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Last update 19 Apr 2025

Tamoxifen Citrate

Last update 19 Apr 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(Z)-2-(4-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylethanamine, (Z)-2-(para-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylamine, 1-p-beta-Dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene

+ [18]

Target

Action

antagonists

Mechanism

ERs antagonists(Estrogen receptors antagonists)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal DiseasesUrogenital Diseases

Active Indication

Estrogen receptor positive breast cancerNoninfiltrating Intraductal CarcinomaBreast Cancer+ [1]

Inactive Indication

Advanced Malignant Solid NeoplasmBreast Cancer, FamilialDementia+ [8]

Originator Organization

AstraZeneca PLC

Active Organization

Mayne Pharma Commercial LLC

Daré Bioscience, Inc.AstraZeneca KK

+ [1]

Inactive Organization

AstraZeneca PLCAstraZeneca Pharmaceuticals LP

Drug Highest PhaseApproved

First Approval Date

United States (30 Dec 1977),

Breast Cancer

RegulationOrphan Drug (European Union)

Structure/Sequence

Molecular FormulaC32H37NO8

InChIKeyFQZYTYWMLGAPFJ-OQKDUQJOSA-N

CAS Registry54965-24-1

379

Clinical Trials associated with Tamoxifen Citrate

NCT06348134

/ Not yet recruitingPhase 2IIT

Assessing the Efficacy and Safety of Optimal Neoadjuvant to Adjuvant Anti-HER2- Based Therapy in Nigerian Women With HER2+ Breast Cancer

Doctors leading this study would like to learn about providing cancer treatment/therapies to Nigerian women with breast cancer based on their human epidermal growth factor receptor 2 (HER2) status. This study will focus on the efficacy and safety of anti-HER2 cancer treatment before and after surgery.

Start Date01 Jan 2026

Sponsor / Collaborator

The University of Chicago

NCT06434064

/ Not yet recruitingPhase 2IIT

A Pilot, Single-Arm, Phase II Trial of Tamoxifen Plus Pegylated Liposomal Doxorubicin in Patients With Metastatic Triple Negative Breast Cancer

This phase II trial tests how well tamoxifen and pegylated liposomal doxorubicin works in treating patients with triple negative breast cancer that has spread from where it first started (primary site) to other places in the body (metastatic) or that has spread to nearby tissue or lymph nodes (locally advanced) and is unable to be operated on (inoperable). Tamoxifen works by blocking the effects of estrogen in the breast. This may help stop the growth of tumor cells that need estrogen to grow. Doxorubicin is in a class of medications called anthracyclines. Doxorubicin damages the cell's DNA and may kill cancer cells. It also blocks a certain enzyme needed for cell division and DNA repair. Liposomal doxorubicin is a form of the anticancer drug doxorubicin that is contained inside very tiny, fat-like particles. Liposomal doxorubicin may have fewer side effects and work better than other forms of the drug. Giving tamoxifen and pegylated liposomal doxorubicin together may work better in treating patients with metastatic or inoperable, locally advanced triple negative breast cancer than giving either of these drugs alone.

Start Date15 May 2025

Sponsor / Collaborator

Roswell Park Comprehensive Cancer Center

NCT06671912

/ RecruitingPhase 3IIT

LoTam: A Randomized, Phase III Clinical Trial of Low-Dose Tamoxifen for Selected Patients With Molecular Low-Risk Early-Stage Breast Cancer

This phase III trial compares the effect of low dose tamoxifen to usual hormonal therapy, including aromatase inhibitors, in treating post-menopausal women with hormone positive, HER2 negative early stage breast cancer. Tamoxifen is in a class of medications known as antiestrogens. It blocks the activity of estrogen (a female hormone) in the breast. This may stop the growth of some breast tumors that need estrogen to grow. Aromatase inhibitors, such as anastrozole, letrozole, and exemestane, prevent the formation of estradiol, a female hormone, by interfering with an aromatase enzyme. Aromatase inhibitors are used as a type of hormone therapy to treat postmenopausal women with hormone-dependent breast cancer. Giving low dose tamoxifen may be more effective compared to usual hormone therapy in treating post-menopausal women with hormone-positive, HER2 negative early stage breast cancer.

Start Date15 Apr 2025

Sponsor / Collaborator

Alliance for Clinical Trials in Oncology

[+1]

100 Clinical Results associated with Tamoxifen Citrate

100 Translational Medicine associated with Tamoxifen Citrate

100 Patents (Medical) associated with Tamoxifen Citrate

24,322

Literatures (Medical) associated with Tamoxifen Citrate

01 Nov 2025·Neural Regeneration Research

The sexually dimorphic expression of glutamate transporters and their implication in pain after spinal cord injury

Article

Author: Rivera, Luis H. Pagan ; Salgado, Iris K. ; Colón-Mercado, Jennifer M. ; Miranda, Jorge D. ; Bracho-Rincon, Dina P. ; Torrado-Tapias, Aranza I. ; Santiago, José M. ; Rivera, Samuel E. Ocasio

