doxercalciferol / Generic mfg. - LARVOL DELTA

Inhibition of WAC alleviates the chondrocyte proinflammatory secretory phenotype and cartilage degradation via H2BK120ub1 and H3K27me3 coregulation. (PubMed, Acta Pharm Sin B) - "Through molecular docking and dynamic simulation, doxercalciferol was found to inhibit WAC and the development of cartilage degradation in the CIA and CIOA models. Our study demonstrated that WAC is a key factor of cartilage degradation in arthritis, and targeting WAC by doxercalciferol could be a viable therapeutic strategy for treating cartilage destruction in several types of arthritis."

Journal • Immunology • Inflammation • Osteoarthritis • Pain • Rheumatoid Arthritis • Rheumatology • KDM6B

Safety and Efficacy of Hectorol in Pediatric Patients With Chronic Kidney Disease Stage 3 and 4 With Secondary Hyperparathyroidism Not Yet on Dialysis (clinicaltrials.gov) - P3 | N=21 | Terminated | Sponsor: Sanofi | N=84 ➔ 21 | Trial completion date: Nov 2025 ➔ Jun 2025 | Active, not recruiting ➔ Terminated | Trial primary completion date: Nov 2025 ➔ Jun 2025; The study was conducted to fulfill a post-marketing commitment (PMC).FDA acknowledged the fulfillment of this PMC.

Enrollment change • Trial completion date • Trial primary completion date • Trial termination • Chronic Kidney Disease • Endocrine Disorders • Nephrology • Pediatrics • Renal Disease • Secondary Hyperparathyroidism

Repurposing Acebutolol for Osteoporosis Treatment: Insights From Multi-Omics and Multi-Modal Data Analysis. (PubMed, Clin Pharmacol Ther) - "Our findings indicate four drugs, including Ruxolitinib, Alfacalcidol, and Doxercalciferol, may exert anti-osteoporosis effects. In summary, this study integrates multi-omics approaches, experimental validation, and real-world population data to propose acebutolol as a novel candidate for osteoporosis treatment. These findings warrant further mechanistic studies and clinical trials to evaluate its efficacy in osteoporosis management."

Journal • Cardiovascular • Hypertension • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Efficacy and safety of intermittent intravenous doxercalciferol in the treatment of secondary hyperparathyroidism in Chinese patients on maintenance hemodialysis: a phase II, open-label, prospective, multicenter study. (PubMed, Front Pharmacol) - P=N/A | "This study supports doxercalciferol as a potential treatment option for SHPT in Chinese MHD patients. Clinical Trial Registration: https://www.chictr.org.cn/showproj.html?proj=187332, identifier ChiCTR2300073196."

Clinical • Journal • P2 data • Endocrine Disorders • Metabolic Disorders • Secondary Hyperparathyroidism

Utilising Human Myometrial and Uterine Fibroid Stem Cell-Derived Three Dimentional Organoids as a Robust Model System for Understanding the Pathophysiology of Uterine Fibroids. (PubMed, Cell Prolif) - "Additionally, our research demonstrated significant decreases in fibrotic markers upon treatment with Vitamin D3 and Doxercalciferol. Furthermore, the pro-fibroid effects of environmental phthalates further elucidate the potential factors contributing to UF pathology. The 3D organoid model can serve as a robust platform to study the underlying molecular mechanisms of UFs, besides offering invaluable insights for potential therapeutic interventions."

Journal • Fibrosis • Gynecologic Cancers • Gynecology • Oncology • Solid Tumor • Uterine Leiomyoma • Women's Health • ER • FN1

Minimal Impact on MBD Markers Following Transition from Intravenous to Oral Vitamin D Therapy (NKF-SCM 2025) - "The average dose of active Vitamin D prior to transition was 3.74 mcg IV doxercalciferol /treatment and 0.98 mcg oral calcitriol / treatment at 6 months post-transition. A conversion factor of 4 mcg IV doxercalciferol to 1 mcg oral calcitriol was used by ordering prescribers indicating that there was minimal change in the patients' average active Vitamin D dose between the 2 forms.Conclusion The transition to oral Vitamin D in a large ICHD population was implemented quickly without negative impact on MBD outcomes."

