Targretin oral (bexarotene oral) News

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|||||||||| Targretin oral (bexarotene oral) / ReXceptor
Hypofractionated Low-Dose Total Skin Electron Beam Therapy for Primary Cutaneous T-Cell Lymphoma: Analysis of Efficacy and Toxicity (GWCC - Hall B5, Level 1) - Nov 5, 2021 - Abstract #ASH2021ASH_2941;
This novel condensed low-dose TSEBT comes with the added benefits of convenience and cost-effectiveness, as well as decreased patient exposure to the healthcare system during the current pandemic, and should be considered for all CTCL patients needing TSEBT. Moving forward, we look to evaluate the impact of radiation therapy with concurrent or adjuvant treatments for patients with CTCL as alternative options for possibly supplementing the efficacy of radiotherapy and/or reducing the need for recurrent radiation altogether.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
Genetic Ablation of Nuclear Receptor Interacting Protein 1 (NRIP1) Sensitizes Acute Myeloid Leukemia Cells to Retinoic Acids (GWCC - Hall B5, Level 1) - Nov 5, 2021 - Abstract #ASH2021ASH_2702;
We next assessed the sensitivity of the NRIP1 WT/KO cells to retinoic acids ATRA and bexarotene...This study suggests a potential mechanism of differentiation inhibition mediated by corepressor NRIP1 in AML cells unresponsive to retinoic acids. Further in-depth analyses of molecular pathways governed by NRIP1 during ligand activation of NHRs are warranted to design differentiation therapies for AML.

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Journal: Nose-to-brain drug delivery mediated by polymeric nanoparticles: influence of PEG surface coating. (Pubmed Central) - Nov 4, 2021
In order to overcome rapid nasal mucociliary clearance, low epithelial permeation, and local enzymatic degradation, we investigated the influence of PEGylation on nose-to-brain delivery of polycaprolactone (PCL) nanoparticles (PCL-NPs) encapsulating bexarotene, a potential neuroprotective compound...Combined, these results indicate that PEGylation of PCL-NPs with PCL-PEG is able to reduce NP interactions with the mucus, leading to a more efficient drug delivery to the brain following intranasal administration. Graphical abstract.

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Review, Journal: Synthetic Retinoids as Potential Therapeutics in Prostate Cancer-An Update of the Last Decade of Research: A Review. (Pubmed Central) - Oct 29, 2021
Therefore, in this review, we present the results of the experimental studies on synthetic retinoids conducted within the last decade. Our primary aim is to highlight the molecular targets of these compounds and to identify their potential promise in the treatment of PC.

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Journal: Identification of Novel Anthracycline Resistance Genes and Their Inhibitors. (Pubmed Central) - Oct 25, 2021
Bexarotene treatment had a comparable doxorubicin-sensitizing effect in HMOX1-transfected cells and desloratadine in PRKCA-transfected cells. Novel drug resistance mechanisms independent of ABC transporters have been identified that contribute to anthracycline resistance in MDR cells.

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Journal: Bexarotene inhibits cell proliferation by inducing oxidative stress, DNA damage and apoptosis via PPARγ/ NF-κB signaling pathway in C6 glioma cells. (Pubmed Central) - Oct 15, 2021
Furthermore, we determined that bexarotene-induced apoptotic C6 cells enhanced through Annexin V-FITC/PI staining and caspase-3/-7 activation analyses since phosphatidylserine level on the outer surface of the cell membrane and caspase-3/-7 activities were increased in the cells treated with bexarotene. In conclusion, bexarotene treatment in C6 glioma cells could modulate apoptosis profile, DNA damage, ROS production, and reduction of TAS levels through inhibition of NF-κB by enhancing PPARγ expression.

