raloxifene hydrochloride / Generic mfg. - LARVOL DELTA

Raloxifene and progesterone neuroprotection in a female mouse model of Parkinson's disease. (PubMed, Front Neurosci) - "Striatal glial fibrillary acidic protein (GFAP), an astrogliosis marker, levels were elevated in MPTP-lesioned mice and this was similarly prevented with the hormonal treatment alone or in combination. Raloxifene and progesterone treatment was neuroprotective without excessive uterine stimulation in OVX mice supporting repurposing of these drugs for PD and their high translational value."

Journal • Preclinical • CNS Disorders • Movement Disorders • Parkinson's Disease • GFAP

Advances in Machine Learning for Drug Repurposing: From Methodologies to Precision Medicine with Case Studies in COVID-19, Parkinson's Disease, and Cancer. (PubMed, IEEE J Biomed Health Inform) - "Case studies demonstrate how integrated models leveraging heterogeneous data (e.g., gene expression, chemical structure, EHRs) facilitated the identification of repurposable candidates like baricitinib, raloxifene, and rapamycin. We examine the role of foundation models and large language models (LLMs) in drug repurposing, including zero-shot molecular property prediction and literature-informed mining. This work outlines an ML-driven framework that balances computational scalability with biological validity, enabling actionable predictions in precision medicine."

Journal • CNS Disorders • Infectious Disease • Movement Disorders • Novel Coronavirus Disease • Oncology • Parkinson's Disease

MemoryRT: Memantine +/- Raloxifene for Cognitive Preservation After Radiation Therapy to the Brain (clinicaltrials.gov) - P2 | N=108 | Recruiting | Sponsor: The University of Texas Health Science Center at San Antonio | Not yet recruiting ➔ Recruiting | Trial completion date: Mar 2031 ➔ Jul 2031 | Initiation date: Mar 2026 ➔ Jul 2026 | Trial primary completion date: Mar 2030 ➔ Jul 2030

Enrollment open • Trial completion date • Trial initiation date • Trial primary completion date • Brain Cancer • Oncology • Solid Tumor

Sex differences and sex-dependent effects of maternal immune activation and raloxifene on neurotransmitter gene expression in the adult rat dorsal striatum. (PubMed, Prog Neuropsychopharmacol Biol Psychiatry) - "We identified significant sex differences in dSTR molecular profiles relating to dopaminergic activity, astrocyte activity and inhibitory interneuron markers, and sex-dependent molecular consequences of MIA and raloxifene treatment on dopaminergic-related gene and protein expression and of MIA on astrocytic GABA synthesis enzyme transcripts. This study highlights the importance of sex as a biological variable and identifies candidate molecular pathways through which prenatal immune insult and estrogen receptor modulation may influence vulnerability and treatment response in neurodevelopmental disorders."

Journal • Preclinical • CNS Disorders • Developmental Disorders • Psychiatry • Schizophrenia

Estrogen signaling and ferroptosis in intervertebral disc degeneration: A proposed mechanistic framework and its evidence gaps. (PubMed, Tissue Cell) - "Estrogen replacement and the selective estrogen receptor modulator raloxifene preserve disc structure in ovariectomized and aging rodent models, and ferrostatin-1 and iron chelation are independently protective in disc models; no study has combined the two approaches, and receptor selection remains unsettled, since the one directly demonstrated estrogen-ferroptosis mechanism operates through GPER rather than the nuclear receptors targeted by available modulators. This review therefore presents the estrogen-ferroptosis intersection as a biologically coherent hypothesis rather than an established mechanism, specifies the minimum experiment that would test it, and identifies the evidence gaps that currently prevent its translation."

Journal • Review • Acute Kidney Injury • Back Pain • Fibrosis • Lumbar Back Pain • Musculoskeletal Pain • Nephrology • Oncology • Pain • Renal Disease • ACSL4 • GPX4 • SLC7A11

Improvement of Bone Healing by Combined Treatment with Selective Androgen and Estrogen Receptor Modulators in Female and Male Rats. (PubMed, Calcif Tissue Int) - "This study examined whether bone healing could be improved by combined treatment with the selective androgen and estrogen receptor modulators ostarine (Ost) and raloxifene (Ral), and compared its efficacy with monotherapy in female and male rat models. The combination with Ral reduced the androgenic effect of Ost on prostate. Combined treatment may represent a promising approach for osteoporotic bone repair in both sexes, though potential side effects of Ost require consideration."

