ormeloxifene / Generic mfg. - LARVOL DELTA

Targeting Breast Cancer via Dual Antagonism of Estrogen Receptor α and GPER (SABCS 2025) - "However,tamoxifen's clinical success is often compromised due to both inherent and acquired resistance.Notably, tamoxifen inhibits ERα but paradoxically acts as an agonist for GPER/GPR30, estrogenreceptor that mediates non-classical estrogen signaling in normal and cancerous cells...Mechanistically,Ormeloxifene suppresses GPER-induced calcium signaling and downstream activation of EGFR,ERK, YAP, and TAZ pathways, thereby inhibiting gene transcription and tumor growth.Additionally, metagenomic analysis of Hispanic breast cancer tissues revealed specific microbialpopulations associated with GPER expression and tumor subtypes.ConclusionsGPER is significantly overexpressed in ERα-positive and some Triple-Negative breast cancers,especially within the Hispanic population. The exclusive antagonistic activity exerted byOrmeloxifene on both ERα and GPER represents an innovative pharmacological approach fortargeting breast carcinomas expressing one or both receptors at..."

Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • ER • HER-2

Management of Severe Menorrhagia in an Adolescent with Glanzmann Thrombasthenia: A Case Report and Treatment Approach. (PubMed, J Pediatr Adolesc Gynecol) - "Treatment included blood product transfusions, tranexamic acid, and ormeloxifene administration...Long-term management involves oral contraceptives, desmopressin, and counseling on bleeding precautions...The report also discusses the rationale behind the treatment choices, including the use of ormeloxifene and cryoprecipitate, and compares the management approach to established guidelines. Additionally, it addresses the importance of genetic counseling, patient education, and ongoing research in improving outcomes for patients with GT."

Journal • Bone Marrow Transplantation • Gene Therapies • Gynecology • Hematological Disorders • Transplantation

Ormeloxifene in the treatment of mastalgia: A systematic review and meta-analysis (ESSO 2025) - "The ACG consisted of alternative medications, such as Tamoxifen, Danazol, or Gamma Linolenic Acid (GLA), used to treat mastalgia. There is no additional benefit observed after six months of treatment. The use of Ormeloxifene appears to be associated with more side effects."

Retrospective data • Review • Pain • Women's Health

Efficacy and Safety of Ormeloxifene Versus Conventional Hormonal Therapy in Women With Non-structural Abnormal Uterine Bleeding: A Systematic Review and Meta-Analysis. (PubMed, Cureus) - "Weight gain as an adverse event was observed to be significantly higher (MD=0.13, 95% CI (0.03, 0.52), p=0.004) in women using hormonal therapy, whereas amenorrhea was found more among women receiving ORM (MD=12.11, 95% CI (4.61,31.85), p=<0.00001).  The results of this study supplement the body of knowledge regarding the safety and effectiveness of ORM, although this study mostly consisted of randomized controlled trials. Further, multicenter studies with larger sample sizes are needed in the future to determine additional aspects, such as cost-effectiveness, patient satisfaction, and improvements in quality of life with ORM."

Journal • Retrospective data • Review • Gynecology • Women's Health

Centchroman and tamoxifen in mastalgia: A randomized controlled trial. (PubMed, Med J Armed Forces India) - "In the event that no symptomatic relief is observed within a one-month trial of either medication, discontinuation is recommended, as prolonged use is unlikely to yield additional relief. CTRI registration no.- CTRI/2021/01/030206."

Journal • Pain • Women's Health

Efficacy and Safety of Centchroman in the Treatment of Breast Fibroadenoma: A Systematic Review and Meta-Analysis. (PubMed, Cureus) - "With these findings of meta-analysis, we conclude that centchroman is as efficacious as the control in causing regression of fibroadenoma and centchroman has significantly higher number of adverse effects than the control, although none of the adverse effects were serious. More RCTs with larger sample size and from diverse geographical settings are needed to generate more robust evidence and to expand generalizability over a broader population."

Journal • Retrospective data • Review • Breast Cancer • Pain

Expanding contraceptive options: A scoping review of medically approved contraceptive methods that are not in the WHO Medical Eligibility Criteria. (PubMed, Contraception) - "Rigorous systematic reviews of the evidence on safety, efficacy and dosage of ormeloxifene, quinestrol-containing contraception, and mifepristone for EC are needed to inform WHO recommendations on these methods. As these methods are already being used, international guidance for practitioners is essential."

Journal • Review

Clinical outcomes among Centchroman users across six medical college hospitals in India. (PubMed, Int J Gynaecol Obstet) - "Centchroman appears to be an effective and affordable non-hormonal contraceptive option, particularly for women contraindicated for hormonal methods. However, pre-emptive counseling regarding potential menstrual side effects is crucial."

