanced
with C max approximately equal to 1900 μg/L thereby, enhanced
bioavailability.
7. Synthesis of antitumor medicine bexarotene CN1205166C An eco-friendly method for the synthesis of bexarotene [73]
suitable for industrial production.
8. Process for the preparation of highly pure WO2011141928A1 A highly pure form of bexarotene was obtained with [74]
bexarotene identified impurities of<0.15% and unidentified impurities
of<0.10%.
9. Bexarotene analogs US9174917B2 The invented analogs had a lower toxicity profile, increased [75]
apoptosis by 4.3 folds, and decreased tumorigenesis by 3.5
folds compared to the already available analogs.

combined with bexarotene to form a mixed liquid drug. psoriasis, Kaposi’s sarcoma, lung cancer, and Cushing’s
Furthermore, the invention emphasizes ensuring dosage disease .
[72]
uniformity during the capsule-filling process .
[71]
9.2. Patents related to a modification in the
9.1.6. Bexarotene and ligustrazine eutectic chemistry of bexarotene
compound, preparation method, composition, and 9.2.1. Synthesis of antitumor medicine bexarotene
application thereof (2019) (2001)
Assigned to: “Institute of Materia Medica, Chinese Academy Assigned to: “Shanghai Institute of Materia Medica, Chinese
of Medical Sciences” CN111718257A Academy of Sciences, Shanghai Huatuo Pharmaceutical
The patent discloses the method of preparation, Technology Development Co., Ltd.” CN1205166C
application, and composition of bexarotene and ligustrazine The patent presents an eco-friendly process for the
eutectic crystals. Bexarotene is used as the medicinal agent, preparation of synthetic bexarotene. Bexarotene is
while ligustrazine acts as a eutectic precursor, used in the chemically known as 4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-
molar ratio of 2:1. The eutectic mixture demonstrated tetrahydrochysene-2-naphthyl)vinyl) phenylformic acid.
enhanced solubility and bioavailability compared to The method involves using diethyl ether, which induces a
bexarotene alone. The resulting formulation is preferably nucleophilic addition reaction at the ketone carbonyl group
a unit dosage form and can be administered orally, of 1-(3,5) of phenylformic acid. The patent declares to avert
parenterally, through the eyes, vagina, rectum, skin, etc. environmental pollution and other drawbacks such as
These eutectic compounds offer treatment potential for difficult operations, by avoiding the use of uneconomical
various ailments, such as glioma, CTCL, breast cancer, atoms, such as phosphorous compounds .
[73]

Volume 2 Issue 2 (2023) 11 https://doi.org/10.36922/td.0436