Adjunctive active vitamin D (AVD) decreases kidney function during treatment of secondary hyperparathyroidism (SHPT) with extended-release calcifediol (ERC) in non-dialysis chronic kidney disease (ND-CKD). (PubMed, Am J Nephrol) - "Adj AVD at these doses enabled 35% more iPTH reduction in ND-CKD patients with mild to moderate SHPT on long-term ERC treatment but increased mean serum Ca and P by 0.40 and 0.27 mg/dL, respectively, FGF23 by more than 2-fold and eGFR decline by 4-fold, suggesting that adding AVD to ERC has untoward effects that override the nephrosparing impact of iPTH reductions with ERC treatment alone. Corroboration is warranted with a larger, longer RCT."

Journal • Chronic Kidney Disease • Endocrine Disorders • Nephrology • Renal Disease • Secondary Hyperparathyroidism • FGF23

DeepDrug as an expert guided and AI driven drug repurposing methodology for selecting the lead combination of drugs for Alzheimer's disease. (PubMed, Sci Rep) - "A five-drug lead combination, consisting of Tofacitinib, Niraparib, Baricitinib, Empagliflozin, and Doxercalciferol, has been selected from the top drug candidates based on DeepDrug scores to achieve the maximum synergistic effect. These five drugs target neuroinflammation, mitochondrial dysfunction, and glucose metabolism, which are all related to AD pathology. DeepDrug offers a novel AI-and-big-data, expert-guided mechanism for new drug combination discovery and drug-repurposing across AD and other neuro-degenerative diseases, with immediate clinical applications."

IO biomarker • Journal • Alzheimer's Disease • CNS Disorders • Inflammation • Metabolic Disorders

Impact of Adjunctive Active Vitamin D on Kidney Function during Treatment of Secondary Hyperparathyroidism (SHPT) with Extended-Release Calcifediol (ERC) in Nondialysis-Dependent CKD (ND-CKD) (KIDNEY WEEK 2024) - "They were randomized to continuing daily ERC (60 mcg) with (n=40) or without (n=38) immediate-release adjunctive daily oral calcitriol (0.25 mcg; n=12), doxercalciferol (0.5 mcg; n=14) or paricalcitol (1.0 mcg; n=14) for 14 weeks. Although adjunctive active vitamin D enabled more iPTH reduction (35%) in CKD patients taking ERC for 52 weeks, it increased serum Ca by 0.5 mg/dL, FGF23 by 136% and hastened eGFR decline by 10%. Higher doses of ERC alone may be more suitable for improving iPTH control and eGFR stabilization in obese patients."

Late-breaking abstract • Chronic Kidney Disease • Endocrine Disorders • Genetic Disorders • Nephrology • Obesity • Secondary Hyperparathyroidism • FGF23

Antiviral activity of vitamin D derivatives against severe fever with thrombocytopenia syndrome virus in vitro and in vivo. (PubMed, Virol Sin) - "Subsequently, in vivo studies revealed that doxercalciferol and alfacalcidol were associated with increased survival and reduced viral RNA load in the blood. The combination of alfacalcidol and T-705 significantly enhanced the therapeutic effects in mice. This study highlights the potential of vitamin D derivatives against SFTSV and suggests that they may have synergistic effects with other compounds used in the treatment of SFTSV infection."

Journal • Preclinical • Hematological Disorders • Infectious Disease • Thrombocytopenia

Decoding cardiovascular risks: analyzing type 2 diabetes mellitus and ASCVD gene expression. (PubMed, Front Endocrinol (Lausanne)) - "Notably, RITA, ON-01910, doxercalciferol, and topiramate emerged as potential therapeutic agents for both T2DM and ASCVD, indicating their possible clinical significance. Our findings pinpoint ABCC5 and WDR7 as new target genes between T2DM and ASCVD, with RITA, ON-01910, doxercalciferol, and topiramate highlighted as promising therapeutic agents."

Journal • Atherosclerosis • Cardiovascular • Diabetes • Dyslipidemia • Metabolic Disorders • Type 2 Diabetes Mellitus • ABCC5

The antimicrobial effect of different vitamin D compounds on Streptococcus mutans and their impact on glycosyltransferase expression. (PubMed, J Oral Microbiol) - "This in vitro study aimed to investigate the antimicrobial effects of Cholecalciferol (D3) and Doxercalciferol (D2), against S. mutans and on glycosyltransferase gene expression...Vitamin D2 and D3 inhibited S. mutans mediated pH drop in sucrose supplemented cultures and altered glycosyltransferase expression, suggesting potential therapeutic roles in dental caries prevention. Further research is needed to assess their full impact on S. mutans survival under environmental stresses."

