Last update 07 Nov 2024

Estradiol

Last update 07 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

SummaryEstradiol (E2), a predominant female sex hormone and a member of the estrogen family, is responsible for regulating the menstrual and estrous cycles. It plays a pivotal role in orchestrating the development of female secondary sexual characteristics such as breast growth, widening of the hips, and a characteristic fat distribution pattern, as well as the development and sustenance of female reproductive tissues such as the mammary glands, uterus, and vagina. Apart from these crucial functions, E2 exerts significant effects on various other tissues in the body, including the liver, bone, fat, skin, and the brain. Estradiol activates both subtypes of the estrogen receptor (ERα and ERβ), is considered a potent agonist of these nuclear steroid hormone receptors. The hormone has multiple clinical applications, such as treating menopause symptoms, preventing osteoporosis in menopausal women, and treating low estrogen levels in women with ovarian failure. Moreover, it is also indicated in the treatment of certain types of breast and prostate cancer, which highlights its versatility and clinical significance. Interestingly, E2 is available in a diverse range of forms including oral tablets, topical gels or patches, vaginal creams, and injections, which provide ample options for individuals to choose from, based on their unique and specific requirements, preferences, and medical history.

Drug Type

Small molecule drug

Synonyms

17β-estradiol, 17β-Oestradiol, E2

+ [63]

Target

Mechanism

ERs agonists(Estrogen receptors agonists)

Therapeutic Areas

Cardiovascular DiseasesEndocrinology and Metabolic DiseaseSkin and Musculoskeletal Diseases+ [2]

Active Indication

InfertilityOvarian StimulationsDyspareunia+ [11]

Inactive Indication

Advanced Prostate CarcinomaAlzheimer DiseaseCicatrix+ [8]

Originator Organization

Mylan NV

Active Organization

Hisamitsu Pharmaceutical Co., Inc.WATSON LABS INC

Bayer Yakuhin Ltd.

+ [20]

Inactive Organization

Novo Nordisk A/S

AbbVie, Inc.

TherapeuticsMD, Inc.

+ [12]

Drug Highest PhaseApproved

First Approval Date

US (22 Dec 1994),

HypoestrogenismUterine HemorrhageVasomotor symptom+ [1]

RegulationOrphan Drug (US)

Structure

Molecular FormulaC18H24O2

InChIKeyVOXZDWNPVJITMN-ZBRFXRBCSA-N

CAS Registry50-28-2

452

Clinical Trials associated with Estradiol

TCTR20170322001 / CompletedPhase 1IIT

Effect of estradiol vaginal gel on vaginal atrophy in menopausal women: A randomized control trial

Start Date05 Jul 2560

Sponsor / Collaborator

Mahidol University

NCT06369363 / Not yet recruitingEarly Phase 1IIT

Estrogen Deficiency on Cardiovascular Risk: Sympathetic Responses and Pro-inflammatory Cytokines

To explore how estrogen deficiency impacts the blood pressure (BP) and sympathetic nerve activity (SNA), and how it impacts the production of the key pro-inflammatory mediators such as Tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6). It is hypothesized that estrogen deficiency increases BP, SNA and the pathway activities of the key pro-inflammatory mediators. Those effects are impacted through the downregulation of the estrogen receptor.

Start Date01 Sep 2025

Sponsor / Collaborator

Hershey Medical Center

CTRI/2024/09/073380 / Not yet recruitingPhase 2IIT

Randomized, Open labelled, Phase IIa /IIb Clinical trial to study the safety and efficacy of intravenous estrogen therapy in reducing the incidence of sepsis/septic shock in Trauma Hemorrhagic Shock patients - PROTECT-THS

Start Date12 Nov 2024

Sponsor / Collaborator

Indian Council of Medical Research

100 Clinical Results associated with Estradiol

100 Translational Medicine associated with Estradiol

100 Patents (Medical) associated with Estradiol

124,218

Literatures (Medical) associated with Estradiol

01 Feb 2025·TALANTA

A highly sensitive electrochemical aptasensor for detecting broad-spectrum estrogen molecules in clinical samples

Article

Author: Zhao, Ya ; Liu, Siyao ; Gao, Shunxiang ; Li, Shengjie ; Yin, Ning ; Yan, Biao

The lack of sensitive and accurate monitoring methods for in vivo estrogen levels presents challenges for better prevention of estrogen-induced diseases. We have developed a label-free electrochemical aptasensor that demonstrates high sensitivity and selectivity for the broad-spectrum detection of estrogen molecules. This biosensor uses gold nanoparticles for electrochemical signal amplification and aptamers for broad-spectrum target recognition, enabling precise detection of trace amounts of estrogen in serum samples. The aptasensor demonstrates high sensitivity in estrogen detection, with a linear detection range of 0.01-1 nM and a minimum detection limit of 3 pM. It also exhibits excellent selectivity and interference resistance, with a detection error of less than 19 %, even in the presence of high concentrations of other biological substances. Additionally, molecular dynamics simulations were performed to provide insights into the molecular mechanism of aptamer broad-spectrum recognition and construction principles underlying the sensor. We anticipate that this aptasensor will serve as a robust, convenient, and cost-effective detection method, offering a valuable solution for the prevention of estrogen-induced diseases.

