raloxifene hydrochloride / Generic mfg. - LARVOL DELTA

Real world evidence of treatment patterns in hereditary hemorrhagic telangiectasia (ASH 2025) - "Treatment examinedincluded bevacizumab, pazopanib, pomalidomide, aminocaproate, tranexamic acid (TXA), octreotide,lanreotide, thalidomide, tacrolimus, sirolimus, tamoxifen and raloxifene...The majority of HHT patients were treated withferrous sulfate (n=910), followed by iron sucrose, ferrous gluconate, ferric carboxymaltose, iron dextran,and ferric derisomaltose...While 8% of patients treated with TXA had VTE, the data does not support a definitiveconclusion of increased VTE in patients treated with anti-fibrinolytics. To further elucidate treatmentpractices in HHT, a multi-center approach incorporating review of medical records would providevaluable insights into real-world practices."

Clinical • HEOR • Real-world • Real-world evidence • Anemia • Aplastic Anemia • Cardiovascular • Cerebral Hemorrhage • CNS Disorders • Gastrointestinal Disorder • Hematological Disorders • Hypertension • Renal Disease • Venous Thromboembolism

Drugs against osteoporosis in perimenopausal and postmenopausal women. (PubMed, Front Med (Lausanne)) - "Commonly used anti-resorptive drugs include bisphosphonates, denosumab, hormone replacement therapy, and raloxifene...Common examples include teriparatide, romosozumab, and parathyroid hormone...Phytoestrogens. These are non-steroidal, naturally occurring plant compounds with estrogenic and/or anti-estrogenic properties that resemble estrogen."

Journal • Review • Osteoporosis • Rheumatology

Unveiling the ESR1 dysfunction orchestrates the link per- and polyfluoroalkyl substances exposure to osteoarthritis: Insights from multi-scale evidence. (PubMed, Ecotoxicol Environ Saf) - "Importantly, the ESR1 agonist raloxifene effectively reversed these detrimental effects to maintain cartilage homeostasis. Overall, these findings revealed ESR1 dysfunction as a critical molecular event in PFAS exposure-related OA, providing novel insights into environmental etiologies of OA and potential therapeutic strategies."

Journal • Immunology • Osteoarthritis • Pain • Rheumatology • ER

BPH Management: New Treatment Strategies and Epigenetic Biomarker for Management of Benign Prostatic Hyperplasia (clinicaltrials.gov) - P2 | N=242 | Recruiting | Sponsor: Beth Israel Deaconess Medical Center | Not yet recruiting ➔ Recruiting

Biomarker • Enrollment open • Monotherapy • Benign Prostatic Hyperplasia

Factors associated with uptake of endocrine prevention in patients with atypical hyperplasia and lobular carcinoma in situ (SABCS 2025) - "After 2019, low-dose tamoxifen became the most commonly prescribed endocrine prevention regimen in HRL patients who accepted a prescription."

Clinical • Breast Cancer • Oncology

Adherence to endocrine prevention in patients with atypical hyperplasia and lobular carcinoma in situ: promising trends from real-world use of low dose tamoxifen. (SABCS 2025) - "Low-dose tamoxifen was the most common regimen prescribed (64.2%), compared to regular dose tamoxifen (11.3%), raloxifene (19.8%), and anastrozole (4.7%). Adherence to endocrine prevention is high in women who initiate medication with few discontinuing due to side effects. Many women who initiate low dose tamoxifen remain adherent, with some electing to continue the regimen for 5 years total."

Adherence • Clinical • Real-world • Real-world evidence • Breast Cancer • Oncology

FDA-approved drug repurposing identifies small molecules with antitumor activity and temozolomide sensitization in glioblastoma (SNO 2025) - "Three agents - decitabine, raloxifene, and gefitinib – the targets of which are upregulated in GBM, demonstrated selective toxicity in ≥6 GBM models and collectively covered all 12. As a single agent, avapritinib significantly reduced viability in all GBM lines – especially of interest given its preliminary efficacy in pediatric high-grade glioma...Further in vitro and in vivo experiments are in progress. These findings nominate several drug candidates for rapid clinical evaluation in GBM."

Brain Cancer • Glioblastoma • Glioma • High Grade Glioma • Oncology • Solid Tumor • PDGFRA

Pharmacological Prevention in Breast Cancer: Current Evidence, Challenges, and Future Directions. (PubMed, Cancers (Basel)) - " Tamoxifen, raloxifene, and AIs significantly reduce the incidence of estrogen receptor-positive breast cancer in high-risk populations. Pharmacoprevention offers substantial benefits in appropriately selected women. Future efforts should focus on new drugs, precision risk stratification, individualized decision-making, and overcoming barriers to implementation to maximize the impact of preventive strategies in breast cancer control."

