raloxifene hydrochloride

Although anti-estrogen treatments such as tamoxifen have significantly improved treatment outcomes, but their prolonged use is associated with therapeutic resistance and adverse effects...The multistep screening identified HIT 1 compound with a superior docking score (-13.901 kcal/mol) as compared to standard drug raloxifene (-12.136 kcal/mol), as well as favourable pharmacokinetic properties and enhanced MM-GBSA binding free energies...In addition, DFT calculations supported its electronic stability and bio-feasibility through analysing its HOMO-LUMO energy gap. These results suggest that the HIT 1 molecule serves as a promising scaffold for the development of a novel ERα modulator with potential to suppress ERα-mediated BC progression and angiogenesis.

Raloxifene remains the only benzothiophene-based drug approved for an oncological indication, highlighting both the scaffold's clinical promise and the translational barriers that have limited its broader therapeutic advancement. This review also examines key structure-activity relationships, binding determinants, and optimization strategies guiding benzothiophene-based anti-cancer therapeutics.

Several established therapeutic agents, including minoxidil, raloxifene, propranolol, aspirin, chloroquine, and metformin, have been successfully repurposed to explore additional pharmacological applications. These agents also exert antitumor effects by modulating key oncogenic pathways, such as Wnt/β-catenin, mTOR, and Hedgehog, and by selectively targeting cancer stem cells as well as tumor-associated microbiota. This review aims to explore the burgeoning potential of antimicrobial agents in oncology, highlighting their roles in reducing infection-related mortality, enhancing therapeutic effectiveness, and improving the overall quality of life in cancer patients.

E2 and RAL improved renal function and histology, reduced inflammation and oxidative stress, restored GPER expression, increased nuclear Nrf2, and upregulated HO-1 and NAD(P)H:quinone oxidoreductase 1 (NQO1). Co-treatment with ML385 or G15 reversed RAL's benefits, reduced nuclear Nrf2, and worsened injury; E2 and RAL exert renoprotective effects against OVX-related renal IRI in a manner consistent with GPER-dependent Nrf2 nuclear translocation, which suggests involvement of the downstream antioxidant gene activation pathway.

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.