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Preclinical, Journal: The RXR Agonist MSU42011 Is Effective for the Treatment of Preclinical HER2+ Breast Cancer and Kras-Driven Lung Cancer. (Pubmed Central) - Oct 14, 2021
Bexarotene, the only FDA-approved RXR agonist, is still used to treat cutaneous T-cell lymphoma...However, MSU42011 was ineffective in an athymic human A549 lung cancer xenograft model, supporting an immunomodulatory mechanism of action. (4) Collectively, these data suggest that the RXR agonist MSU42011 can be used to modulate the tumor microenvironment in breast and lung cancer.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
#Remyelination compound #bexarotene reduced visual evoked potential latency in people with relapsing-remitting #MS; faster nerve conduction in optic nerves. Cambridge Centre for Myelin Repair. #ECTRIMS2021 (Twitter) - Oct 13, 2021

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Clinical, Reimbursement, Medicare: Bexarotene: A Case Study of Medicare Part D’s Specialty Drug Shortcomings. Why do so many Medicare patients continue to receive brand-name bexarotene despite the availability of generic alternatives? @MayoProceedings https://t.co/2zC13cgIE7 (Twitter) - Oct 11, 2021

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Journal: Pharmacological Activation of RXR-α Promotes Hematoma Absorption via a PPAR-γ-dependent Pathway After Intracerebral Hemorrhage. (Pubmed Central) - Oct 8, 2021
Our results showed that pharmacologically activating RXR-α with bexarotene significantly accelerated hematoma clearance and alleviated neurological dysfunction after ICH...In conclusion, the pharmacological activation of RXR-α confers robust neuroprotection against ICH by accelerating hematoma clearance and repolarizing microglia/macrophages towards the M2 phenotype through PPAR-γ-related mechanisms. Our data support the notion that RXR-α might be a promising therapeutic target for ICH.

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Journal: Bexarotene combined with lapatinib for the treatment of Cushing's disease: evidence based on drug repositioning and experimental confirmation. (Pubmed Central) - Oct 6, 2021
Our data support the notion that RXR-α might be a promising therapeutic target for ICH. No abstract available

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Journal: Multi-Omics Approach to Dissect the Mechanisms of Rexinoid Signaling in Myoblast Differentiation. (Pubmed Central) - Oct 5, 2021
We have previously shown that bexarotene, an agonist of retinoid X receptor (RXR) approved for cancer therapy, promotes the specification and differentiation of skeletal muscle progenitors...Our analyses also reveal molecular pathways underlying different patterns of gene expression and p300-associated histone acetylation at distinct chromatin states in rexinoid-enhanced myoblast differentiation. These datasets can be repurposed for future studies to examine the relationship between signaling molecules, chromatin modifiers and histone acetylation in myogenic regulation, providing a framework for discovery and functional characterization of muscle-specific loci.

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Journal, IO biomarker: Potential therapeutic uses of rexinoids. (Pubmed Central) - Oct 3, 2021
Bexarotene was approved in 1999 for the treatment of cutaneous T cell lymphoma...This beneficial effect on immune cells supports the promise of combining rexinoids with approved checkpoint blockade therapies in order to enhance efficacy of the latter and to delay or potentially eliminate drug resistance. The data compiled in this review strongly suggest that targeting RXR nuclear receptors is a promising new avenue in immunomodulation for cancer and other chronic inflammatory diseases.

|||||||||| Cametor (cetilistat) / Norgine, Targretin oral (bexarotene oral) / ReXceptor
FDA event, Journal: Inhibitory activity of FDA-approved drugs cetilistat, abiraterone, diiodohydroxyquinoline, bexarotene, remdesivir, and hydroxychloroquine on COVID-19 main protease and human ACE2 receptor: A comparative in silico approach. (Pubmed Central) - Sep 28, 2021
The MD simulation results demonstrated that these drugs interact to stabilize the systems, allowing them to be used as effective inhibitors of these proteins. Meanwhile, bexarotene, abiraterone, cetilistat, and diiodohydroxyquinoline's systemic effects should be further investigated in suitable ex vivo human organ culture or organoids, animal models, or clinical trials.