Journal • Review • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Infectious Disease • Oncology • Solid Tumor

From Genes to Lifestyle: A Multi-Dimensional Framework for Alzheimer's Disease Prevention and Therapy. (PubMed, Ageing Res Rev) - "Drug repurposing analyses using DrugBank have identified promising therapeutic candidates, including FDA-approved agents (e.g., valproic acid, raloxifene, and clomipramine) and naturally derived compounds (e.g., quercetin and fisetin), which may modulate key AD-related pathways. Collectively, these integrative insights advocated for a multidimensional precision medicine framework that spans genetic, cellular,network, and lifestyle levels of regulation. This shift from single-target therapeutics to an integrated "gene-cell-network-lifestyle" paradigm open new theoretical and translational avenues for delaying or mitigating AD progression."

Journal • Review • Alzheimer's Disease • CNS Disorders • Inflammation

FDA-approved drug repurposing identifies small molecules with antitumor activity and temozolomide sensitization in glioblastoma (WFNOS 2025) - "Three agents - decitabine, raloxifene, and gefitinib – the targets of which are upregulated in GBM, demonstrated selective toxicity in ≥6 GBM models and collectively covered all 12. As a single agent, avapritinib significantly reduced viability in all GBM lines – especially of interest given its preliminary efficacy in pediatric high-grade glioma...Further in vitro and in vivo experiments are in progress. These findings nominate several drug candidates for rapid clinical evaluation in GBM."

Brain Cancer • Glioblastoma • Oncology • Solid Tumor • PDGFRA

Recent Advances in Osteoporosis Therapeutics. (PubMed, Annu Rev Med) - "Current therapies for osteoporosis include antiresorptive treatments, including bisphosphonates, denosumab, and raloxifene, and osteoanabolic treatments, including teriparatide, abaloparatide, and romosozumab, which is a dual-action agent. Recent guidelines have suggested categorical risk stratification and a goal-directed individualized therapy strategy. New treatments under investigation also hold promise for further improving bone health in postmenopausal osteoporosis."

Journal • Review • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

A systematic review of combination treatment strategies for osteoporosis. (PubMed, JBMR Plus) - "In conclusion, there is evidence supporting the use of combination treatment with teriparatide and denosumab, teriparatide and zoledronic acid, and alendronate and raloxifene for osteoporosis for increasing BMD more than monotherapy, although several of the studies showing benefit of these combinations are small, and data are lacking on fracture outcomes. These combinations can be considered for treatment of patients with osteoporosis; however, further larger studies would be useful to evaluate fracture outcomes as well as other combinations for potential efficacy."

Journal • Review • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Persistence With Osteoporosis Medication Treatments Among Chinese Patients With Osteoporosis: A Retrospective Cohort Study (ISPOR-EU 2025) - "The remaining patients received raloxifene, menopausal hormone therapy (MHT), teriparatide, or menatetrenone. Patients treated with denosumab exhibited higher treatment persistence compared to those receiving other anti-resorptive therapies, including oral bisphosphonates. Efforts to improve persistence are warranted, particularly among high-risk populations."

Retrospective data • Gastroenterology • Immunology • Osteoarthritis • Osteoporosis • Rare Diseases • Rheumatology

COMPARISON OF CARDIOTOXIC EFFECTS BETWEEN AIs AEROMATASE INHIBITORS) AND SERMs (SELECTIVE ESTROGEN RECEPTOR INHIBITORS): A PHARMACOVIGILANCE ANALYSIS (AHA 2025) - "We included Anastrozole, Letrozole, and Exemestane for AIs and Raloxifene, Tamoxifen, Fulvestrant, and Toremifene for SERMs. AIs are observed to be associated with higher rates of CV AEs compared to SERMs. Further studies are warranted to establish the CV risk profile of these agents."

Adverse events • Breast Cancer • Developmental Disorders • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Solid Tumor • ROR1

Research progress of DUB enzyme in breast cancer. (PubMed, Clin Exp Med) - "Despite great advances in breast cancer (BC) treatment-including agents such as Tamoxifen, Fulvestrant, Toremifene, and Raloxifene, all of which are approved for the systemic treatment of BC patients-these agents only prolong survival by a few months, and patients with advanced BC remain susceptible to drug resistance. In this review, we focused on several DUBs associated with breast cancer, including their structure, function, and relationship to BC. Among them, we focused on the USP family and OTU family, which are more extensively studied in BC."

Journal • Review • Breast Cancer • Lung Cancer • Oncology • Solid Tumor • Targeted Protein Degradation

Rational design, synthesis, and biological evaluation of Raloxifene-based potent degrader of estrogen receptor alpha. (PubMed, Bioorg Chem) - "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."

Journal • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER

The comparative efficacy of 12-mo of alendronate and raloxifene in maintaining denosumab-induced improvement in peripheral volumetric BMD, microarchitecture, and estimated strength. (PubMed, JBMR Plus) - "No significant changes in cortical porosity or thickness were observed, either during denosumab treatment or after the transition to alternate antiresorptive therapy. We conclude that denosumab improved vBMD and bone strength, and these gains were maintained with both alendronate and raloxifene, supporting raloxifene as an option for those unable or unwilling to take bisphosphonates after short-term denosumab exposure."