JOURNAL/nrgr/04.03/01300535-202511000-00033/figure1/v/2025-03-16T134409Z/r/image-tiff In addition to the loss of motor function, ~60% of patients develop pain after spinal cord injury. The cellular-molecular mechanisms are not well understood, but the data suggests that plasticity within the rostral, epicenter, and caudal penumbra of the injury site initiates a cellular-molecular interplay that acts as a rewiring mechanism leading to central neuropathic pain. Sprouting can lead to the formation of new connections triggering abnormal sensory transmission. The excitatory glutamate transporters are responsible for the reuptake of extracellular glutamate which makes them a critical target to prevent neuronal hyperexcitability and excitotoxicity. Our previous studies showed a sexually dimorphic therapeutic window for spinal cord injury after treatment with the selective estrogen receptor modulator tamoxifen. In this study, we investigated the anti-allodynic effects of tamoxifen in male and female rats with spinal cord injury. We hypothesized that tamoxifen exerts anti-allodynic effects by increasing the expression of glutamate transporters, leading to reduced hyperexcitability of the secondary neuron or by decreasing aberrant sprouting. Male and female rats received a moderate contusion to the thoracic spinal cord followed by subcutaneous slow-release treatment of tamoxifen or matrix pellets as a control (placebo). We used von Frey monofilaments and the “up-down method” to evaluate mechanical allodynia. Tamoxifen treatment decreased allodynia only in female rats with spinal cord injury revealing a sex-dependent effect. The expression profile of glutamatergic transporters (excitatory amino acid transporter 1/glutamate aspartate transporter and excitatory amino acid transporter 2/glutamate transporter-1) revealed a sexual dimorphism in the rostral, epicenter, and caudal areas of the spinal cord with a pattern of expression primarily on astrocytes. Female rodents showed a significantly higher level of excitatory amino acid transporter-1 expression while male rodents showed increased excitatory amino acid transporter-2 expression compared with female rodents. Analyses of peptidergic (calcitonin gene-related peptide-α) and non-peptidergic (isolectin B4) fibers outgrowth in the dorsal horn after spinal cord injury showed an increased calcitonin gene-related peptide-α/ isolectin B4 ratio in comparison with sham, suggesting increased receptive fields in the dorsal horn. Although the behavioral assay shows decreased allodynia in tamoxifen-treated female rats, this was not associated with overexpression of glutamate transporters or alterations in the dorsal horn laminae fibers at 28 days post-injury. Our findings provide new evidence of the sexually dimorphic expression of glutamate transporters in the spinal cord. The dimorphic expression revealed in this study provides a therapeutic opportunity for treating chronic pain, an area with a critical need for treatment.

01 Jun 2025·LIFE SCIENCES

Metabolic reprogramming and synergistic cytotoxicity of genistein and chemotherapy in human breast cancer cells

Article

Author: Vargas-Castillo, Ariana ; Torres, Nimbe ; Tobón-Cornejo, Sandra ; Schcolnik-Cabrera, Alejandro ; Noriega, Lilia G ; Morales-Bárcenas, Rocío ; Acevedo-Carabantes, Joshua Ayork ; Granados-Portillo, Omar ; Tovar, Armando R ; Chávez-Blanco, Alma ; Juarez, Mandy

Breast cancer (BCa) is a heterogeneous disease, initially responsive to hormone therapy but often developing resistance to both hormonal and chemotherapy treatments. Novel therapeutic strategies are needed for drug-resistant BCa. Genistein, a phytoestrogen structurally similar to estrogen, competes with estrogen for receptor binding and exhibits anti-cancer effects. In this study, we investigated the cellular and metabolic impacts of genistein, alone or in combination with chemotherapy, in two human BCa cell lines-one estrogen receptor-positive (ER+) and one estrogen receptor-negative (ER-). We observed a strong synergistic effect on cell viability at low concentrations of genistein and chemotherapy, resulting in reduced clonogenic capacity and impaired cell migration. Genistein alone modulated cellular energy metabolism, notably reducing ATP production in MCF7 (ER+) cells. This metabolic shift was linked to a decreased dependence on fatty acids for energy, coupled with a decrease in the rate-limiting mitochondrial translocase CPT1 required for fatty acid oxidation, alongside with an increase in intracellular fatty acid levels. While the most significant changes occurred in ER+ cells, ER- cells also showed responses to genistein treatment. Collectively, our findings suggest that low genistein concentrations, in combination with conventional chemotherapy, induces synergistic anti-cancer effects, promoting cellular senescence.

01 May 2025·BREAST CANCER RESEARCH AND TREATMENT

The impact of coadministration of venlafaxine, citalopram or gabapentin on the metabolic activation of tamoxifen

Article

Author: Goetz, Matthew P ; Stearns, Vered ; Ames, Matthew M ; Denduluri, Neelima ; Henry, N Lynn ; Suman, Vera J ; Ingle, James N ; Loprinzi, Charles L ; Weinshilboum, Richard M ; Black, John L ; Kosel, Matthew L ; Irvin, William ; Sideras, Kostantinos ; Leon Ferre, Roberto A ; Safgren, Stephanie L ; Reid, Joel M

PURPOSE:

Tamoxifen undergoes metabolic activation by cytochrome P450 (CYP) enzymes to metabolites with more potent anti-estrogenic effects. Numerous studies demonstrate decreased tamoxifen efficacy associated with reduced CYP2D6 activity or lower Z-endoxifen concentrations. Women taking tamoxifen frequently experience vasomotor symptoms (VMS) that may require medical treatment. Many medications used for VMS or depression are CYP substrates that may reduce Z-endoxifen concentrations. While the drug-drug interactions (DDI) from potent CYP2D6 inhibitors (CYPi) on tamoxifen metabolism has been studied, the impact of less potent CYPi including drugs used to treat VMS remains largely unknown.