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Clinical, Journal: Lichen planopilaris in a patient treated with bexarotene for lymphomatoid papulosis. (Pubmed Central) - Sep 26, 2021
Meanwhile, bexarotene, abiraterone, cetilistat, and diiodohydroxyquinoline's systemic effects should be further investigated in suitable ex vivo human organ culture or organoids, animal models, or clinical trials. No abstract available

|||||||||| Targretin oral (bexarotene oral) / ReXceptor, sulindac / Generic mfg.
From the September issue: Combination of Sulindac and Bexarotene for Prevention of Intestinal Carcinogenesis in Familial Adenomatous Polyposis. https://t.co/K6RZAKNAv5. @MDAndersonNews @evilarsan @Charles_M_Bowen (Twitter) - Sep 24, 2021

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Journal: Targeting the TR4 nuclear receptor with antagonist bexarotene can suppress the proopiomelanocortin signalling in AtT-20 cells. (Pubmed Central) - Sep 23, 2021
Results from in vivo mouse model also revealed that oral bexarotene administration markedly suppressed ACTH-secreting tumour growth, adrenal enlargement and the secretion of ACTH and corticosterone in mice with already established tumours. Together, these results suggest that bexarotene may be developed as a potential novel therapeutic drug to better suppress Cushing's disease.

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[VIRTUAL] Bexarotene treatment leads to durable improvements in visual evoked potential latency; a follow-up study of the Cambridge Centre for Myelin Repair trial One (ePoster Library) - Sep 23, 2021 - Abstract #ECTRIMS2021ECTRIMS_2278;
This follow-up study to CCMR One shows that the full-field VEP latency improvements observed in the original trial are durable, suggests long-term benefits from exposure to a remyelinating drug, and supports the potential importance of MF-VEP assessments in remyelination trials. While these data support the original trial finding that bexarotene has a biological effect to promote remyelination in humans, they should be interpreted in light of the significant adverse events that were observed on the trial.

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[VIRTUAL] Bexarotene treatment leads to durable improvements in visual evoked potential latency; a follow-up study of the Cambridge Centre for Myelin Repair trial One (Stream 7 Therapy / Global views) - Sep 23, 2021 - Abstract #ECTRIMS2021ECTRIMS_1536;
This follow-up study to CCMR One shows that the full-field VEP latency improvements observed in the original trial are durable, suggests long-term benefits from exposure to a remyelinating drug, and supports the potential importance of MF-VEP assessments in remyelination trials. While these data support the original trial finding that bexarotene has a biological effect to promote remyelination in humans, they should be interpreted in light of the significant adverse events that were observed on the trial.

|||||||||| Poteligeo (mogamulizumab) / Kyowa Kirin, Targretin oral (bexarotene oral) / ReXceptor, Adcetris (brentuximab vedotin) / Seagen, Takeda
Cutaneous T-cell lymphomas - under targeted therapy with brentuximab vedotin and mogamulizumab (Stream 6) - Sep 20, 2021 - Abstract #ADO2021ADO_228;
As part of a systemic therapy, interferon alpha, bexarotene and methotrexate are used...In later lines of therapy, polychemotherapy, gemcitabine and doxorubicin have proven to be effective therapy options...The patient collective was analyzed with regard to the effectiveness (depth of response, duration of response) and tolerability (frequency and severity of side effects as well as dropout rate) under brentuximab vedotin and mogamulizumab. Results to follow.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
Foudroyant course of cutaneous T-cell lymphoma (Stream 6) - Sep 20, 2021 - Abstract #ADO2021ADO_222;
According to the decision of the tumor conference, mogamulizumab was last given...The mentioned guidelines-compliant therapy options could not stop the progression. The early stem cell transplantation in stage IVA2 remains to be discussed here too, due to the repeatedly described poor response as a result.