Journal • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Raloxifene Is Associated with Total Knee Arthroplasty in Postmenopausal Women: A Comparative Cohort Study. (PubMed, Life (Basel)) - "Kaplan-Meier analysis demonstrated raloxifene maintained the lowest cumulative TKR incidence compared to alendronate and denosumab over time, particularly beyond 5 years. These findings suggest that raloxifene may offer superior joint protection compared with alendronate and denosumab in postmenopausal women with PTOA, supporting its potential as a disease-modifying therapeutic option for this vulnerable population."

Journal • Immunology • Musculoskeletal Diseases • Orthopedics • Osteoarthritis • Osteoporosis • Pain • Rheumatology

Study of Biochemical Changes Seen in Postmenopausal Women Receiving Hormone Replacement Therapy in Comparison to Raloxifene. (PubMed, J Pharm Bioallied Sci) - "Comparison of the two groups revealed that raloxifene resulted in a greater decrease at 3 months (P < 0.001). Favorable effect of raloxifene on serum lipids and its good tolerability profile make it a good alternative to hormone replacement therapy (HRT) in postmenopausal women."

Journal

SARS-CoV-2 Entry Can Be Mimicked in C. elegans Expressing Human ACE2: A New Tool for Pharmacological Studies. (PubMed, Viruses) - "In vitro, 1-3 μM of Raloxifene reduced the entry of lentiviral particles carrying the Wuhan variant and B.1.1.7 UK and B.1.1.529 Omicron strains into HEK293-ACE2, in addition to particles expressing N501Y-mutated or P681H-mutated spike proteins. Raloxifene (0.1-1 μM) completely counteracted RBD toxicity in ACE2 worms, indicating that this strain offers a cost-effective in vivo screening platform for molecules with effects involving interactions with the ACE2 receptor."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases • ACE2

Effects of Combined Treatment With Selective Androgen and Estrogen Receptor Modulators Ostarine and Raloxifen on Bone Tissue In Ovariectomized Rats. (PubMed, Calcif Tissue Int) - "Here, a combined treatment with a selective estrogen receptor modulator (raloxifene, RAL) and a selective androgen receptor modulator (ostarine, OST) was investigated in ovariectomized rats. Conversely, the combined treatment increased serum phosphorus and luteinizing hormone levels, decreased serum magnesium and calcium, and did not attenuate the organ and uterus weight increase observed after OST, raising safety concerns. These findings highlight the need for cautious evaluation of combination therapies and suggest that there is a need for alternative compounds with improved safety profiles for future osteoporosis treatments."

Journal • Preclinical • Osteoporosis • Rheumatology

LONG-TERM BONE HEALTH IN OBETICHOLIC ACID–TREATED PATIENTS WITH PRIMARY BILIARY CHOLANGITIS: A POISE POST HOC ANALYSIS (AASLD 2025) - P3 | " Patients with PBC who had inadequate response or intolerance to ursodeoxycholic acid were randomized to receive oral placebo (n=73), OCA 5–10 mg (n=70), or OCA 10 mg (n=73) daily in the 12-month double-blind phase...Subgroup analyses were performed in women and postmenopausal women, as well as in patients on osteoporosis medications (eg, bisphosphonates, abaloparatide, denosumab, and raloxifene) and those not on osteoporosis medications... While there was a slight decline in T-scores over 72 months with OCA treatment, BMD remained relatively stable, including in high-risk subgroups and patients being treated for osteoporosis."

Clinical • Retrospective data • Hepatology • Immunology • Orthopedics • Osteoporosis • Primary Biliary Cholangitis • Rheumatology

Exploiting the angiotensin-converting enzyme pathway to augment endogenous opioid signaling. (PubMed, Commun Biol) - "We recently identified a non-canonical central role of ACE in the degradation of enkephalin heptapeptide, Met-enkephalin-Arg-Phe (MERF)...Our primary hits (thiorphan, D609, and raloxifene) were selected for dose-response characterization, in vitro enkephalin release, in vivo analgesic potency, and in silico analysis...Molecular docking provided additional insight into the active site interactions of these scaffolds, which could be exploited further for creation of more potent inhibitors. These results showcase the potential of central ACE inhibitors to modulate endogenous MERF signaling."

Journal • Pain • PENK

Intelligence modeling of solubility of raloxifene and density of solvent for green supercritical processing of medicines for enhanced solubility. (PubMed, Sci Rep) - "Hence, the GPR model is recommended for accurate solubility predictions of raloxifene. Overall, the GPR model consistently demonstrated excellent predictive performance for both CO2 density and solubility, making it the preferred choice for modeling these relationships."

Journal

Solubility enhancement of raloxifene hydrochloride by in situ micronization technique: physicochemical characterization and pharmacokinetic studies. (PubMed, Drug Dev Ind Pharm) - "The AUC0-24 was also inclined about four times more in nanoparticles compared to the pure drug while Tmax was the same in both groups. The obtained results demonstrated in situ micronization technique by solvent change method was successful in improving RH bioavailability."

Journal • PK/PD data • Osteoporosis • Rheumatology