Clinical data • Journal • Infectious Disease • Novel Coronavirus Disease • Women's Health

Ormeloxifene induces mitochondrial fission-mediated pro-death autophagy in colon cancer cells. (PubMed, Biochem Biophys Res Commun) - "Inhibition of mitochondrial fission resulted in enhanced cell survival and a concomitant decrease in the autophagic markers, implying that ORM-induced autophagy depends on mitochondrial fission. Taken together, our findings bring to light a novel mechanism where Ormeloxifene targets mitochondrial dynamics to promote autophagy-associated cell death in colon cancer cells."

Journal • Breast Cancer • Colon Cancer • Colorectal Cancer • Hormone Receptor Breast Cancer • Oncology • Solid Tumor • ATG7 • BECN1

Magnitude and pattern of usage of contraception and counselling services in an urban health centre in East Delhi: A secondary data analysis. (PubMed, J Family Med Prim Care) - "condom, injectables, centchroman tablets, oral contraceptive pills and sterilization, including tubectomy and vasectomy...The study underscores the importance of counselling in shaping family planning decisions. Insights gained in this study can help healthcare providers tailor counselling approaches to better address the diverse needs of individuals and couples."

Journal

Assessment of satisfaction of using socially marketed health consumables at government settings among beneficiaries in a rural area of Hooghly District, West Bengal. (PubMed, J Family Med Prim Care) - "Ever use of government-supplied contraceptives like Chhaya (Ormeloxifene), Antara (Injectable contraceptive), emergency contraceptive pills, and intrauterine contraceptive devices (IUCD) was done by only 15.3%, 10.7%, 7.3%, 32% of eligible beneficiary households, respectively...Key informant interviews among healthcare personnel revealed avoidance of using modern contraceptive methods and frequent unavailability of some socially marketed health consumables were the predominant causes of reduced uptake of those products by beneficiaries. Proper social marketing strategies, adequate promotion, regular awareness campaigns, and tailored training of field healthcare workers are required to improve the acceptability, availability, and marketing of these health consumables."

Journal • Long-acting Reversible Contraceptives

Role of centchroman in regression of fibroadenoma: A 2-arm randomized control trial. (PubMed, Clinics (Sao Paulo)) - "Centchroman effectively reduces fibroadenoma size especially those with multiple fibroadenoma, mastalgia, and psychological distress in patients with fibroadenoma."

Journal • Breast Cancer • CNS Disorders • Depression • Mood Disorders • Oncology • Pain • Psychiatry • Women's Health

Dr. Nitya Anand: The Visionary Behind Saheli and the Advances in Medicinal Chemistry. (PubMed, Cureus) - "His innovation of Centchroman (Saheli), the world's first non-steroidal oral contraceptive pill, changes the course of contraception use in India...With over 400 publications and 130 patents, he supervised over 100 PhD students. His work has been recognized with many prestigious awards, including the Padma Shri and the National Nehru Science Award, which have left a long-lasting impact on medicinal chemistry and public health."

Journal • Review

Exosomes derived from tumor adjacent fibroblasts efficiently target pancreatic tumors. (PubMed, Acta Pharm Sin B) - "NAF-derived EXs (NAF-EXs) were used for loading ormeloxifene (ORM), a potent anti-cancer and desmoplasia inhibitor as a model drug...In conclusion, our data suggests preferential tropism of NAF-EXs for PDAC tumors, thus imply feasibility of developing a novel personalized medicine for PDAC patients using autologous NAF-EXs for improved therapeutic outcome of anti-cancer drugs. Additionally, it provides the opportunity of utilizing this biological scaffold for effective therapeutics in combination with standard therapeutic regimen."

Journal • Fibrosis • Gastrointestinal Cancer • Hepatology • Oncology • Pancreatic Cancer • Solid Tumor

Evaluation of molecular effects associated with apoptosis, tumour progression, angiogenesis and metastasis by a novel combination of drugs with ormeloxifene in triple negative breast cancer cells. (PubMed, Explor Target Antitumor Ther) - "To investigate the molecular effects of a novel combination [sertraline and plumbagin (comb) with ormeloxifene (Orm)] for anticancer activity in triple negative breast cancer cell line "MDA-MB-231". Collectively this study reveals the efficacy of Orm + comb as more significant than the clinically used tamoxifen (Tam). The study elucidates the promising novelty of the combination as a potential chemotherapeutic intervention for mitigating the aggressiveness of triple negative breast cancer and it addresses the intrinsic resistance caused by single drug treatments."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • ANXA5 • CASP3 • CDKN1A • TP53 • ZEB1

Ormeloxifene in the treatment of mastalgia: A systematic review and meta-analysis (JBCS 2024) - "Medical management including Danazol, Tamoxifen, GLA, placebo, or just observation fairs better in the management of Mastalgia in the first 12 weeks as compared to Ormeloxifene with no benefit after 6 months. Side effects appear to be more with the usage of Ormeloxifene"

Retrospective data • Review • Pain • Women's Health

SIGNIFICANCE OF EXOSOMES DERIVED FROM TUMOR ADJACENT FIBROBLASTS FOR PANCREATIC CANCER THERAPY (APCM 2024) - "NAF-derived EXs (NAF-EXs) were used for loading ormeloxifene (ORM), a potent anti-cancer and desmoplasia inhibitor as a model drug to test its efficiency in targeting pancreatic tumors... In conclusion, our data suggests preferential tropism of NAF-EXs for PDAC tumors, thus imply feasibility of developing a novel personalized medicine for PDAC patients using autologous NAF-EXs for improved therapeutic outcome. Additionally, it provides the opportunity of utilizing this biological scaffold for effective therapeutics in combination with standard therapeutic regimen."

