Drug Database
BE

bexarotene (Targretin Gel)

✓ Approved

Eisai Co., Ltd. · RXRA · Small Molecule

What is bexarotene?

bexarotene is a small molecule developed by Eisai Co., Ltd.. It is approved for therapeutic indications via topical.

Drug Profile

Brand NamesTargretin Gel
CompanyEisai Co., Ltd.
Drug ClassSmall Molecule
Molecular TargetRXRA, RXRB, RXRG
RouteTopical
StatusApproved
Sources: ClinicalTrials.gov, Eisai Co., Ltd.

Mechanism of Action

Molecular Targets

bexarotene acts on 3 molecular targets:

RXRAretinoid X receptor alpha (RXR-alpha, RXRalpha)
RXRBretinoid X receptor beta (DAUDI6, H-2RIIBP)
RXRGretinoid X receptor gamma (RXR-gamma, RXRC)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

bexarotene is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Cutaneous T-cell lymphoma✓ Approved

Related Research Articles

PubMedBioconjugate chemistry2026-10-22

Co-delivery of siPD-L1 and Tat-HSPB1 by G5PBA Enhances the Efficacy of Antitumor Therapy in Clear Cell Renal Cell Carcinoma.

Xiong Kui K, Xia Lili L, Zhang Lin L, Li Weiyuan W et al.

Clear cell renal cell carcinoma (ccRCC) is the most common subtype of renal cell carcinoma and remains challenging to treat at advanced stages due to immune evasion and inefficient intracellular delivery of therapeutic agents. In this study, we synthesized a modified generation 5 (G5) poly(amidoamine) dendrimer (G5PBA) to co-deliver small-interfering RNA targeting programmed death-ligand 1 (siPD-L1) and the antitumor peptide Tat-HSPB1, forming the G5PBA/siPD-L1/Tat-HSPB1 nanocomplex. The agarose gel retardation assay demonstrated that G5PBA efficiently condensed siPD-L1. Furthermore, the peptide encapsulation efficiency and loading capacity were measured, confirming the loading of Tat-HSPB1 into G5PBA/siPD-L1. Flow cytometry showed that G5PBA enhanced the cellular uptake of siPD-L1, while confocal microscopy demonstrated that G5PBA promoted lysosomal escape in Caki-1 cells. Western blot analysis further confirmed that G5PBA effectively reduced the PD-L1 protein expression. In cellular experiments, CCK-8, EdU, and wound-healing assays demonstrated that G5PBA/siPD-L1/Tat-HSPB1 inhibited the viability and migration of ccRCC cells. G5PBA/siPD-L1/Tat-HSPB1 suppressed tumor growth, downregulated PD-L1 expression, enhanced CD4+ and CD8+ T-cell infiltration, and elevated serum levels of IL-2, IL-6, TNF-α, and IFN-γ in mice. Major organs exhibited no obvious histopathological abnormalities upon H&E staining. Serum ALT, AST, and BUN levels showed no significant changes compared with the PBS group, suggesting the preliminary safety profile of G5PBA/siPD-L1/Tat-HSPB1. Collectively, the nanocomplex achieved efficient peptide/siPD-L1 co-delivery and demonstrated significant antitumor activity. This system thus provides a promising strategy and experimental basis for local administration of ccRCC.

PMID 42902944
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PubMedMaterials horizons2026-10-22

Controlled exposure of Ti-O-related sites in a dual-ligand Ti-based MOF heterostructure via alkaline etching for ultrafast Cs+ and Sr2+ capture.

Tang Haixiang H, Bai Xiuyi X, Xue Bingxin B, Wang Xinpeng X et al.

Since various radionuclides, such as Cs+ and Sr2+, typically coexist in real-world radioactive-contaminated wastewater, the comprehensive, highly efficient, and highly selective separation of these radionuclides from complex water bodies remains a major challenge in environmental radioactive remediation. Herein, a dual-ligand Ti-based MOF heterostructure was constructed and subsequently regulated through controlled ammonia-based alkaline etching. Through a novel ammonia-based alkaline etching method, active Ti-O-related sites were effectively exposed within the MOF structure, endowing COMIL-2 with excellent adsorption performance. Benefiting from the synergistic effect between the in situ exposed active Ti-O-related sites and the intrinsic three-dimensional porous framework of the MOF, COMIL-2 exhibited ultrafast adsorption kinetics (with adsorption capacities approaching plateau values within approximately 15 s for Cs+ and 20 s for Sr2+) and high experimental adsorption capacities (252.45 mg g-1 and 92.20 mg g-1, respectively). Even in the presence of competing ions such as Na+, K+, and Mg2+, as well as in Cs+/Sr2+-spiked environmental water samples such as North Sea groundwater, COMIL-2 retained appreciable adsorption performance. Density functional theory calculations further indicate that interfacial electronic reconstruction and the resulting local polarization contribute to the favorable interaction of Cs+ and Sr2+ with the accessible Ti-O-related regions. This structural evolution induces spatial charge separation and the migration of surface electrostatic potential, enabling the electron-rich microenvironment to stably anchor the target cations via nucleophilic interactions. This study provides valuable insights for the rational design and fabrication of novel MOFs with multiple specific adsorption sites at the atomic scale.

PMID 42902758
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PubMedBioconjugate chemistry2026-10-22

Systematic Evaluation of Washing Conditions to Preserve Low Affinity Binders in DEL Selections.

Fabbri Mosè M, Campari Lorenzo L, Puglioli Sara S, Alvigini Laura L et al.