|||||||||| Poteligeo (mogamulizumab) / Kyowa Kirin, Targretin oral (bexarotene oral) / ReXceptor
Effective therapy of folliculotropic mycosis fungoides using low-dose Total Skin Electron Beam Therapy (LD-TSEBT) and subsequent systemic maintenance therapy with mogamulizumab (Stream 6) - Sep 20, 2021 - Abstract #ADO2021ADO_221;
The combination of LD-TSEBT and maintenance therapy using mogamulizumab achieved a so far sustained, almost complete therapeutic response in our patient with mycosis fungoides, which had previously been refractory to treatment. This combination therefore represents a promising way of controlling disease activity in patients with cutaneous T-Tell lymphoma quickly and, in particular, over the long term.

|||||||||| Poteligeo (mogamulizumab) / Kyowa Kirin, Targretin oral (bexarotene oral) / ReXceptor
Maintenance of long-term remission of Sezary's syndrome with extended therapy intervals with mogamulizumab (Stream 6) - Sep 20, 2021 - Abstract #ADO2021ADO_220;
The pivotal study showed a better response compared to the HDAC inhibitor vorinostat (28% vs. 5%) and a longer progression-free interval of 7.7 months compared to 3.1 months...Neither therapy with systemic PUVA and interferon-alpha sc 3 × 9 million IU, extracorporeal photopheresis (ECP), metothrexate up to 20 mg / week sc nor bexarotene (2 × 225 mg / d) achieved more than a slight partial remission...Pruritus medication with cetirizine + loratadine or aprepitant and intensive moisturizing of the skin were continuously necessary...In addition, if the remission persists, extending the intervals can be considered. Clinical studies are necessary here to confirm the effectiveness of extended intervals as a maintenance dose.

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Preclinical, Journal: Ex Vivo Investigation of Bexarotene and Nicotinamide Function as a Protectıve Agent on Rat Synaptosomes Treated with Aβ(1-42). (Pubmed Central) - Sep 16, 2021
On the other hand, bexarotene caused a moderate increase in SIRT1 levels with PPARγ activation. Consequently, we found that nicotinamide can be more effective than bexarotene in AD pathogenesis by regulating mitochondrial functions in synaptosomes.

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Preclinical, Journal: Suppression of TLR4/MyD88/TAK1/NF-κB/COX-2 Signaling Pathway in the Central Nervous System by Bexarotene, a Selective RXR Agonist, Prevents Hyperalgesia in the Lipopolysaccharide-Induced Pain Mouse Model. (Pubmed Central) - Sep 9, 2021
Bexarotene also prevented the reduction in RXRα protein expression associated with a rise in the expression of TLR4, MyD88, phosphorylated TAK1, NF-κB p65, phosphorylated NF-κB p65, COX-2, and IL-1β proteins, in addition to COX-2 activity and levels of PGE and IL-1β in the brains and spinal cords of the LPS-treated animals. Likely, decreased activity of TLR4/MyD88/TAK1/NF-κB/COX-2 signaling pathway in addition to increased pro-inflammatory cytokine formation in the CNS of mice participates in the protective effect of bexarotene against hyperalgesia induced by LPS.

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Clinical, P2a data, Journal: Safety and efficacy of bexarotene in patients with relapsing-remitting multiple sclerosis (CCMR One): a randomised, double-blind, placebo-controlled, parallel-group, phase 2a study. (Pubmed Central) - Sep 4, 2021
We do not recommend the use of bexarotene to treat patients with multiple sclerosis because of its poor tolerability and negative primary efficacy outcome. However, statistically significant effects were seen in some exploratory MRI and electrophysiological analyses, suggesting that other retinoid X receptor agonists might have small biological effects that could be investigated in further studies.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor, Adcetris (brentuximab vedotin) / Seagen, Takeda
Journal: Brentuximab Vedotin for Relapsed or Refractory Sézary Syndrome. (Pubmed Central) - Sep 2, 2021
In this case series, brentuximab vedotin use was associated with some efficacy in SS across multiple disease compartments and in the setting of refractory disease or low CD30 skin expression. Brentuximab vedotin may offer a manageable treatment schedule and low incidence of significant toxic effects.

