raloxifene hydrochloride / Generic mfg. - LARVOL DELTA

Raloxifene injections normalize age-related mechanical sensitization in female and male mice and augment intervertebral disc structure in old female mice. (PubMed, Osteoarthritis Cartilage) - "Raloxifene injections significantly reduced IVDD in female mice and reduced mechanical sensitivity to evoked mechanical pain in both male and female mice, suggesting that raloxifene may serve as a therapeutic for painful age-related IVDD."

Journal • Preclinical • Back Pain • Lumbar Back Pain • Musculoskeletal Pain • Osteoporosis • Pain • Rheumatology

MemoryRT: Memantine +/- Raloxifene for Cognitive Preservation After Radiation Therapy to the Brain (clinicaltrials.gov) - P2 | N=108 | Not yet recruiting | Sponsor: The University of Texas Health Science Center at San Antonio

New P2 trial • Brain Cancer • Oncology • Solid Tumor

Sex-informed estrogen receptor modulation in schizophrenia: a male-focused ERβ/GPER1 framework for cognitive and negative symptoms. (PubMed, Front Psychiatry) - "This review synthesizes evidence supporting selective estrogen receptor modulators (SERMs), with an emphasis on raloxifene, as adjunctive agents capable of engaging central estrogenic pathways without feminizing systemic effects...Finally, emerging innovations-including GPER1-biased ligands, tissue-selective estrogen complexes, and nanoparticle delivery systems-are discussed as strategies to optimize central nervous system targeting while minimizing peripheral risk. Together, these insights position receptor-selective estrogenic modulation as a mechanistically grounded and clinically relevant approach for improving cognitive and negative symptom outcomes in TRS."

Journal • CNS Disorders • Psychiatry • Schizophrenia • CYP19A1 • GPER1

Identification and validation of paraptosis-related prognostic biomarkers in lung adenocarcinoma: An observational study based on transcriptomics and clinical outcomes. (PubMed, Medicine (Baltimore)) - "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."

Biomarker • Clinical data • Journal • Observational data • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • CDK3 • CDKN3 • PEBP1 • TNFRSF19 • TNFRSF9

The Effect of SERM/CB2 Receptor Modulators on Repetitive Behaviours in Juvenile and Young Adult Mice May Have Implications for Tourette Syndrome Treatment. (PubMed, Int J Mol Sci) - "DOI-induced juvenile male and female mice responded to raloxifene, while only adolescent DOI-induced females responded to raloxifene. These results suggest that SERM drugs that are also CB2 receptor antagonists/inverse-agonists may be a new class of drugs to reduce motor tics and OCD symptoms in patients with TS/OCD."

Journal • Preclinical • CNS Disorders • Developmental Disorders • Mood Disorders • Movement Disorders • Obsessive-Compulsive Disorder • Psychiatry • Tic Disorders • Tourette Syndrome

Cell-Type-Specific Causal Inference Unveils Novel Targets for Parkinson's Disease. (PubMed, Mov Disord) - "This study contributed to cell-type-specific genetic mechanisms in PD, linking risk variants to molecular alterations and nominating therapeutic targets."

Journal • CNS Disorders • Movement Disorders • Parkinson's Disease • ARL17A • KANSL1

Treatment of ER-positive breast cancer with FDA-approved aromatase inhibitors. (PubMed, Cancer Treat Res Commun) - "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."

FDA event • Journal • Review • Breast Cancer • Estrogen Receptor Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • ER

Combined Nanoparticle-Based Delivery of Estrogens and Raloxifen in Postmenopausal Osteoporosis. (PubMed, Nanomaterials (Basel)) - "Pharmacotherapy uses, among others, 17beta-estradiol (E2), which has been replaced in recent years by raloxifene hydrochloride (RLX)...However, these findings are based on preclinical models and require further validation in clinical studies. The analysis concludes that while NP systems significantly enhance the pharmacokinetic profile and safety of E2 and RLX in preclinical models, claims of true bone-specific targeting remain largely unsubstantiated, highlighting a key area for future research."

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

Antiosteoporotic treatment promotes tendon-to-bone healing after rotator cuff repair : a systematic review of animal studies. (PubMed, Bone Joint Res) - "Bisphosphonates (n = 5), parathyroid hormone (PTH) (n = 8), growth factors (n = 3), raloxifene (n = 1), denosumab (n = 1), and sclerostin antibody (n = 1) were applied as interventions. The current study had high heterogeneity and major methodological flaws in the included studies, which limit the scope of these conclusions. However, based on histological, radiological, biomechanical, muscle quality, and serum biochemical analyses, antiosteoporosis treatments may be considered to enhance tendon-to-bone healing after RCR."

Journal • Review • Rheumatology

Effectiveness of romosozumab following prior raloxifene treatment in primary osteoporosis: An observational study. (PubMed, Bone Rep) - "We did not detect significant differences in the changes in BTMs according to whether there was previous treatment with raloxifene. Prior raloxifene treatment may be well tolerated and may not affect increases in BMD, changes in BTMs, and fracture prevention in romosozumab therapy."

Journal • Observational data • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Adherence to Endocrine Prevention in Patients with Atypical Hyperplasia and Lobular Carcinoma In Situ: Promising Trends from Real-World Use of Low-Dose Tamoxifen. (PubMed, Ann Surg Oncol) - "Adherence to endocrine prevention is high in women who initiate medication, with few discontinuing due to side effects."