DNA-encoded chemical libraries (DELs) accelerate ligand discovery by combining combinatorial synthesis with parallel affinity selection of DNA-tagged compounds. Conventional DEL selection protocols involve the immobilization of protein targets on a solid support such as magnetic beads. Several washes are performed on the beads after library incubation to remove non-binder library members and to enrich for binding compounds. However, excessive washing could also deplete weak or rapidly dissociating binders. Here, we systematically study the impact of the number of washing steps on DEL hit enrichment during screening of a newly synthesized library named THPP-DEL and based on a central 2-amino-3-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)propanoic acid scaffold and containing ∼8 million compounds. THPP-DEL was screened against Carbonic Anhydrase IX (CAIX), Prostate-Specific Membrane Antigen (PSMA), and Human Serum Albumin (HSA) by systematically varying the number of washing steps from 0 to 20. High-throughput sequencing revealed enriched chemotypes against the three targets, with affinities ranging from low nanomolar to low micromolar concentration values. For all hits, total counts and enrichment factors depended on washing conditions and stabilized after three washing steps. The results presented in this paper define practical selection conditions that preserve micromolar binders, control background levels, and reduce unnecessary hit resynthesis of false positives.

PMID 42902950
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PubMedDrug testing and analysis2026-10-22

Doping Control Analysis of Darbepoetin Alfa Biosimilars in Human Urine, Serum, Plasma, and Dried Blood Spots.

Akiyama Kentaro K, Sakurai Hikaru H, Sato Mitsuhiko M, Momobayashi Atsushi A et al.

Following the patent expiration of the originator darbepoetin alfa, three biosimilar products have been marketed in Japan; however, their detectability by current anti-doping methods has not yet been verified. The present study assessed whether these biosimilars can be detected in human urine, serum, plasma, and dried blood spots (DBS) using the established initial testing procedure and confirmation analysis for erythropoietin-receptor agonists. The originator product and three biosimilars (5 μg, i.v.) were administered to healthy male volunteers. Samples collected up to 72 h postdose were subjected to immunopurification followed by sodium N-lauroyl sarcosinate polyacrylamide-gel electrophoresis (SAR-PAGE) as the initial testing procedure. Confirmation was performed by SAR-PAGE with double blotting for serum and plasma. DBS and urine samples were confirmed by SAR-PAGE using an alternative antibody, and urine samples were further examined by liquid chromatography-tandem mass spectrometry (LC-MS/MS). SAR-PAGE analysis of the pharmaceutical preparations revealed product-specific electrophoretic profiles: two biosimilars migrated slightly above one originator product as diffused smears, whereas the third produced a sharp band comparable to that of another originator product. Similar profiles were observed in postdose samples from all biological matrices, and all biosimilars remained detectable in urine, serum, plasma, and DBS for at least 72 h. Although some biosimilars showed distinct SAR-PAGE banding patterns, product attribution remained limited. LC-MS/MS confirmed administered darbepoetin alfa in the 24 h urine samples but did not detect analyte in lower concentration samples, indicating that its performance was concentration-dependent. Accordingly, SAR-PAGE should incorporate reference standards beyond the originator product, particularly those with different band morphologies.

PMID 42902912
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PubMedMacromolecular rapid communications2026-10-21

Anion-Regulated Phase Separation Constructs Mechanically Tunable Ion Gels for Strain Sensing.

Gao Jie J, Guo Song S, Ji Zhe Z, Cao Mo M et al.

Although ion gels are promising for flexible sensing, simultaneously achieving high mechanical strength, stretchability, ionic conductivity, and interfacial adhesion remains challenging. Here, we report the preparation of ion gels with tunable mechanical properties using two ionic liquids (ILs) with different compatibilities with poly(acrylic acid) (PAA) via a one-pot ultraviolet (UV)-initiated polymerization. Adjusting the mixing ratio of the two ILs can regulate the phase separation of the gel and promote the formation of a bicontinuous phase. The optimized ion gel exhibits a tensile strength of 11 MPa, high elongation at break (363%), excellent ionic conductivity (1.4 × 10- 2 mS cm- 1), and robust interfacial adhesion. Ion gel-based strain sensors exhibit sensitive, reproducible resistance responses over a wide strain range and enable repeatable monitoring of human joint motions and daily activities. This work establishes a simple anion-regulated phase separation strategy for engineering high-performance ion gels for wearable sensing.

PMID 42902532
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PubMedMacromolecular rapid communications2026-10-21

A One-Stone-Two-Birds Strategy to Develop P-Por COF/PDES Composite Gels for Photothermal/Photodynamic Antibacterial Activity and Wearable Strain Sensing.

Ma Zheng Z, Wang Linlin L, Fan Ziyang Z, Yang Wenjie W et al.

Flexible wearable electronics face growing bacterial infection risks from prolonged skin contact, creating an urgent demand for flexible materials integrating efficient sensing and antibacterial functions. Herein, a novel phosphorus-containing porphyrin covalent organic framework (P-Por COF) was synthesized via a solvothermal Schiff-base reaction, and incorporated into a polymerizable deep eutectic solvent to fabricate P-Por COF/PDES composite gels through in-situ UV polymerization. The resulting gel exhibited enhanced photothermal performance, improved mechanical properties, and excellent near-infrared (NIR) triggered antibacterial activity. Under 730 nm NIR light irradiation, the P-Por COF/PDES composite gel could reach 76 °C with 4 min, while showing excellent stability of photothermal cycle. Based on the synergistic effect of photodynamic production of singlet oxygen and photothermal effect, the P-Por COF/PDES composite gel resulted in a high bactericidal rate of nearly 100% against both Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli). The P-Por COF/PDES composite gel delivered a fracture strain up to 2435.82% and 2.6-fold higher toughness than pure PDES, along with stable, sensitive and self-healable strain sensing for human motion monitoring. Overall, this work provides a simple and effective strategy for developing antibacterial materials and multifunctional gels with integrated therapeutic and sensing capabilities.

PMID 42902540
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