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Journal: Photodegradation of Bexarotene and Its Implication for Cytotoxicity. (Pubmed Central) - Aug 29, 2021
The cytotoxicity of the formed products after 4 h of UV irradiation was significantly higher than that of the parent compound (p < 0.05). Furthermore non-cancerous murine fibroblasts exhibited marked concentration-dependent inhibition by bexarotene, while the degradation products elicited more pronounced antiproliferative action only at the highest applied concentration.

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Journal: Acitretin and Retinoic Acid Derivatives Inhibit BK Polyomavirus Replication in Primary Human Proximal Renal Tubular Epithelial and Urothelial Cells. (Pubmed Central) - Aug 27, 2021
Retinoic acid-agonists (all-trans-retinoic acid, 9-cis-RA, 13-cis-RA, bexarotene, tamibarotene) and the RAR/RXR-antagonist RO41-5253 also inhibited BKPyV-replication, pointing to as yet undefined mechanism.ImportanceAcitretin selectively inhibits BKPyV-replication in primary human cell culture models of nephropathy and hemorrhagic cystitis. Since acitretin is an approved drug in clinical use reaching BKPyV-inhibiting concentrations in systemically treated patients, further studies are warranted to provide data for clinical repurposing of retinoids for treatment and prevention of replicative BKPyV-diseases.

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Journal: Teratogen update: Topical use and third-generation retinoids. (Pubmed Central) - Aug 20, 2021
Additionally, rational drug design has been applied to create today's third-generation retinoids (adapalene, tazarotene, and bexarotene)...Given the paucity of epidemiologic data available at this time, however, it is recommended that the use of topical retinoids during pregnancy be avoided. However, in circumstances when inadvertent exposure in pregnancy may occur, the available data provide some reassurance that adverse pregnancy outcomes are unlikely.

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Journal: Effectiveness of combined bexarotene and excimer laser treatment for folliculotropic mycosis fungoides. (Pubmed Central) - Aug 19, 2021
However, in circumstances when inadvertent exposure in pregnancy may occur, the available data provide some reassurance that adverse pregnancy outcomes are unlikely. No abstract available

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Preclinical, Journal: Inhibition of MAPT enhances the effect of bexarotene and attenuates the damage after traumatic brain injury using in vivo and in vitro experiments. (Pubmed Central) - Aug 19, 2021
These effects might be mediated by activation of the Nrf2/HO-1 signalling pathway and inhibition of the MAPK/NF-kB signalling pathway. Thus, we concluded that inhibition of MAPT might represent a novel treatment target for TBI.

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Visual evoked potentials record the time it takes for signals to travel from the eye to the brain ["latency"]. This is increased after attacks of demyelination, because the nerve does not work well. Bexarotene restores myelin, speeds up conduction and reduces the VEP latency. (Twitter) - Aug 19, 2021

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Not all lesions remyelinate equally! Bexarotene promotes #remyelination most effectively in grey matter lesions. (Twitter) - Aug 19, 2021

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
We show that bexarotene improves the MTR signal from demyelinated lesions... suggesting that there has been #remyelination. (Twitter) - Aug 19, 2021

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
Adverse events: We show that the cancer drug bexarotene, a RXRgamma agonist, has too many side-effects to use in #MS. And we did not reach our primary endpoint. But there is evidence that bexarotene promotes #remyelination, from MRI and electrophysiology. https://t.co/ao7qUVvMkK (Twitter) - Aug 19, 2021

|||||||||| Review: Anticancer drugs repurposed for Alzheimer’s disease: a systematic review with a therapeutic rationale for repurposing for dementia: Vorinostat Bosutinib Masitinib Dasatinib Nilotinib Pexidartinib Bexarotene Tamibarotene Thalidomide Lenalidomide Daratumumab https://t.co/3yqqpczjGC (Twitter) - Aug 18, 2021

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Journal, IO biomarker: A dual macrophage polarizer conjugate for synergistic melanoma therapy. (Pubmed Central) - Aug 13, 2021
Bexarotene (BEX) is a retinoid that induce the expression of phagocytic receptors in macrophages besides its ability to downregulate the M2 polarization...Immunoprofiling of the excised tumors revealed a significant increase in the M1/M2 ratio of TAMs in mice treated with the dual conjugate. Our intravenously injectable HA conjugate of RES and BEX provides a promising immunotherapeutic combination strategy for resetting the M1/M2 ratio, supporting the tumoricidal activity of TAMs for effective melanoma treatment.