Journal • Preclinical • Orthopedics • Osteoporosis

Interactive effects of mechanical loading and raloxifene in a murine model of diabetic kidney disease (ASBMR 2026) - No abstract available

Late-breaking abstract • Preclinical • Chronic Kidney Disease • Diabetic Nephropathy • Nephrology • Renal Disease

Alendronate-induced morphological changes in osteoclasts and eroded pores during cortical bone remodeling in lactating Sprague Dawley rats. (PubMed, Bone) - "Bisphosphonates (BPs) are widely used to treat bone complications, yet their impact on the coupling between resorption and formation during cortical bone remodeling remains incompletely understood. Raloxifene was associated with minimal differences on early remodeling events. Together, these findings support the interpretation that short-term bisphosphonate treatment is associated with early alterations in cortical remodeling dynamics under high-turnover conditions and highlight the importance of site-specific evaluation within defined physiological remodeling contexts."

Journal • Preclinical

Validating raloxifene-mediated restoration of DNMT-TET epigenetic balance in breast and lung cancer. (PubMed, Cancer Treat Res Commun) - "Together, our data represent a molecular signature for breast and lung tumorigenesis, the DNMT-TET disequilibrium, and place raloxifene in a dual SERM-epigenetic context. These results support the concept of precision oncology in which reversible, locus-directed methylation changes are combined with endocrine modulation to target hormone-responsive and epigenetically biased cancers."

Journal • Breast Cancer • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • BRCA • DNMT1 • TET2

Raloxifene suppresses growth and promotes intrinsic apoptotic signaling in C6 glioma cells. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "Our findings show that RAL significantly induces apoptosis and suppresses cell growth in a concentration- and time-dependent pattern compared to the vehicle control (0.1% DMSO). These findings would position RAL as a promising candidate for GBM therapy, warranting further investigation into its translational potential."

Journal • Brain Cancer • Glioblastoma • Glioma • Oncology • Solid Tumor

Crosstalk between estrogen signaling and Fas-mediated apoptosis determines neuronal resilience after menopause. (PubMed, Exp Eye Res) - "However, combined treatment with the selective estrogen receptor modulator Raloxifene and the Fas receptor antagonist KP7-6 produced a powerful synergistic effect, limiting RGC somatic loss to a mere 18% and restoring stratified retinal function to near-physiological levels in both ovariectomized and non-ovariectomized animals...These findings identify endocrine aging as a modifiable driver of neuronal vulnerability and demonstrate that simultaneous targeting of estrogen-dependent survival signaling, and Fas-mediated apoptosis can restore a youthful neuroprotective phenotype. Our results establish convergent hormonal and apoptotic pathways as one of regulators of neuronal resilience during aging and suggest a combinatorial therapeutic strategy for age-related neurodegenerative disorders."

Journal • Cardiovascular • CNS Disorders • Reperfusion Injury

Oestrogen modulators as augmentation to antipsychotics for the treatment of post- and perimenopausal psychosis: a systematic review. (PubMed, Ther Adv Psychopharmacol) - "Raloxifene shows potential as an adjunctive treatment in post- and perimenopausal psychosis, but further high-quality clinical trials are needed to inform practice and develop hormone-informed treatment protocols. Not registered."

Journal • Review • CNS Disorders • Psychiatry • Schizophrenia

Genetic pleiotropy differentially linking brain variation to cannabis use and cannabis use disorder. (PubMed, Neuropsychopharmacology) - "Applying gene2drug framework, our drug-repurposing analyses identified nine molecular compounds, also including raloxifene (a cannabinoid-receptor 2 inverse agonist) and albendazole (reported to interact with cannabis smoking). Overall, these findings provide new insights into the neurobiological pathways underlying CU and its progression to CUD."

Journal • Inflammation • Psychiatry • Substance Abuse

Using Deep Learning Models of Gene Regulation to Guide Drug Prioritization. (PubMed, Pharmaceuticals (Basel)) - "TF-based prioritization, integrating FOXA1 knockdown-induced and drug-induced gene expression profiles, identified 63 candidate compounds, including 18 approved drugs, and recovered fulvestrant, an established breast cancer therapy. Gene-based prioritization, mapping candidate regulatory variants to 347 target genes, identified 140 candidate compounds, including approved breast cancer drugs toremifene and raloxifene... Recovery of approved breast cancer therapeutics supports the biological relevance of deep learning-predicted regulatory variants. This study establishes a regulatory variant-guided drug repurposing framework that connects noncoding genetic variation to candidate therapeutics and provides a scalable strategy for generating pharmacologically relevant hypotheses from the noncoding genome."