METHODS:

We performed a prospective trial to evaluate the impact of gabapentin or non-potent CYPi (venlafaxine citalopram) on plasma concentrations of tamoxifen and its metabolites (Z-endoxifen, N-desmethyl-tamoxifen (NDMT) and 4-hydroxy-tamoxifen (4HT).

RESULTS:

Patients enrolled were intermediate to extensive metabolizers by CYP2D6 genotyping. While tamoxifen and NDMT plasma concentrations were not significantly altered, the percent decrease in plasma Z-endoxifen concentration was statistically significant with the addition of venlafaxine (n = 22) or citalopram (n = 18) (median - 14.7 and - 14.4%, respectively) but not with gabapentin (n = 14) (median - 2.3%). A reduction in Z-endoxifen concentrations below the 5.9 ng/ml threshold associated with tamoxifen efficacy was observed in 12% of patients.

CONCLUSION:

The addition of venlafaxine and citalopram but not gabapentin during tamoxifen treatment decreases plasma Z-endoxifen concentrations. SSRIs/SNRIs affecting tamoxifen biotransformation pathways, but with less potent CYPi potential, should be used cautiously in tamoxifen-treated patients and non-CYP inhibiting medications considered when possible.

News (Medical) associated with Tamoxifen Citrate

13 Mar 2025

·www.prnewswire.com

VERZENIO's Market Potential Soars as Demand for CDK4/6 Inhibitors Grows | DelveInsight

