ormeloxifene / Generic mfg. - LARVOL DELTA

Contraceptive effectiveness and safety of ormeloxifene: a systematic review. (PubMed, BMJ Sex Reprod Health) - "Ormeloxifene shows promise as a moderately effective, safe and user-acceptable contraceptive option. The current evidence is limited by methodological weaknesses and geographic concentration. High-quality, large-scale studies in diverse populations are essential to establish ormeloxifene's comparative effectiveness and safety with greater certainty and support its inclusion in global contraceptive guidelines."

Journal • Review • Cardiovascular • Women's Health

A small GTPase, RHOH, is upregulated in the uterus during miscarriage in human and mouse model. (PubMed, Placenta) - "RHOH was upregulated in the placenta and decidua-placenta tissues of human miscarriage cases. Similarly, in mouse models, RHOH expression increased in the endometrium during miscarriage/abortion. In contrast, RHOH expression decreased at implantation sites and in the decidualized endometrium. These findings suggest that RHOH functions as a regulator of endometrial receptivity, potentially involving RAC1, and that their upregulation is associated with miscarriage/abortion."

Journal • Preclinical • IFNG • RAC1 • RHOH

Molecular Mechanisms of New and Re-purposed Synthetic as well as Natural Bioactive Molecules Against Breast Cancer: Elucidating Targets, Signaling Pathways, Resistance Modulation, and Synergistic Combinations for Prevention. (PubMed, Curr Mol Med) - "The selective estrogen receptor modulator (SERM) ormeloxifene exemplifies the promise of drug repurposing, exerting multi-target cytotoxicity through mitochondrial membrane depolarization, G0/G1 cell-cycle arrest, caspase-dependent apoptosis, ERα modulation, and disruption of proliferative signaling circuits...This convergence underscores their translational potential for developing combination or sequential regimens that enhance selectivity, circumvent drug resistance, and minimize off-target toxicity. Collectively, these mechanistically validated agents represent promising leads for preclinical optimization and rational design of next-generation, pathway-directed breast cancer therapeutics."

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

GPER as an actionable target in endocrine resistant breast cancer (AACR 2026) - "Notably, tamoxifen functions as a GPER agonist, potentially promoting tumor growth despite antagonizing estrogen receptor alpha (ERα). This study establishes GPER as a key mediator of endocrine resistance and identifies ormeloxifene as a clinically translatable dual ERα-GPER inhibitor, providing a translatable strategy to overcome endocrine resistance in breast cancer. Dual targeting of ERα and GPER represents a distinct therapeutic approach, while integration of tumor microbiome signatures offers additional opportunities for precision oncology."

Late-breaking abstract • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • HER-2

Assessing the Acceptance of and Compliance With Centchroman Usage, a Non-hormonal Contraceptive Pill, Among Postpartum Women: A Cross-Sectional Study at a Tertiary Care Centre in North India. (PubMed, Cureus) - " Centchroman demonstrated high acceptability, satisfaction, and a low failure rate among postpartum women, reaffirming its role as a reliable non-hormonal oral contraceptive. Strengthening early counseling and ensuring consistent availability may improve compliance, continuation, and wider utilization within national family planning programs."

Compliance • Journal • Observational data • Gynecology • Obstetrics

Effectiveness of Midwife Led Teaching on Knowledge, Attitude, and Readiness to Practice on Chhaya Pills among Reproductive Women in Puducherry. (PubMed, Indian J Community Med) - "The result also shows that the parity of women had a significant association with the pretest level of knowledge and attitude, type of family, and women adapting any contraception had a significant association. The study concludes that Midwife led teaching was efficiently improved the level of knowledge and attitude on Chhaya pills."

Journal

Real-world contraceptive performance of ormeloxifene among reproductive-age women. (PubMed, Indian J Med Res) - No abstract available

Journal • Real-world evidence

Ormeloxifene Versus Norethisterone for Anovulatory Abnormal Uterine Bleeding: An India-Based Systematic Review and Meta-Analysis. (PubMed, Cureus) - "This meta-analysis suggests that ormeloxifene is more effective than norethisterone in improving clinical outcomes of AUB-O, with better control of menstrual blood loss, hemoglobin levels, and endometrial thickness. Larger, high-quality multicenter trials with longer follow-up are warranted to confirm long-term safety and efficacy."

Journal • Retrospective data • Review • Women's Health

Comparative Efficacy of Ormeloxifene Versus Norethisterone Acetate in the Management of Abnormal Uterine Bleeding: A Randomized Controlled Trial. (PubMed, Cureus) - "Side effects were infrequent and well-controlled, and surgical intervention was rarely required. Conclusions Ormeloxifene demonstrates superior efficacy in reducing menstrual blood loss, improving anemia, and suppressing endometrial proliferation in women with AUB compared to norethisterone acetate, with an acceptable safety profile."

Journal • Gynecology • Hematological Disorders • Women's Health

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