raloxifene hydrochloride

In this study, we rationally optimized the benzothiophene scaffold of the SERM raloxifene through strategic linker modifications, culminating in the discovery of B7, a potent ERα degrader validated by structure-activity relationship analysis. In the T47D xenograft mouse model, the combination of B7 and Palbociclib demonstrated potent antitumor activity, achieving a tumor growth inhibition rate of 89.2 %. Further structural modification based on B7 may lead to the development of a candidate.

This framework invites translational trials using biomarker-enriched patient stratification. If validated, it could reshape the role of sex hormones in male psychiatry-not as contraindications, but as precision neuromodulators aligned with neurobiological pathology.

Through a signature similarity search using the Library of Integrated Network-Based Cellular Signatures dataset, we identified raloxifene, purpurogallin and enoxacin as pharmacological agents that mimic the effects of CBP20 knockdown. Treatment with these agents significantly inhibited cell growth, highlighting a potential avenue for targeted cancer therapy. These findings suggest that CBP20 plays a pivotal role in RNA modification-mediated tumor progression and may represent a promising therapeutic target in cancer treatment.

The AS1411 aptamer was conjugated to the nanoliposomes to target nucleolin, a protein overexpressed in cancer cells...The encapsulation efficiencies were 88.63% (raloxifene), 41.73% (etoricoxib), and 39.26% (naringin) without the aptamer, and 81.99%, 36.66%, and 38.33%, respectively, with the aptamer. The IC50 of the formula for the three co-loaded agents was 167.4 µg/mL for A549 cells and 2.6 µg/mL for MCF-7 cells. Cytotoxicity was further enhanced using their aptamer conjugate, particularly against the MDA-MB-231 cell line.ConclusionThe novel triple-drug-loaded, aptamer-conjugated nanoliposome formula may be a future cancer treatment strategy.

Raloxifene, another SERM, has risk-reducing benefits with a better safety profile compared to tamoxifen. AI, like anastrozole and exemestane, reduced invasive breast cancer with better side effect profile. Denosumab, a monoclonal antibody that tackles receptor activator of nuclear factor kappa B (RANK-RANKL), is promising in preventing breast cancer in healthy carriers of pathogenic BRCA1 variants...However, careful consideration of side effects and individual risk factors are crucial to enhance uptake rate. Further research is needed to compare the effectiveness of SERMs and AI in preventing breast cancer, especially in high-risk populations with pathogenic germline mutations.

P=N/A, N=98, Recruiting, Guangzhou University of Traditional Chinese Medicine | Trial completion date: Feb 2025 --> Dec 2026 | Trial primary completion date: Dec 2024 --> Jun 2026

P2, N=242, Not yet recruiting, Beth Israel Deaconess Medical Center | Trial completion date: Aug 2029 --> Aug 2030 | Initiation date: Jun 2025 --> Oct 2025

TMX was associated with an increased risk of EC in premenopausal and perimenopausal women (mean relative risk 2.25; standard deviation 0.9) compared to no treatment or treatment with raloxifene or aromatase inhibitors. TMX seems to increase EC risk and significantly increase the risk of gynecological symptoms in premenopausal and perimenopausal women, with risk persisting years following treatment cessation. Healthcare professionals should counsel these women on potential risks and emphasize prompt evaluation of gynecological symptoms.

Female Wistar rats orally administered with SRC@LNPs4 (∼10 mg/kg of RLX) exhibited a hike (unpaired t-test, p < 0.05) of 1.87-fold in the AUC0-t of SRC@LNPs4 (43.04 ± 0.50 h·μg/mL) compared to RLX (22.95 ± 4.30 h·μg/mL) Furthermore, the notable changes observed in the pharmacokinetic parameters of SRC@LNPs4 in rats previously injected with cycloheximide (CHX; 3 mg/kg) suggest that the drug is primarily absorbed into systemic circulation through lymphatic uptake. In conclusion, SRC@LNPs4 presents a valuable strategy to augment oral absorption and bioavailability via lymphatic targeting.

In addition, the combination of PDT with NAC resulted in an improved therapeutic outcome in vivo in SKH-1 mice with cSCC photogenerated by chronic exposition to ultraviolet light. In conclusion, the combination of PDT with NAC or raloxifene enhances PDT efficacy by mitigating resistance mechanisms, which can open new avenues for the treatment of cSCC.

Proximal jejunal and terminal ileal spheroid-derived differentiated cell monolayers showed H+- and Na+-coupled uptake of methotrexate and [3H]-taurocholic acid, respectively. The functional expression of CYP3A, CYP2C9, UGT1A, P-glycoprotein, and breast cancer resistance protein (BCRP) was confirmed based on the formation of metabolites (1'-hydroxy midazolam, 4'-hydroxy diclofenac, raloxifene-4'-glucuronide, and raloxifene-6-glucuronide) and the efflux ratio of typical substrates (digoxin, sulfasalazine, rosuvastatin, dantrolene, and furosemide). Terminal ileum-derived differentiated cell monolayers showed extensive taurocholic acid-d5 transport in the apical-to-basal direction, which was markedly inhibited by the ASBT inhibitor elobixibat...To date, there is no in vitro model that can reproduce regional differences in the transporter-mediated transport of nutrients and drugs in the intestine. This study successfully demonstrated that the functional expression of region-specific transporters, the proton-coupled folate transporter and the apical sodium-dependent bile acid transporter, was maintained in human proximal jejunal and terminal ileal spheroid-derived differentiated cell monolayers.

The combination of SSRIs with cisplatin, 5-fluorouracil, and raloxifene resulted in either synergistic or additive effects...Dapoxetine, paroxetine, and sertraline resulted in cell cycle arrest at the G0/G1 phase...At the same time, sertraline decreases the expression of Bcl-2 and VEGF and increases the expression of CASP8 and DR5. Results revealed that SSRIs can potentially act as antiproliferative agents against prostate cancer cells, and their activity is mediated through different signaling pathways.