Journal • Breast Cancer • Gene Therapies • Oncology • Solid Tumor • FOXA1

Romosozumab Treatment After Parathyroidectomy for Primary Hyperparathyroidism-Complicated Osteoporosis: A Two-Case Report. (PubMed, AACE Endocrinol Diabetes) - "Parathyroidectomy increases bone mineral density (BMD) by 3% to 4% in patients with primary hyperparathyroidism (PHPT); however, limited studies have demonstrated the effect of postoperative medical therapy, particularly with bisphosphonate and denosumab, on BMD...After parathyroidectomy and 5-year treatment with eldecalcitol and raloxifene, T-scores were -3.3 and -5.6 in the LS and DR, respectively...These cases suggest that postoperative romosozumab therapy may be a potential therapeutic option in patients with PHPT and osteoporosis. Romosozumab may be a promising postoperative therapy for patients with PHPT and osteoporosis."

Journal • Endocrine Disorders • Metabolic Disorders • Osteoporosis • Rheumatology

In silico investigations of inhibition capabilities of selective estrogen receptor modulators against estrogen receptor - α (ER-α) in breast cancer. (PubMed, J Mol Graph Model) - "This comprehensive study presents a comparative evaluation of three prominent selective estrogen receptor modulators (SERMs), including two benzothiophene-derived compounds, Raloxifene and Arzoxifene, and one tetrahydronaphthalene-based molecule, Lasofoxifene, using an integrated computational approach. A combined evaluation of docking scores, stability parameters, and energetic profiles consistently identifies Lasofoxifene as forming the most stable complex with ER-α among the investigated ligands. So, the investigations provide a molecular-level understanding of ER-α inhibition and highlight Lasofoxifene as a promising candidate with strong inhibitory potential."

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

Dietary and supplemental calcium intake and bone changes during antiresorptive osteoporosis treatment in older women: a longitudinal observational study. (PubMed, Osteoporos Int) - "In calcium-replete older women, protein intake rather than CaS influences total hip bone changes with OM. These findings question routine CaS in women with adequate calcium intake and emphasize the importance of sufficient protein intake for optimal osteoporosis management."

Journal • Observational data • Osteoporosis • Rheumatology

Histoprotective and antiproliferative effects of Raloxifene treatment during prostate carcinogenesis in rats. (PubMed, Toxicol Appl Pharmacol) - "Additionally, the periacinar smooth muscle layer and the stromal distribution of collagen fibers were preserved in Raloxifene group. These results pointed to a protective role of Raloxifene on the prostatic microenvironment, attenuating the structural and proliferative alterations that accumulate during the carcinogenic process."

Journal • Preclinical • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • ER

Post-Marketing Ocular Adverse Events Associated with Tamoxifen and Raloxifene: A Population-Based Pharmacovigilance Study. (PubMed, Retina) - "Tamoxifen and raloxifene had unique ocular AE profiles. Tamoxifen was primarily linked to retinal, optic nerve, and corneal disorders, whereas raloxifene was strongly associated with retinal vascular and thromboembolic events. These findings underscore the importance of clinician awareness and future prospective studies to further elucidate the risks."

Adverse events • Journal • P4 data • Age-related Macular Degeneration • Breast Cancer • Cardiovascular • Cataract • Glaucoma • Hematological Disorders • Hormone Receptor Breast Cancer • Macular Degeneration • Ocular Inflammation • Oncology • Ophthalmology • Optic Neuritis • Pain • Retinal Disorders • Retinal Vein Occlusion • Rheumatology • Solid Tumor • Thrombosis • Transplant Rejection • Transplantation

Multi-omics integration and in vitro validation identify IL4R, IMPA2, and PRR4 as key therapeutic targets in chronic rhinosinusitis with nasal polyps. (PubMed, Front Immunol) - "Drug prediction yielded 26 potential drugs, with molecular docking confirming strong binding of raloxifene (IL4R), luteolin (IMPA2), and metronidazole (PRR4)...This multi-omics approach identified three key genes in CRSwNP pathogenesis and their regulatory mechanisms. In vitro functional experiments further validated that modulation of these key genes can effectively protect nasal epithelial cells from inflammatory injury, providing new molecular targets and potential therapeutic drugs for CRSwNP diagnosis and treatment."