Journal • Dental Disorders

Targeting Sirtuin 1 for therapeutic potential: Drug repurposing approach integrating docking and molecular dynamics simulations. (PubMed, PLoS One) - "The MD simulations illustrated that the SIRT1-Doxercalciferol and SIRT1-Timiperone complexes maintain stability over a 500 ns trajectory. These insightful outcomes propose that Doxercalciferol and Timiperone hold promise as viable scaffolds for developing potential SIRT1 inhibitors, with implications for tackling complex diseases such as cancer, neurodegenerative disorders, and metabolic syndromes."

Journal • CNS Disorders • Metabolic Disorders • Oncology • SIRT1

Doxercalciferol alleviates UVB-induced HaCaT cell senescence and skin photoaging. (PubMed, Int Immunopharmacol) - "Furthermore, Dox inhibited UVB-induced skin photoaging and damage in mice. In summary, Dox has been improved to inhibit photoaging, which may help to develop therapies to delay skin photoaging."

Journal • Cardiovascular • Endocrine Disorders • Inflammation • Nephrology • Renal Disease • CDKN1A • IL1B • IL6 • MMP1 • MMP9

Interactome-Based Machine Learning Predicts Potential Therapeutics for COVID-19. (PubMed, ACS Omega) - "Such predictions are carried out by random forest as it is found to perform better than other predictors, providing an accuracy of 90.53% for human-spike PPI and 96.15% for drug-protein interactions. Finally, 40 unique drugs like eicosapentaenoic acid, doxercalciferol, ciclesonide, dexamethasone, methylprednisolone, etc. are identified that target 32 human proteins like ACACA, DST, DYNC1H1, etc."

Journal • Machine learning • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Vitamin D and Its Analogues: From Differences in Molecular Mechanisms to Potential Benefits of Adapted Use in the Treatment of Alzheimer's Disease. (PubMed, Nutrients) - "Here, we discuss these aspects, especially those of the commonly used vitamin D analogues alfacalcidol, paricalcitol, doxercalciferol, tacalcitol, calcipotriol, and eldecalcitol. Furthermore, the formation of intracellular neurofibrillary tangles involving hyperphosphorylated tau proteins contributes to the pathology of AD. In conclusion, this review emphasizes the importance of an adequate vitamin D supply and discusses the specifics of administering various vitamin D analogues compared with vitamin D in geriatric patients, especially those suffering from AD."

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

Novel Medical Therapy for PCOS: VDR Agonist Induces Substantial Weight Loss and Improves Fertility in a Mouse Model. (SRI 2023) - "For in vivo study, we induced PCOS in C57/BL6 mice by letrozole (LTZ). Our study provides a compelling data for PCOS treatment using VDR agonists such as Doxercalciferol. Our study revealed that vitamin-D analogues is a promising family of compounds to reduce bodyweight, glucose level and reverse infertility in PCOS animal model by inhibiting insulin resistance and androgen production."

Preclinical • Diabetes • Genetic Disorders • Infertility • Liposarcoma • Metabolic Disorders • Obesity • Oncology • Polycystic Ovary Syndrome • Sarcoma • Sexual Disorders • Solid Tumor • CYP17A1

Doxercalciferol Decreases Uterine Fibroid Growth Rate Through the Regulation of ECM Synthesis and Cell Proliferation. (SRI 2023) - "Our results suggest that DOX reduces UF growth rate through the regulation of ECM synthesis and cell proliferation, while no deleterious effect on the ovarian reserve markers or toxic effects were observed. Based on that, DOX could be a therapeutic alternative for UF in patients aiming to preserve their fertility potential."

Gynecology • Solid Tumor • Uterine Leiomyoma • Women's Health • ADRA1B • ARG1 • DUSP1

Extended release calcifediol and paricalcitol in the treatment of secondary hyperparathyroidism: a network meta-analysis of indirect comparison (PubMed, G Ital Nefrol) - "Paricalcitol (PCT), other active vitamin D analogous (doxercalciferol and alfacalcidol), and active vitamin D (calcitriol) have been commonly used to treat SHPT in non-dialysis CKD (ND-CKD) for several years. The evidence suggests that both PCT and ERC are effective in reducing levels of PTH, whereas calcium levels tended to increase from treatment with PCT. Therefore, ERC may be an equally effective, but more tolerable treatment alternative to PCT."