01 Feb 2025·SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY

ATR-FTIR spectroscopy to evaluate serum protein expression in a murine cerebral ischemia model

Article

Author: Espinosa-García, Claudia ; González-Flores, Oscar ; Delgado-Macuil, Raúl Jacobo ; Montes-Narváez, Omar ; Beltrán-Pérez, Georgina ; García-Juárez, Marcos

Stroke is a prevalent vascular disease that causes disability and death worldwide. Molecular techniques have been developed to assess serum concentrations of biomarkers associated with this disease, such as some proteins. ATR-FTIR was proposed as an alternative technique to determine protein expression during the early stages of stroke. Serum samples from sham, ischemic, and ischemic treated with estradiol benzoate (EB; as a neuroprotective agent) male rats were evaluated at 0, 2-, 4-, 6-, 12-, and 24-hours post-ischemia. The analysis was developed in the mid-infrared region but mainly focused on the protein region (1500-1700 cm^-1), where it was possible to observe the modulation in the absorbance intensity. The peaks at 1545, 1645, 1635, and 1650 cm^-1 associated with amide II, amide I, β-sheets, and α-helixes, respectively, were prominent peaks where protein modulation was observed. The results demonstrate that infrared spectroscopy could be a good alternative technique to determine the modulation of protein expression during stroke events.

01 Jan 2025·JOURNAL OF ETHNOPHARMACOLOGY

Dan’e fukang decoction reduces hemorrhage in a rat model of mifepristone induced incomplete abortion and may correlate with cell adhesion molecule signaling interference

Article

Author: Ni, Qi-Cheng ; Zhou, Jie-Yun ; Yang, Wen-Jie ; Zhong, Rui-Hua ; Wu, Jianhui ; Ni, Qi-cheng ; Zhu, Yan ; Zhou, Jie-yun ; Hu, Ying-Yi ; Yang, Wen-jie ; Hu, Ying-yi ; Zhong, Rui-hua ; Yang, Ye ; Li, Guo-Ting ; Li, Guo-ting

ETHNOPHARMACOLOGICAL RELEVANCE:

Dan'e fukang decoction (DFD) is a traditional Chinese medicine formula. DFD obtains 10 herbs, including Salvia yunnanensis C.H.Wright (Zidanshen), Curcuma zedoaria (Christm.) Roscoe (Ezhu), Angelica sinensis (Oliv.) Diels (Danggui), Cyperus rotundus L. (Xiangfuzi), Corydalis yanhusuo (Y.H.Chou & Chun C. Hsu) W.T.Wang ex Z.Y.Su & C.Y.Wu, Bupleurum marginatum Wall. ex DC. (Yanhusuo), Sparganium stoloniferum (Buch.-Ham. ex Graebn.) Buch.-Ham. ex Juz. (Sanleng), Panax notoginseng (Burkill) F.H.Chen (Sanqi), Paeonia lactiflora Pall. (Shaoyao) and Glycyrrhiza uralensis Fisch. (Gancao). DFD is now clinically used for the treatment of menstrual irregularities, dysmenorrhea and menstrual discomfort caused by blood stasis and easing of endometriosis. Based on this, it is reasonable to presume that DFD may be effective in treating incomplete abortion and reducing postpartum bleeding, but no specific studies have been reported so far.

AIM OF THE STUDY:

To investigate the efficacy of Dan'e fukang decoction (DFD) in reducing prolonged vaginal bleeding followed by mifepristone induced incomplete abortion and explore the mechanisms of action of DFD in treating incomplete abortion.

METHODS:

An incomplete abortion model of rat was established by single intragastrically administered 8.5 mg/kg mifepristone on the 7th day of pregnancy. From the 8th day of pregnancy, the abortive rats were administered solvent, a positive control drug, or different doses of DFD, respectively for seven consecutive days. The efficacy of DFD was assessed by measuring the vaginal bleeding volume of the rats. Four coagulation parameters and platelet counts were measured. Hematoxylin and eosin (HE) staining was performed to evaluate pathological changes in the uterine embryos. Serum levels of progesterone and estrogen were measured using ELISA. Network pharmacology and transcriptomics were used to predict potential targets and pathways for DFD to reduce hemorrhage. The levels of mRNA related to cell adhesion molecules (CAMs) were detected by RT-qPCR. The levels of progesterone and estrogen receptors and the proteins associated with CAMs pathway in uterine tissues were detected by Western Blot.

