raloxifene hydrochloride

P2, N=108, Not yet recruiting, The University of Texas Health Science Center at San Antonio

Vorinostat and raloxifene exhibited notable binding affinity for PEBP1. Furthermore, an independent prognostic model for LUAD was developed, enhancing our understanding of high-/low-risk cohorts' functional pathways. Drug prediction results provided valuable insights into potential therapeutic strategies for LUAD, warranting further investigation.

The current FDA-approved SERMs include tamoxifen, toremifene, and raloxifene, while the only SERD that has been approved to date is fulvestrant. Various generations of AIs are available for the treatment of hormone-positive breast cancers, including exemestane, letrozole, and anastrozole. Aromatase inhibitors are often utilized following relapse with therapies such as tamoxifen. Herein, we focus on and review the major FDA-approved aromatase inhibitors used to treat ER-positive breast cancer.

Among the most studied SERMs are Tamoxifen and Raloxifene. The pharmacological profile of SERMs therefore reflects a delicate equilibrium between receptor-mediated vascular protection and thrombotic liability. Indeed, their raison d'être increasingly extends beyond oncology into cardiovascular endocrine pharmacology, where they serve as prototypes for designing next-generation agents with optimized receptor selectivity and safer vascular outcomes.

The existing treatments, such as hormonal drugs and selective estrogen receptor modulators like raloxifene, have side effects and recurrence, and thus indicate the need for less harmful non-hormonal therapies...Procyanidin is a phytochemical lead that shows promise for controlling ESR1 signaling in fibroids and endometriosis as a non-hormonal candidate. Procyanidin emerged as a promising in-silico lead for ESR1 modulation, showing high binding affinity and dynamic stability; nevertheless, further pharmacokinetic, ADMET, and experimental validation are required to substantiate its therapeutic potential.

P2, N=242, Recruiting, Beth Israel Deaconess Medical Center | Not yet recruiting --> Recruiting

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