Journal • Preclinical • Chronic Rhinosinusitis With Nasal Polyps • Immunology • Inflammation • Nasal Polyps • Otorhinolaryngology • Respiratory Diseases • Sinusitis • ATP6AP2 • CD4 • GATA2 • IL4R • IL4R

Raloxifene and tamoxifen reshape the immunometabolic phenotype of TLRs-activated macrophages through AEBS inhibition and lysosomal stress. (PubMed, Biomed Pharmacother) - "Cathepsin B inhibition further enhances NRF2-target gene responses, suggesting functional crosstalk between lysosomal and NRF2-associated pathways. Overall, these findings indicate that RAL and TAM elicit an integrated immunometabolic reshaping of macrophage inflammatory phenotypes, through cholesterol-pathway remodeling and lysosomal stress, supporting SERMs as host-directed chemotherapeutic agents."

IO biomarker • Journal • Infectious Disease • Inflammation • CTSB • IL1B • IL6 • TLR2 • TLR4 • TLR7 • TNFA

Raloxifene inhibits the proliferation of pediatric acute myeloid leukemia by targeting the ANP32B gene and regulating C-MYC expression. (PubMed, Hematology) - "By targeting ANP32B, Raloxifene effectively inhibits the proliferation of AML cells, induces cell apoptosis, and reduces the expression of C-MYC. Raloxifene may potentially serve as a candidate drug for the treatment of acute myeloid leukemia."

Journal • Acute Myelogenous Leukemia • Hematological Malignancies • Leukemia • Oncology • Pediatrics • ANP32B • MYC

Severe Treatment-Refractory Osteoporosis as the Initial Manifestation of Indolent Systemic Mastocytosis: A Case Report (ENDO 2026) - "Case Presentation: A 51-year-old Caucasian postmenopausal woman presented in 2021 with rapidly progressive osteoporosis and multiple atraumatic vertebral compression fractures (L1, L2, T10, T12, L3) on raloxifene, requiring repeated kyphoplasty...After starting intravenous zoledronic acid in 2023, her bone density declined further (femoral neck T-score −2.5 to −3.1 by 2025) with more atraumatic vertebral fractures...She remains on avapritinib, romosozumab, antihistamines as needed, an epinephrine auto-injector for emergencies, and calcium/vitamin D under multidisciplinary care with endocrinology, hematology-oncology, and allergy/immunology... ISM should be considered in patients with unexplained, severe, or treatment-resistant osteoporosis and early vertebral fractures. Absence of flushing at diagnosis, even with high tryptase, shows skeletal disease may precede mediator related symptoms. Recognizing skeletal-predominant ISM is crucial, as fracture risk remains high..."

Case report • Clinical • Endocrine Disorders • Hematological Disorders • Immunology • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology • CD2 • IL2RA

Cardiovascular Risk Associated with Romosozumab Treatment in Osteoporosis (ENDO 2026) - "Background Patients were characterized by the original studies using the Raloxifene Use for the Heart ("RUTH") cardiovascular risk scoring system...When CVE events during year one of ARCH (romosozumab vs alendronate) was compared with CVE during the 2-year follow up (romosozumab followed by alendronate vs alendronate followed by alendronate ) there was a significant RD in ischemic CVE only during the romosozumab treatment year , which was not sustained during follow-up years (RD year 1 vs year 3 = 0.006 ± 0.002, p = 0.014)...These findings support the use of baseline cardiovascular risk assessment when considering romosozumab therapy. Further analyses would be necessary to evaluate these short-term cardiovascular risks against the potential survival benefits associated with romosozumab fracture-prevention."

Cardiovascular • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Targeting Neuroendocrine Dysregulation in Schizophrenia: A Pharmacological Review (CINP 2026) - "In men, associations between gonadal hormones and schizophrenia are less well-defined.Estrogen-based treatments, including adjunctive estradiol and Selective Estrogen Receptor Modulators (SERMs) such as raloxifene, have demonstrated symptomatic improvement in postmenopausal women with schizophrenia... Neuroendocrine dysregulation contributes to the pathophysiology of schizophrenia. However, interventions targeting the adrenal and thyroid axes have shown limited efficacy. Modulation of the gonadal axis through estrogen-based therapies or SERMs appears promising, especially in women, while neurosteroids may provide additional symptom relief."

Late-breaking abstract • Review • CNS Disorders • Depression • Infectious Disease • Mental Retardation • Mood Disorders • Psychiatry • Schizophrenia