As VERZENIO gains traction in early-stage treatments and broadens its approved uses, its revenue is expected to keep growing. While the global CDK4/6 inhibitor market remains highly competitive, VERZENIO's distinct clinical advantages and ongoing studies could contribute to further market expansion. LAS VEGAS, March 13, 2025 /PRNewswire/ -- DelveInsight's " VERZENIO Market Size, Forecast, and Market Insight Report" highlights the details around VERZENIO, which is a targeted treatment known as a CDK4/6 inhibitor. The drug is a non-chemotherapy oral tablet. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of VERZENIO. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan]. Eli Lilly and Company's VERZENIO (abemaciclib) Overview VERZENIO (abemaciclib) is a prescription medication used to treat adults with HR-positive, HER2-negative breast cancer that has metastasized (spread to other parts of the body). It is administered orally and is prescribed in combination with an aromatase inhibitor as an initial endocrine-based therapy. Additionally, the drug is being developed for the treatment of prostate cancer. VERZENIO is approved for the following indications: In combination with endocrine therapy for the adjuvant treatment of adults with HR+/HER2-, node-positive, early-stage breast cancer at high risk of recurrence. In combination with an aromatase inhibitor as the initial endocrine-based therapy for adults with HR+/HER2- advanced or metastatic breast cancer. In combination with fulvestrant for adults with HR+/HER2- advanced or metastatic breast cancer that has progressed after prior endocrine therapy. As monotherapy for adults with HR+/HER2- advanced or metastatic breast cancer that has progressed following endocrine therapy and prior chemotherapy in the metastatic setting. Learn more about VERZENIO projected market size for breast cancer @ VERZENIO Market Potential HR+/HER2- breast cancer is the most common subtype of breast cancer, defined by the presence of estrogen and progesterone hormone receptors but lacking HER2 overexpression. This form of breast cancer generally has a favorable prognosis and is primarily managed with hormone therapy to suppress hormone-driven tumor growth. According to DelveInsight's estimates, around 211,000 new cases of HR+/HER2− breast cancer were reported in the US in 2024. Over the past decade, endocrine therapy has remained the cornerstone of treatment, including for cases with visceral involvement. The current preferred approach involves combining endocrine therapy—using aromatase inhibitors or fulvestrant—with CDK4/6 inhibitors. The approval of CDK4/6 inhibitors has significantly transformed the treatment landscape for HR+/HER2− breast cancer. Currently, five selective CDK4/6 inhibitors— ENHERTU, DATROWAY, IBRANCE, KISQALI, and VERZENIO—are used in combination with endocrine therapy. In November 2023, the FDA approved TRUQAP (capivasertib) in combination with FASLODEX for patients with advanced HR+/HER2− breast cancer harboring specific biomarker alterations (PIK3CA, AKT1, or PTEN). The NCCN Guidelines have designated KISQALI as the only Category 1 Preferred CDK4/6 inhibitor for first-line treatment in combination with an aromatase inhibitor, strengthening its position in the U.S. market. This led to KISQALI recovering its lost market share, with its U.S. revenue contribution rebounding to 50%, following declines to 46% in 2020, 36% in 2021, and 38% in 2022. In January 2025, the FDA approved DATROWAY for patients with unresectable or metastatic HR+/HER2- breast cancer (IHC 0, IHC 1+, or IHC 2+/ISH-) who had previously received endocrine-based therapy and chemotherapy. Additionally, ENHERTU was approved for patients with unresectable or metastatic HR+, HER2-low (IHC 1+ or IHC 2+/ISH-) or HER2-ultralow (IHC 0 with membrane staining) breast cancer that had progressed after at least one prior endocrine therapy in the metastatic setting. Also, in January 2025, Roche reported positive topline results from its Phase III INAVO120 trial, assessing ITOVEBI in combination with IBRANCE and fulvestrant for patients with PIK3CA-mutated HR+/HER2−, endocrine-resistant, locally advanced, or metastatic breast cancer. Among the seven major markets, the US accounted for the largest market share in HR+/HER2− breast cancer, generating USD 7.5 billion in revenue in 2023. The market is expected to experience substantial growth from 2025 to 2034, driven by the introduction of novel therapeutic options. Discover more about the breast cancer market in detail @ Metastatic HR+/HER2- Breast Cancer Market Report Emerging Competitors of VERZENIO Some of the competing emerging key players in HR+/HER2- breast cancer market are, Merck (KEYTRUDA), Arvinas (ARV-471 (vepdegestrant)), Olema Pharmaceuticals (OP1250 (palazestrant)), Celcuity (Gedatolisib), Roche (Giredestrant (RG6171, GDC-9545); Inavolisib), AstraZeneca and Daiichi Sankyo (Datopotamab Deruxtecan (Dato-DXd)), AstraZeneca (Camizestrant (AZD9833); Capivasertib), Eli Lilly (LY3484356/Imlunestrant), Sermonix Pharmaceuticals (Lasofoxifene), Veru Pharma (Enobosarm), DualityBio/BioNtech (DB-1303), Evgen Pharma (SFX-01), Carrick Therapeutics (Samuraciclib (CT-7001)), EQRx/G1 Therapeutics (Lerociclib), Immutep (Eftilagimod Alpha (LAG-3lg/IMP321)), and others. To know more about the number of competing drugs in development, visit @ VERZENIO Market Positioning Compared to Other Drugs Key Milestones of VERZENIO In 2024, Phase III trials did not meet primary endpoints or were terminated for futility. Negative Phase III CYCLONE-2 results, in which VERZENIO added to abiraterone did not meet the primary endpoint