Journal • Real-world evidence • Oncology • Solid Tumor

HSD17B7 Counters Bone Loss in Estrogen Deficiency via Estrogen Receptor Stabilization and Mediates the Effect of Raloxifene. (PubMed, MedComm (2020)) - "Finally, raloxifene, which boosts ERα, did not inhibit bone loss without HSD17B7, confirming the modulation of ERα through HSD17B7. Therefore, HSD17B7 regulation is a novel therapeutic approach for alleviating estrogen-deficient osteoporosis."

Journal • Osteoporosis • Rheumatology • Targeted Protein Degradation • ER

Pharmacotherapeutic considerations of selective estrogen receptor modulators for vascular protection. (PubMed, Front Pharmacol) - "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."

Journal • Review • Cardiovascular • Oncology • Venous Thromboembolism • CYP3A4 • NOS3

The effect of estradiol and selective estrogen receptor modulators on lipid profile in the ovariectomized rat model. (PubMed, Res Pharm Sci) - "Then, the animals were subjected to receive SERMs including tamoxifen (TAM), raloxifene (RAL), and bazedoxifene (BZA) and E2. The HDL2 subfraction was found to be significantly enhanced in TAM, RAL, and BZA/CE therapy. The therapy with SERMs, alone or in combination with E2, may be efficiently utilized instead of E2 replacement therapy in post-menopausal conditions."

Journal • Preclinical • Cardiovascular • Diabetes • Dyslipidemia • Metabolic Disorders

Genomic and AI-Driven Discovery in Chronic Prostatitis: Causal Role of ITPR3 and Therapeutic Repurposing of Raloxifene. (PubMed, Eur J Pharmacol) - "ITPR3 is a novel therapeutic target for chronic prostatitis, and the computational repurposing of raloxifene as its inhibitor warrants further experimental investigation. These findings provide new insights for developing clinical interventions in chronic prostatitis."

Journal • SMAD7 • TGFB1

Effects of estradiol, tamoxifen, and raloxifene on human temporal lobe cortex astroglial cell spreading. (PubMed, Gynecol Endocrinol) - "Estradiol, tamoxifen, and raloxifene - widely used hormonal agents - were associated with distinct effects on astrocyte morphology in human cortical tissue. These findings support a role for estrogen receptor modulation in astroglial structural regulation and suggest a potential cellular mechanism contributing to central nervous system symptoms reported in clinical settings."

Journal • GFAP

In silico evaluation of procyanidin as a potential ESR1 inhibitor: docking and MD insights in uterine fibroids and endometriosis. (PubMed, In Silico Pharmacol) - "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."

Journal • Endometriosis • Gynecology • Solid Tumor • Uterine Leiomyoma • Women's Health • ER

Alternative Osteoporosis Therapies After Bisphosphonate Associated Atypical Femur Fractures: A Retrospective Analysis. (PubMed, Geriatr Orthop Surg Rehabil) - "Current expert guidelines recommend discontinuing bisphosphonates and initiating alternative anti-fracture therapies (AFT), such as denosumab, teriparatide, or raloxifene, following an AFF to support skeletal health and reduce future fracture risk. Despite expert recommendations, AFT was initiated in only a small percentage of patients following AFFs. These findings highlight a significant care gap in secondary fracture prevention and underscore the need for a multidisciplinary approach, including coordination between endocrinology, orthopaedics, and primary care, to improve adherence to post-fracture osteoporosis management guidelines."

Journal • Retrospective data • Endocrine Disorders • Geriatric Disorders • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

In vitro assessment of injectable alginate-based scaffolds functionalized with osteotropic drug-loaded bioactive glass. (PubMed, Biomed Mater) - "Here, we developed injectable sodium alginate hydrogels (HP) incorporating 45S5 bioactive glass (HB) or the same glass functionalized with two osteoporosis-relevant osteotropic drugs deliberately selected for distinct mechanisms of action: raloxifene hydrochloride (HBRx; selective estrogen receptor modulation) and strontium ranelate (HBSr; dual action on bone remodeling)...Collectively, these findings indicate that osteoporosis-relevant drug-functionalized 45S5 within injectable alginate hydrogels provides a quantitative route to tune microstructure and interfacial behavior while preserving cytocompatibility and osteogenic potential. Future work will prioritize in vivo validation in osteoporotic models to assess bone repair efficacy and determine whether localized delivery mitigates drug-specific drawbacks associated with systemic therapies."

Journal • Preclinical • Osteoporosis • Rheumatology

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

Effectiveness of treatments to prevent femoral periprosthetic bone loss following total hip arthroplasty: a network meta-analysis. (PubMed, Front Pharmacol) - "At 6 months, alendronate, alendronate + alfacalcidol, denosumab, ibandronate, raloxifene, teriparatide + alendronate, and zoledronic acid were beneficial in increasing BMD, with denosumab ranking highest (based on surface under the cumulative ranking curve (SUCRA) values). At 12 months, alendronate, alendronate + alfacalcidol, denosumab, ibandronate, risedronate, and zoledronic acid showed benefits, with alendronate + alfacalcidol ranking highest (SUCRA = 0.97)...Analysis of BMD at 5-10 years, involving four studies on alendronate, pamidronate, and placebo, indicated that alendronate achieved the highest SUCRA value (0.87)...Denosumab was the most efficient agent for increasing BMD at 6 months post-THA, while alendronate combined with alfacalcidol or feriparatide was most efficient at 12 months and 24 months. More high-quality direct comparisons and long-term follow-up studies are needed to determine the optimal drug and dosage for THA..."

Journal • Retrospective data • Orthopedics • Osteoporosis • Rheumatology

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

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