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Journal: Targeting BRF2 in Cancer Using Repurposed Drugs. (Pubmed Central) - Aug 8, 2021
We found that bexarotene (Bex) treatment resulted in a dramatic decline in oxidative stress and Tert-butylhydroquinone (tBHQ)-induced levels of BRF2 and consequently led to a decrease in the cellular proliferation of cancer cells which may in part be due to the drug pretreatment-induced reduction of ROS generated by the oxidizing agent. Our data thus provide the first experimental evidence that BRF2 is a novel player in the DNA damage response pathway and that bexarotene can be used as a potential inhibitor to treat cancers with the specific elevation of oxidative stress.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
[VIRTUAL] Targeting TR4 nuclear receptor with antagonist Bexarotene increases Docetaxel sensitivity to better suppress the metastatic castration-resistant prostate cancer progression () - Aug 5, 2021 - Abstract #AUA2021AUA_1244;
Our data thus provide the first experimental evidence that BRF2 is a novel player in the DNA damage response pathway and that bexarotene can be used as a potential inhibitor to treat cancers with the specific elevation of oxidative stress. We identify a novel role of TR4 that may function via altering the TR4/lincRNA-p21/HIF-1a/VEGF-A signaling to modulate the DTX-resistance in PCa, and targeting this newly identified signaling with Bex, a FDA-approved drug, may lead to increase DTX chemo-sensitivity to better suppress the mCRPC progression.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
[VIRTUAL] An RXR agonist causes age-dependent remyelination in people with relapsing remitting MS (Stream 7 Therapy / Global views) - Aug 3, 2021 - Abstract #ECTRIMS2021ECTRIMS_1288;
We identify a novel role of TR4 that may function via altering the TR4/lincRNA-p21/HIF-1a/VEGF-A signaling to modulate the DTX-resistance in PCa, and targeting this newly identified signaling with Bex, a FDA-approved drug, may lead to increase DTX chemo-sensitivity to better suppress the mCRPC progression. These results provide evidence that bexarotene promotes remyelination best in younger patients, reinforcing the need to address the age-associated decline in remyelination capacity to develop successful remyelinating therapies that work across the lifespan.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
[VIRTUAL] Bexarotene treatment leads to durable improvements in visual evoked potential latency; a follow-up study of the Cambridge Centre for Myelin Repair trial One (ePoster Library) - Aug 3, 2021 - Abstract #ECTRIMS2021ECTRIMS_698;
This follow-up study to CCMR One shows that the full-field VEP latency improvements observed in the original trial are durable, suggests long-term benefits from exposure to a remyelinating drug, and supports the potential importance of MF-VEP assessments in remyelination trials. While these data support the original trial finding that bexarotene has a biological effect to promote remyelination in humans, they should be interpreted in light of the significant adverse events that were observed on the trial.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
Retrospective data, Journal: Management experience of advanced-stage mycosis fungoides/ Sézary syndrome: a retrospective study from Spanish haematology referral units. (Pubmed Central) - Jul 21, 2021
Survival is more favourable for MF compared to SS. Current chemoimmunotherapies are insufficient to control disease, making allo-SCT the best therapeutic approach in selected patients.

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Journal: lncRNA NEAT1 ameliorates LPS‑induced inflammation in MG63 cells by activating autophagy and suppressing the NLRP3 inflammasome. (Pubmed Central) - Jul 14, 2021
LPS upregulated the expression of inflammatory cytokines and NLRP3, inhibited the expression of autophagy‑related and osteogenesis‑related proteins, promoted apoptosis and altered the cell cycle, which was partially inhibited by NEAT1 overexpression and promoted by bexarotene. LPS stimulated inflammation in the MG63 cells and inhibited the retinoid X receptor (RXR)‑α to downregulate the expression of NEAT1 and decrease levels of autophagy, which promoted the activation of NLRP3 and the release of inflammatory factors, and impaired the functional activity of osteoblasts, thus promoting the development of inflammation.