Journal • Retrospective data • Review • Chronic Kidney Disease • Endocrine Disorders • Nephrology • Renal Disease • Secondary Hyperparathyroidism • FGF23

Safety and Efficacy of Hectorol in Pediatric Patients With Chronic Kidney Disease Stage 3 and 4 With Secondary Hyperparathyroidism Not Yet on Dialysis (clinicaltrials.gov) - P3 | N=84 | Active, not recruiting | Sponsor: Sanofi | Recruiting ➔ Active, not recruiting

Enrollment closed • Chronic Kidney Disease • Endocrine Disorders • Nephrology • Pediatrics • Renal Disease • Secondary Hyperparathyroidism

A case of calcific uremic arteriolopathy with severe secondary hyperparathyroidism, how high is high? (NKF-SCM 2022) - "Patient was on Cinacalcet, sevelamer, and Hectorol. CONCLUSION CUA is a life-threatening ischemic skin disease that is caused by ESRD related mineral disorders. It is essential to identify this illness early to prevent poor outcomes."

Clinical • Calciphylaxis • Cardiovascular • Chronic Kidney Disease • Dermatology • Endocrine Disorders • Hematological Disorders • Infectious Disease • Myocardial Infarction • Nephrology • Pain • Rare Diseases • Renal Disease • Secondary Hyperparathyroidism • Septic Shock • Thrombosis

Integration of lipidomics and metabolomics for the authentication of camellia oil by ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry coupled with chemometrics. (PubMed, Food Chem) - "Lariciresinol, sinapic acid, doxercalciferol, and an unknown compound were identified as markers for rapeseed oil...The established OPLS-DA and OPLS prediction models were highly accurate in the qualitative and quantitative analyses of camellia oil adulterated with 5% other oils. These results indicate that the integration of lipidomics and metabolomics approaches has great potential for the authentication of edible oils."

Journal

[VIRTUAL] A Case of Severe Penile Pain (KIDNEY WEEK 2021) - "Since starting HD 1 year prior, his serum phosphorous ranged 7.8-9.0mg/dL, Ca 8.0-9.0mg/dL and parathyroid hormone downtrended from 611 to 127pg/mL on hectorol, phoslo and Ca carbonate...Treatment goals included phosphate normalization by 4 weekly HD sessions, low Ca dialysate, non Ca based phosphate binders; vasodilators sildenafil and pentoxifylline, and sodium thiosulphate (blocks calcification of smooth muscle cells). He is in a clinical trial for SNF472, a selective calcification inhibitor, for wound healing and pain management...It is essential that we identify penile calciphylaxis, given its significant morbidity and mortality. Penile calciphylaxis"

Clinical • Atherosclerosis • Calciphylaxis • Cardiovascular • Chronic Kidney Disease • Dermatology • Diabetes • Diabetic Nephropathy • Dyslipidemia • Endocrine Disorders • Hematological Disorders • Infectious Disease • Metabolic Disorders • Nephrology • Pain • Peripheral Arterial Disease • Rare Diseases • Renal Disease • Secondary Hyperparathyroidism • Thrombosis • Transplantation • Urology

[VIRTUAL] A Missing Key or Faulty Lock: Use of an Alternative Vitamin D Analog Opens the Door to Success (KIDNEY WEEK 2021) - "Doxercalciferol requires 25-hydroxylation by the liver, a step preserved in end-stage kidney disease (ESKD), but may be subject to genetic polymorphisms that determine responsiveness...We recommend switching vitamin D analogs and consider genetic testing. Characterizing vitamin D receptor protein polymorphisms may influence prescribing practices of vitamin D analogs in the future."

Chronic Kidney Disease • Diabetes • Diabetic Nephropathy • Endocrine Disorders • Metabolic Disorders • Nephrology • Renal Disease • Secondary Hyperparathyroidism • FGF23

Safety and Efficacy of Hectorol in Pediatric Patients With Chronic Kidney Disease Stage 3 and 4 With Secondary Hyperparathyroidism Not Yet on Dialysis (clinicaltrials.gov) - P3; N=84; Recruiting; Sponsor: Sanofi; Trial completion date: Apr 2022 ➔ Nov 2025; Trial primary completion date: Apr 2022 ➔ Nov 2025

Clinical • Trial completion date • Trial primary completion date • Chronic Kidney Disease • Endocrine Disorders • Nephrology • Pediatrics • Renal Disease • Secondary Hyperparathyroidism