of improved radiographic progression-free survival (rPFS) in men with metastatic castration-resistant prostate cancer (mCRPC). In December 2023, Eli Lilly and Company presented results from the MONARCH 3 clinical trial at the 2023 San Antonio Breast Cancer Symposium (SABCS). Results from MONARCH 3 show a numerical improvement in overall survival (OS) of 13.1 months for women with HR+, HER2- metastatic breast cancer treated with VERZENIO plus an aromatase inhibitor in the intent-to-treat population and 14.9 months for women with visceral disease. In March 2023, the US FDA approved an expanded indication for VERZENIO in combination with endocrine therapy for the adjuvant treatment of adult patients with HR+/HER2−, node-positive, early breast cancer (EBC) at a high risk of recurrence. This expanded adjuvant indication removes the Ki-67 score requirement for patient selection. In February 2022, the CHMP adopted a positive opinion recommending a change to the terms of the marketing authorization for the medicinal product VERZENIO. VERZENIO, in combination with endocrine therapy, is indicated for the adjuvant treatment of adult patients with HR+/HER2− negative, node-positive early breast cancer at high risk of recurrence. In October 2021, the US FDA approved VERZENIO, in combination with endocrine therapy (tamoxifen or an aromatase inhibitor), for the adjuvant treatment of adult patients with HR+/HER2−, node-positive, early breast cancer at high risk of recurrence and a Ki-67 score of ≥20% as determined by an FDA-approved test. Ki-67 is a marker of cellular proliferation. In September 2018, VERZENIO was approved in Europe for treating advanced HR+ breast cancer in women if the cancer has already spread to other parts of the body or is locally advanced. In September 2018, VERZENIO was approved for the treatment of patients with HR+/HER2− unresectable or recurrent breast cancer in combination with fulvestrant or an aromatase inhibitor (AI) in Japan. In February 2018, the US FDA approved VERZENIO in combination with an aromatase inhibitor (AI) as initial endocrine-based therapy for the treatment of postmenopausal women with HR+/HER2− advanced or metastatic breast cancer In September 2017, the US FDA approved VERZENIO in combination with an endocrine therapy to treat adult patients who have HR+/HER2− advanced or metastatic breast cancer that has progressed after taking therapy that alters a patient's hormones (endocrine therapy). In October 2015, the US FDA granted Breakthrough Therapy Designation to abemaciclib for patients with refractory hormone-receptor-positive (HR+) advanced or metastatic breast cancer Discover how VERZENIO is shaping the breast cancer treatment landscape @ VERZENIO Breast Cancer VERZENIO Market Dynamics The oral administration of VERZENIO enhances patient convenience, while its expanded approval for the adjuvant treatment of adult patients with HR+/HER2- early breast cancer highlights its role as a differentiated CDK4/6 inhibitor in reducing the risk of recurrence. The rising prevalence of HR+/HER2- breast cancer is driving market demand for effective treatments like VERZENIO. Additionally, its demonstrated efficacy in combination with endocrine therapy and its ability to penetrate the central nervous system further strengthen its market position. Favorable reimbursement policies and increasing awareness among healthcare providers also contribute to its adoption. However, its adoption may be hindered by regulatory hurdles and potential side effects, including severe or life-threatening lung inflammation and serious liver problems. High treatment costs and access disparities in certain regions could also limit market penetration. Competition from other CDK4/6 inhibitors such as IBRANCE and KISQALI poses a challenge, along with concerns over long-term safety data. Additionally, the Phase III CYCLONE-2 trial failed to meet primary endpoints in mCRPC, which may impact its broader clinical prospects and investor confidence. Dive deeper to get more insight into VERZENIO's strengths & weaknesses relative to competitors @ VERZENIO Market Drug Report Table of Contents Related Reports CDK4/6 Inhibitor Market CDK4/6 Inhibitor Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key CDK4/6 inhibitor companies including Pfizer, Prelude Therapeutics, G1 Therapeutics, Pepper Bio, among others. Metastatic HR+/HER2− Breast Cancer Market Metastatic HR+/HER2− Breast Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key metastatic HR+/HER2− breast cancer companies including Pfizer, Novartis, Stemline Therapeutics, Olema Pharmaceuticals, Arvinas, Immutep, AstraZeneca, Roche, Genentech, Evexta Bio, EQRx, Sermonix Pharmaceuticals, Celcuity, Veru Pharma, Evgen Pharma, Eli Lilly, Biotheryx, among others. HR+/HER2− Breast Cancer Pipeline HR+/HER2− Breast Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key HR+/HER2− breast cancer companies, including Regor Therapeuics, Seagen Inc., CytomX Therapeutics, Taizhou EOC Pharma, Chia Tai Tianqing Pharmaceutical Group, AstraZeneca, Daiichi Sankyo, Inc., Tyme, Inc., Seagen Inc., Context Therapeutics, Eisai Inc., Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Simcere Pharmaceutical Co., Kind Pharmaceuticals, Merus N.V., Atossa Therapeutics, Roche, among others. Breast Cancer Market Breast Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key breast cancer companies, including Veru, Sanofi, Roche, AstraZeneca, Eli Lilly, EQRx, Gilead, Sermonix Pharmaceuticals, Evgen Pharma, Tyme, Genentech, Daiichi Sankyo, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Phase 3Drug ApprovalClinical ResultBreakthrough TherapyASCO