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Journal: Dissecting myogenin-mediated retinoid X receptor signaling in myogenic differentiation. (Pubmed Central) - Jun 24, 2021
We have previously established that a rexinoid x receptor (RXR)-selective agonist, bexarotene, enhances the differentiation and fusion of myoblasts through a direct regulation of MyoD expression, coupled with an augmentation of myogenin protein...Moreover, RXR signaling augments residue-specific histone acetylation at enhancers co-occupied by p300 and myogenin. Thus, genomic distribution of transcriptional regulators is an important designate for identifying novel targets as well as developing therapeutics that modulate epigenetic landscape in a selective manner to promote muscle regeneration.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor
Journal: Evaluating Novel RXR Agonists That Induce ApoE and Tyrosine Hydroxylase in Cultured Human Glioblastoma Cells. (Pubmed Central) - Jun 22, 2021
This novel discovery has potential clinical implications for treatment of PD since it suggests that the combination of an RXR agonist and a Nurr1 ligand can significantly enhance RXR-Nurr1 heterodimer activity and drive enhanced therapeutic expression of the TH gene to increase endogenous synthesis of dopamine. These data indicate that is it possible and prudent to develop novel rexinoids for testing of gene expression and side effect profiles for use in potential treatment of neurodegenerative disorders, as individual rexinoids can have markedly different gene expression profiles but similar structures.

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Biomarker, Clinical, Retrospective data, Review, Clinical Trial,Phase I, Journal: Novel Inflammatory Biomarkers in Patients with Mycosis Fungoides Treated with Bexarotene. (Pubmed Central) - Jun 22, 2021
Moreover, these results indicate that decrease in these inflammatory biomarkers may signify improvement of the disease. Key Words: Bexarotene, İnflammatory biomarkers, Mycosis fungoides.

|||||||||| Targretin oral (bexarotene oral) / ReXceptor, Roferon A (recombinant interferon alfa-2a) / Roche, Adcetris (brentuximab vedotin) / Seagen, Takeda
[VIRTUAL] TWO CASES OF ADVANCE STAGE MYCOSIS FUNGOIDES WHİCH WAS ACHİEVED COMPLETE RESPONSE WITH BRENTUXIMAB VEDOTIN THERAPY () - Jun 20, 2021 - Abstract #ICLLM2021ICLLM_127;
Patients with Foliculotrophic MF in advanced stages havea poor prognosis. In this group of patients, there is no consensus aboutthe treatment modalities and the result of treatment is not satisfactory.Brentuximab Vedotin is a new and promising option for advanced stages MFpatients without regard to CD30 expression rate.

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Review, Journal: Some Candidate Drugs for Pharmacotherapy of Alzheimer's Disease. (Pubmed Central) - Jun 3, 2021
The latter, especially when combined with antipsychotics (for instance quetiapine or risperidone), were shown to reduce neuropsychiatric symptoms in AD patients...Considering a close relationship between brain ischemia and AD, they may also reduce post-brain ischemia neurodegeneration. An investigational compound, CN-105 (a lipoprotein E agonist), has a very good profile in AD preclinical studies, and its clinical trial for postoperative dementia is starting soon.

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Journal: Endogenous and combination retinoids are active in myelomonocytic leukemias. (Pubmed Central) - May 28, 2021
Combination synergy could be replicated in additional, but not all, AML cell lines and primary samples, and was associated with improved survival in vivo, although tolerability of bexarotene administration in mice remained an issue. These data provide insight into the basal presence of natural retinoids in leukemias in vivo and a potential strategy for clinical retinoid combination regimens in leukemias beyond acute promyelocytic leukemia.



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