Targretin oral (bexarotene oral)

V-125 but not bexarotene reprograms tumor transcriptional programs and the immune landscape in an anti-tumor manner in the MMTV-neu mouse model and in in vitro models of HER2+ breast cancer. This highlights its promise as a selective RXR agonist with anti-tumor and immunomodulatory activity in HER2+ breast cancer.

Bexarotene activates the Wnt signaling pathway, and treatment with the Wnt inhibitor IWR-1 can partially rescue the neurodevelopmental impairments in embryos. In summary, bexarotene offers new insights into the potential neurodevelopmental risks in zebrafish embryos, emphasizing the importance of preventing drug side effects and ensuring the safe and rational use of medications to protect the health of living organisms.

P1, N=20, Recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: Mar 2026 --> Mar 2027 | Trial primary completion date: Mar 2026 --> Mar 2027

The patient achieved a partial response with methotrexate but discontinued after ~12 months due to elevated transaminases. Following treatment with bexarotene then gemcitabine, CHOP chemotherapy was initiated in December 2019, but, after a period of partial skin response, the patient relapsed with progression of skin lesions...Disease progression in the skin occurred in December 2020; mogamulizumab was continued, and the patient achieved remission with the addition of etoposide and prednisone in August 2021...In October 2022, the patient was diagnosed with large cell CD30+ transformation, and the therapeutic approach was changed to extracorporeal photopheresis, brentuximab vedotin, and topical steroids. The patient died in February 2023 due to sepsis. Our experience adds to the limited evidence that mogamulizumab may be continued in combination with etoposide following disease progression in patients with MF with blood involvement; however, more research is needed on the efficacy and safety of this approach.

This study identified seven prognostic genes and provided a new theoretical basis for exploring immune defense mechanisms and targeted therapeutic drugs in PRAD.

The low-risk group exhibited improved survival outcomes and increased sensitivity to immunotherapy, whereas the high-risk group showed heightened sensitivity to to bexarotene, bicalutamide, embelin, FH535, and pazopanib. Quantitative PCR results indicated that ILF3-DT and PPP1R14B-AS1 were downregulated in CC tissues, whereas RUSC1-AS1 was upregulated. In conclusion, we developed a novel prognostic risk signature based on 9 disulfidptosis-related lncRNAs, which may serve as an independent predictor of immunotherapy response and chemotherapy sensitivity in CC.

GSTK1 was shown to be a tumor suppressor via its role in MQC and L-carnitine metabolism. Bexarotene and L-carnitine supplementation may serve as potential therapeutic strategies for HCC treatment.

This case highlights bexarotene as a promising therapeutic option for refractory pcALCL. Our experience reinforces the potential of bexarotene as a viable treatment for pcALCL, particularly in recurrent or refractory cases where conventional therapies are contraindicated or ineffective.

Bexarotene alleviates BCP in rats by suppressing the aberrant overexpression of SLC38A3, thereby blocking the PI3K/AKT signaling pathway-mediated upregulation of TRPV1. These findings indicate that SLC38A3, through its downstream PI3K/AKT-TRPV1 axis, may serve as a potential molecular mechanism for analgesia in BCP.

Under BXR treatment, a reduced frequency of cells with these gut-homing receptors was observed in the blood of CTCL patients regarding memory T cells (mean off: 1.9%; on: 0.6%) and B cells (mean off: 5.7%, on: 4%). BXR via RXRs directly targets B and T lymphocytes, inducing retinoid target gene expression, including gut-homing receptors.

P1, N=12, Completed, National Cancer Centre, Singapore | Recruiting --> Completed | Trial primary completion date: Sep 2024 --> Aug 2025

These findings suggest a novel extracellular activity of bexarotene and validate the combined use of TRIC and TR-FRET as a scalable screening strategy for SLIT2-targeted small molecules. This platform lays the groundwork for future high-throughput discovery efforts against SLIT2 and its signaling axis.