10 Jan 2025

·pmlive.com

Bayer’s non-hormonal menopause drug shows promise in phase 3 breast cancer trial

Bayer has shared positive results from a late-stage study of its investigational non-hormonal drug in patients experiencing vasomotor symptoms (VMS) as a result of breast cancer treatment. The phase 3 OASIS 4 study has been evaluating the candidate, elinzanetant, as a treatment for moderate-to-severe VMS caused by adjuvant endocrine therapy in women with hormone receptor positive breast cancer or in those who are at high risk of developing breast cancer. VMS, such as hot flashes, are reported by up to 80% of women at some point during the menopausal transition, and over one-third report severe symptoms. Those receiving adjuvant endocrine therapy, including tamoxifen or aromatase inhibitors, for the treatment or prevention of breast cancer may also experience VMS. There are currently no licensed treatment options for this patient population. OASIS 4 met its primary endpoint, with elinzanetant resulting in statistically significant mean reductions in the frequency of moderate-to-severe VMS from baseline to weeks four and 12 compared to placebo. All key secondary endpoints were also achieved, demonstrating a reduction in severity of VMS at weeks four and 12, a reduction in frequency of VMS at week one, as well as improvements in sleep disturbances and menopause-related quality of life at week 12 compared to placebo. Additionally, the safety profile of elinzanetant observed over 52 weeks was generally consistent with previously conducted studies and published data on the drug in postmenopausal women with VMS. Administered orally once daily, elinzanetant is a dual neurokinin-1, 3 receptor antagonist in late-stage clinical development to treat moderate-to-severe VMS associated with menopause or caused by adjuvant endocrine therapy for breast cancer. The latest results for the drug build on positive results from the phase 3 OASIS 1, 2 and 3 trials in women with moderate-to-severe VMS associated with menopause. Fatima Cardoso, principal investigator of OASIS 4, said: “The positive results from OASIS 4 bring us one step closer to a much-needed non-hormonal option for managing VMS in breast cancer patients and women at risk of breast cancer.” Submissions for marketing authorisations for elinzanetant are ongoing in the US, EU, UK and other markets globally, Bayer outlined.