Fibrosis • Gastrointestinal Cancer • Hepatology • Oncology • Pancreatic Cancer • Solid Tumor

A Study Comparing Centchroman and Evening Primrose Oil in the Treatment of Benign Breast Disease. (PubMed, J Pharm Bioallied Sci) - "On the basis of fibroadenoma, partial and complete response was significantly seen in higher number of cases in the centchroman group (P = .007). Centchroman therapy demonstrates that the treatment for benign breast disease is safe, effective, and economical."

Journal • Breast Cancer • Pain • Women's Health

Double blind randomized controlled trial of efficacy of ormeloxifene for the treatment of fibroadenoma (The FIBROCENT study). (PubMed, World J Surg) - "In our study Ormeloxifene was not found to be effective in treatment of fibroadenoma and had concerning side effects."

Journal • Breast Cancer

Clinical Features, Laboratory Characteristics and Outcome from Oral Contraceptives-induced Liver Injury in 43 Consecutive Patients and a Brief Review of Published Reports. (PubMed, J Clin Exp Hepatol) - "Contrastingly, literature search yielded 24 cases of progesterone DILI reported between 1962 and 2019 with no mortality. In contrast to published literature on oral contraceptives, a majority of oral contraceptive-induced DILI in our series were from progesterone monotherapy and a smaller number with ormeloxifene, that often resulted in clinically significant jaundice or liver test abnormalities and rarely in fatality."

Journal • Review • Cholestasis • Hepatology • Liver Failure

Mastalgia - The Burden Beneath. (PubMed, Eur J Breast Health) - "Reassurance, breast support and lifestyle changes are the first line treatment and have good results in a significant number of patients. In our practice topical and oral NSAIDs, evening primrose oil and vitamin E were frequently used as additional treatments to non-pharmacological methods."

Journal • Pain • Women's Health

Psychological Assessment and Treatment Effectiveness in Mastalgia: Developing a Treatment Algorithm. (PubMed, Cureus) - "Group B patients in Category iv were randomized into two groups: topical non-steroidal anti-inflammatory drugs (NSAIDs) or evening primrose oil+vitamin E. The next line of treatment was tamoxifen 10mg followed by danazol 100mg followed by ormeloxifene 30mg. Hence, it is always advisable to start such patients on topical NSAIDs, or evening primrose oil + vitamin E, before switching over (if no resolution of pain is reported with these drugs) to higher and more severe treatment options. The duration or severity of pain did not correlate with the psychological condition of the patient."

Journal • Allergy • CNS Disorders • Depression • Immunology • Pain • Psychiatry • Women's Health

Synthesis and Antitumor Activity of Brominated-Ormeloxifene (Br-ORM) against Cervical Cancer. (PubMed, ACS Omega) - "Consequently, Br-ORM treatment effectively inhibited tumor growth in an orthotopic cervical cancer xenograft mouse model along with EMT associated changes as compared to vehicle control-treated mice. Altogether, experimental findings suggest that Br-ORM is a novel, promising β-catenin inhibitor and therefore can be harnessed as a potent anticancer small molecule for cervical cancer treatment."

Journal • Cervical Cancer • Oncology • Solid Tumor • CDH1 • CDH2 • MMP2 • MMP9 • VIM

Strengths and weaknesses of the Right to Health Act in Rajasthan. (PubMed, Indian J Med Ethics) - "Chhaya Pachauli's editorial in IJME [1] is a firsthand authentic account of The Right to Health Act in Rajasthan. It deals with different aspects of the process of enacting this law and the content of the Act itself in a dispassionate, objective manner. I think three points need to be added to this account in order to make it comprehensive."

Journal

Hormonal and non-hormonal oral contraceptives given long-term to pubertal rats differently affect bone mass, quality and metabolism. (PubMed, Front Endocrinol (Lausanne)) - "The combined hormonal contraceptive (CHC) was ethinyl estradiol and progestin, whereas the non-hormonal contraceptive (NHC) was ormeloxifene...6 metabolites were common between the serum and bone of CHC rats, suggesting their potential as biomarkers of bone health in women taking CHC. Both OCs have adverse effects on various skeletal parameters, with CHC having a greater negative impact on bone strength."

Journal • Preclinical • Musculoskeletal Diseases • Orthopedics