Phase 3Clinical Result

09 Jan 2025

·pipelinereview.com

Elinzanetant meets all primary and secondary endpoints in Phase III study OASIS 4 for treatment of moderate to severe vasomotor symptoms caused by breast cancer treatments

In OASIS 4, a Phase III study conducted outside of the US, the investigational compound elinzanetant met all primary endpoints demonstrating a statistically significant reduction in frequency of moderate to severe vasomotor symptoms (VMS) caused by adjuvant endocrine therapy compared to placebo in women with or at high risk of developing hormone receptor positive breast cancer The study also met all secondary endpoints with a reduction in severity of VMS at weeks 4 and 12, a reduction in frequency of VMS at week 1 as well as improvements in sleep disturbances and menopause related quality of life The safety profile over 52 weeks is generally consistent with previously published data in postmenopausal women with VMS Positive topline results from OASIS 4, the first pivotal international Phase III study addressing this population of unmet medical need, add to the positive results of OASIS 1,2 and 3 and further support the efficacy and safety of elinzanetant Elinzanetant is the first dual neurokinin-1 and 3 (NK-1,3) receptor antagonist in development for the non-hormonal treatment of moderate to severe VMS associated with menopause or caused by adjuvant endocrine therapy, administered orally once daily BERLIN, Germany I January 9, 2025 I Bayer today announced positive topline results of the Phase III study OASIS 4 investigating elinzanetant as non-hormonal treatment for moderate to severe vasomotor symptoms caused by adjuvant endocrine therapy in women with breast cancer or at high risk of developing breast cancer. Elinzanetant successfully met the primary endpoints of the study demonstrating statistically significant reductions in the frequency of moderate to severe vasomotor symptoms (VMS, also known as hot flashes) from baseline to week 4 and 12 compared to placebo. The study also achieved all secondary endpoints demonstrating reductions in severity of VMS at week 4 and 12, VMS frequency reduction at week 1 as well as maintaining the effects over the study period. Elinzanetant also showed improvements of sleep disturbances and menopause-related quality of life at week 12 compared to placebo. The safety profile over 52 weeks observed in the OASIS 4 study is generally consistent with previously conducted studies and published data 1,2,3 on elinzanetant in postmenopausal women with VMS. “Elinzanetant has consistently demonstrated positive results across all four Phase III clinical trials that assessed the efficacy and safety for the treatment moderate to severe vasomotor symptoms associated with menopause or caused by adjuvant endocrine therapy,” said Dr. Christian Rommel, Head of Research and Development and Member of the Executive Committee of Bayer’s Pharmaceuticals Division. “Importantly, OASIS 4 is the first pivotal international study to assess the safety and efficacy of a non-hormonal treatment approach for women with or at high risk of breast cancer who are suffering from VMS caused by adjuvant endocrine therapy, reaffirming our commitment at Bayer to advancing innovative treatments for the different needs of women and their health.” Breast cancer is the most frequent cancer in women globally with 2.3 million new cases in 2020, with nearly 70% of tumors being hormone-receptor positive. Adjuvant endocrine therapy is well established in guidelines worldwide and routinely prescribed to all women with hormone-positive breast cancer. Treatment with adjuvant endocrine therapy (such as tamoxifen or aromatase inhibitors) for up to 10 years substantially reduces the breast cancer mortality rate throughout the 2 decades after diagnosis. 4 Adjuvant endocrine therapy can also be used as primary prevention, in women at high risk of developing breast cancer. VMS (also referred to as hot flashes) is a common adverse reaction of the adjuvant endocrine therapy, which may affect quality of life and treatment compliance, with potential impact on recurrence and long term outcomes 5 . There is unmet medical need for an effective non-hormonal treatment for VMS caused by adjuvant endocrine therapy as currently no approved treatment options are available. “For women undergoing endocrine therapy against breast cancer, menopausal symptoms like VMS and sleep disturbances are very common and can significantly affect quality of life, potentially impacting treatment adherence,” said Dr. Fatima Cardoso, Principal Investigator of OASIS 4, from Lisbon, Portugal. “The positive results from OASIS 4 bring us one step closer to a much-needed non-hormonal option for managing VMS in breast cancer patients and women at risk of breast cancer.” Elinzanetant is the first dual neurokinin-1 and 3 (NK-1,3) receptor antagonist, in late-stage clinical development for the non-hormonal treatment of moderate to severe VMS associated with menopause or caused by adjuvant endocrine therapy for breast cancer, administered orally once daily. OASIS 4 (NCT05030584) is the first pivotal international Phase III study to assess the safety and efficacy of a non-hormonal treatment of moderate to severe VMS caused by adjuvant endocrine therapy. It is the fourth Phase III study in the OASIS clinical development program with positive topline results, with details planned to be presented at upcoming scientific congresses. Data from OASIS 1 and 2 were published in the Journal of the American Medical Association ( JAMA ) 3 in August 2024. Detailed results of the Phase III study OASIS 3 providing additional efficacy and safety data over 52 weeks were presented at The Menopause Society (TMS) annual meeting in September 2024. Based on the positive results from the Phase III clinical development program, submissions for marketing authorizations for elinzanetant are ongoing in the US, EU and other markets around the world. About the Elinzanetant clinical development program The Phase III clinical development program of elinzanetant, OASIS, currently comprises four Phase III studies: OASIS 1, 2, 3 and 4. OASIS 1 and 2 investigated the efficacy and safety of elinzanetant administered orally once daily in women with moderate to severe VMS associated with menopause over 26 weeks and randomized 396 and 400 postmenopausal women between 40 and 65 years across 184 sites in 15 countries. Patients in the elinzanetant arm received a 120 mg dose of elinzanetant once daily for 26 weeks and patients in the control arm received a matching placebo once daily for 12 weeks, followed by elinzanetant 120 mg dose for 14 weeks. OASIS 3 investigated the efficacy and safety of elinzanetant for the treatment of vasomotor symptoms associated with menopause over 52 weeks and randomized 628 postmenopausal women between 40 and 65 years across 83 sites in 9 countries. OASIS 4 is a double-blind, randomized, placebo-controlled multicenter study to investigate efficacy and safety of elinzanetant for the treatment of vasomotor symptoms caused by adjuvant endocrine therapy, over 52 weeks and optionally for an additional 2 years in women with, or at high risk for developing hormone-receptor positive breast cancer. 474 patients at 90 centers in 16 countries (excluding the US) were randomized. About Elinzanetant Elinzanetant is the first dual neurokinin-1 and 3 (NK-1, 3) receptor antagonist, in late-stage clinical development for the non-hormonal treatment of moderate to severe VMS associated with menopause or caused by adjuvant endocrine therapy, administered orally once daily. Elinzanetant may address moderate to severe VMS by modulating a group of estrogen sensitive neurons in the hypothalamus region of the brain (the KNDy neurons) which, with the decrease of estrogen, become hypertrophic and lead to a hyperactivation of the thermoregulatory pathway, consequently disrupting body heat control mechanisms resulting in VMS. Based on key secondary endpoints of OASIS 1 and 2, Elinzanetant may also decrease sleep disturbances associated with menopause. About Vasomotor Symptoms Vasomotor symptoms (VMS; also referred to as hot flashes) result from hyperactivation of the thermoregulatory pathway mediated by hypertrophy of the KNDy neurons. This is due to a decrease of estrogen, which can result from the progressive reduction of ovarian function due to natural menopause or medical intervention by bilateral oophorectomy or adjuvant endocrine therapy. VMS are reported by up to 80% of women at some point during the menopausal transition and are one of the leading causes for seeking medical attention during this phase of a woman’s life. Over one-third of menopausal women report severe symptoms, which can last 10 years or more after the last menstrual period, with relevant impact on quality of life. VMS may also be caused by adjuvant endocrine therapy, for the treatment or prevention of breast cancer, impacting quality of life and treatment adherence. For these women, there are currently no approved treatment options. About Menopause By 2030, the global population of women experiencing menopause is projected to increase to 1.2 billion, with 47 million women entering this phase each year. Menopause is a transitional phase in women’s lives, related to the progressive decline of ovarian function. It usually occurs in women during their 40s or early 50s. The hormonal decline can lead to various symptoms which can substantially affect a woman’s health, quality of life, healthcare utilization and work productivity. The most frequently reported and disruptive symptoms during the menopausal transition are VMS, sleep disturbances and mood changes. Menopausal symptoms can also be the result of surgical or medical treatment. Addressing the symptoms is key to maintaining functional ability and quality of life which is highly relevant from both a healthcare and socio-economic perspective. About Women’s Healthcare at Bayer Women’s Health is in Bayer’s DNA. As a global leader in women’s healthcare Bayer has a long-standing commitment to delivering science for a better life by advancing a portfolio of innovative treatments. Bayer offers a wide range of effective short- and long-acting birth control methods as well as therapies for menopause management and gynecological diseases. Bayer is also focusing on innovative options to address the unmet medical needs of women worldwide and to broadening treatment choices such as in menopause. Additionally, Bayer intends to provide 100 million women per year in low-and-middle income countries by 2030 with access to family planning by funding multi-stakeholder aid programs for capacity building and by ensuring the supply of affordable modern contraceptives. This is part of the comprehensive sustainability measures and commitments from 2020 onwards and in line with the Sustainable Development Goals of the United Nations. About Bayer Bayer is a global enterprise with core competencies in the life science fields of health care and nutrition. In line with its mission, “Health for all, Hunger for none,” the company’s products and services are designed to help people and the planet thrive by supporting efforts to master the major challenges presented by a growing and aging global population. Bayer is committed to driving sustainable development and generating a positive impact with its businesses. At the same time, the Group aims to increase its earning power and create value through innovation and growth. The Bayer brand stands for trust, reliability and quality throughout the world. In fiscal 2023, the Group employed around 100,000 people and had sales of 47.6 billion euros. R&D expenses before special items amounted to 5.8 billion euros. For more information, go to www.bayer.com . Find more information at https://pharma.bayer.com/ Follow us on Facebook: http://www.facebook.com/bayer Follow us on LinkedIn: Bayer | Pharmaceuticals SOURCE: Bayer

Phase 3Clinical Result

100 Deals associated with Tamoxifen Citrate

External Link

KEGG	Wiki	ATC	Drug Bank
D00966	Tamoxifen Citrate	L02BA01	DB00675

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Estrogen receptor positive breast cancer	United States	Mayne Pharma Commercial LLC	25 Sep 2018
Noninfiltrating Intraductal Carcinoma	United States	Mayne Pharma Commercial LLC	29 Oct 2005
Breast Cancer	United States	AstraZeneca Pharmaceuticals LP	30 Dec 1977

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Gynecomastia	Phase 3	Italy	AstraZeneca PLC	01 Dec 2003
Prostatic Cancer	Phase 3	Italy	AstraZeneca PLC	01 Dec 2003
Hormone receptor positive breast cancer	Phase 3	Austria	AstraZeneca PLC	01 Jan 1996
Early Stage Breast Carcinoma	Phase 3	-	AstraZeneca PLC	01 Dec 1990
Vulvovaginal atrophy	Phase 2	Australia	Daré Bioscience, Inc.	22 Nov 2021
Dementia	Phase 2	United States	AstraZeneca PLC	01 Jan 2007
Dementia	Phase 2	Italy	AstraZeneca PLC	01 Jan 2007
Metastatic Neoplasm to the Bladder	Phase 2	United States	AstraZeneca PLC	01 Jan 2007
Metastatic Neoplasm to the Bladder	Phase 2	Italy	AstraZeneca PLC	01 Jan 2007
Transitional Cell Carcinoma	Phase 2	United States	AstraZeneca PLC	01 Jan 2007

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04079517 (Karisma-1, CTgov)	Phase 1/2	Breast Cancer	42	Tamoxifen (Tamoxifen 10mg)	pntuqmexhl(skvdzauocv) = pcqteiahtb pndnelkhsm (pheezavcpz, girzonjswm - byrkjcjuhg) View more	-	06 Feb 2025
				Tamoxifen (Tamoxifen 20mg)	pntuqmexhl(skvdzauocv) = eewaudftxi pndnelkhsm (pheezavcpz, doubrpbzwh - tawarcumqs) View more
NCT03354039 (TAMDMD Group B, Pubmed \| Neuromuscul Disord)	Phase 3	Muscular Dystrophy, Duchenne	15	Tamoxifen 20 mg/day	ulfvbcvofb(czsswbkwah) = drxfciofve prvmjydueo (mxrtxnywak, -26.82 to 11.22)	Negative	01 Feb 2025
NCT00412022 (HOBOE, Pubmed \| ESMO Open)	Phase 3	Hormone receptor positive breast cancer Adjuvant human epidermal growth factor receptor 2 (HER2)	-	Triptorelin + Tamoxifen	hkifwkqicx(wjinjsnjcc): HR = 0.69 (95% CI, 0.49 - 0.97), P-Value = 0.03 View more	Positive	01 Jan 2025
				Triptorelin + Letrozole
NCT05378269 (DARE-VVA1, CTgov)	Phase 1/2	Vulvovaginal atrophy	17	Placebo (Placebo)	pcpdcyhzji = jrcosbpfni fcdmwlhmtb (xqsopfyctu, zxmoocwzjo - alhvjcqqry) View more	-	21 Oct 2024
				Tamoxifen (DARE-VVA1 1mg)	pcpdcyhzji = vmiskoqlge fcdmwlhmtb (xqsopfyctu, shqpfkphqi - mehnhalmoc) View more
NCT02913430 (CTgov)	Early Phase 1	Metastatic breast cancer	7	Fulvestrant+Palbociclib (Fulvestrant + Palbociclib)	zkdohuoqyq(yaczorgiee) = hbjabnnlao bvnavrzfsw (wxoawmdujx, qnlsgipxak - sanzlznnul) View more	-	23 Sep 2024
				Tamoxifen+Palbociclib (Tamoxifen + Palbociclib)	zkdohuoqyq(yaczorgiee) = zjehkwyyge bvnavrzfsw (wxoawmdujx, wbwrifzlft - xxxyqgbqtd) View more
NCT00072462 (IBIS-II DCIS, CTgov)	Phase 3	Ductal Carcinoma \| Breast Cancer \| Noninfiltrating Intraductal Carcinoma	2,980	anastrozole (Anastrozole)	rcanwbmpoe = qlctwvzwni blgapixbab (imwwmisfce, hwbmhonlai - fvmedvaeoj) View more	-	19 Sep 2024
				tamoxifen citrate (Tamoxifen)	rcanwbmpoe = iexigxrauj blgapixbab (imwwmisfce, hqofpyuvzt - gvzjdnhdng) View more
STO-trials (ESMO2024)	Not Applicable	Breast Cancer Adjuvant estrogen receptor (ER)-positive	822	Tamoxifen therapy	eqjgoeovko(dpyctfhcom) = aqikelrntu hcyhcqzdyr (fhpfmaogtn )	Positive	16 Sep 2024
				No endocrine therapy (control)	eqjgoeovko(dpyctfhcom) = lgcsghfobb hcyhcqzdyr (fhpfmaogtn )
ESMO2024	Not Applicable	Breast Cancer ER-positive \| HER2-negative \| luminal A ... View more	952	Tamoxifen therapy	zdmziuarjn(zetyvoeued): HR = 0.58 (95% CI, 0.43 - 0.79)	Positive	16 Sep 2024
				Control
UK/ANZ DCIS randomized trial (ESMO2024)	Not Applicable	Ductal Carcinoma Adjuvant ER (clonal) status	755	tamoxifen (No adjuvant treatment)	rcbkklnhnn(baxbxbnttz): HR = 4.54 (95% CI, 2.27 - 9.06)	Positive	15 Sep 2024
				Radiotherapy
ENDO2024	Not Applicable	Ovarian Hyperstimulation Syndrome \| Breast Cancer Neoadjuvant estrogen receptors (ER)	-	Tamoxifen	twsfwknfbj(jvtejandde) = azmqplstuv ftadqvksxs (lskvitnxdk, 0.66 - 8.75) View more	-	01 Jun 2024

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