RESULTS:

DFD significantly reduced the volume of vaginal bleeding of the abortive rats and significantly downgraded the pathological scores of uterine embryos. DFD significantly increased serum levels of E2, and had no impact on serum levels of P4 and the protein expression of ER and PR in the uteri of the abortive rats. Pathways in cancer, lipid, focal adhesion and immune-related signaling were predicted to be influenced by DFD via the analysis of network pharmacology. The CAMs signaling was found the most critical pathway regulated by both mifepristone and DFD via RNA-seq assay, followed by axon guidance, basal cell carcinoma, hippo signaling pathway and neuroactive ligand-receptor interaction. Combining the two analytical methods, ICAM-1 was predicted likely the key targeted gene by DFD. Finally, DFD was validated to decrease the protein expression of ICAM-1, ITGB2, ITGB7 and RASSF5 in the uterine tissues, which correlated to suppress the CAMs signaling pathway.

CONCLUSION:

DFD significantly reduced hemorrhage. DFD significantly increased the serum levels of E2 and inhibited CAMs signaling pathway, which was likely to be involved in the mechanism of action of DFD facilitating residual uterine embryo expulsion in the rat model of incomplete abortion.

245

News (Medical) associated with Estradiol

30 Oct 2024

·www.gene.com

New England Journal of Medicine Publishes Landmark Phase III Results for Genentech’s Itovebi, Showing More Than Doubling of Progression-Free Survival in Certain Type of HR-Positive Advanced Breast Cancer

Wednesday, Oct 30, 2024 ItovebiTM (inavolisib)-based regimen demonstrated a statistically significant and clinically meaningful benefit, reducing the risk of disease worsening or death by 57% compared with palbociclib and fulvestrant alone in the INAVO120 studyThe U.S. FDA recently approved the Itovebi-based regimen as a first-line treatment for people with HR-positive, HER2-negative breast cancer with a PIK3CA mutation, one of the most commonly mutated genes in HR-positive disease South San Francisco, CA -- October 30, 2024 -- Genentech, a member of the Roche Group (SIX: RO, ROG; OTCQX: RHHBY), announced today that a detailed analysis of the positive Phase III INAVO120 results, evaluating ItovebiTM (inavolisib) in combination with palbociclib (Ibrance®) and fulvestrant was published in the New England Journal of Medicine. The U.S. Food and Drug Administration (FDA) recently approved Itovebi in combination with palbociclib and fulvestrant, for the treatment of adults with endocrine-resistant, PIK3CA-mutated, hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer, as detected by an FDA-approved test, following recurrence on or after completing adjuvant endocrine therapy. Data from INAVO120 are also being used for filing submissions to other global health authorities, including the European Medicines Agency. “With a doubling of progression-free survival and consistent benefits in people whose disease had spread to multiple challenging-to-treat locations, including the liver and lungs, these INAVO120 data are significant for patients,” said Komal Jhaveri, M.D., section head for the endocrine therapy research portfolio and clinical director of the early drug development service at Memorial Sloan Kettering Cancer Center and one of the principal investigators of the INAVO120 study. “I’m confident this Itovebi-based regimen could become a new first-line standard of care for this patient population with one of the most commonly mutated genes in metastatic breast cancer, associated with a poor prognosis.” Results showed the Itovebi-based regimen reduced the risk of disease worsening or death (progression-free survival [PFS]) by 57% compared to palbociclib and fulvestrant alone (15.0 months vs. 7.3 months; hazard ratio [HR]=0.43, 95% CI: 0.32-0.59, p<0.001). PFS benefit was consistent across all pre-specified subgroups, including people whose disease had spread to three or more locations, which is characterized as difficult-to-treat disease. Overall survival (OS) data were immature at the time of analysis, but a clear positive trend has been observed (stratified HR=0.64, 95% CI: 0.43-0.97, p=0.03 [boundary of 0.0098]). Follow-up for OS will continue to the next analysis. “Publication of these Phase III results in the New England Journal of Medicine further highlights the transformative potential of the Itovebi-based regimen,” said Levi Garraway, M.D., Ph.D., Genentech’s chief medical officer and head of Global Product Development. “This new treatment exemplifies our ambition to target specific disease pathways more effectively and improve outcomes in people with breast cancer, while also emphasizing the importance of comprehensive testing for mutations like PIK3CA at the time of diagnosis.” The PIK3CA mutation is found in approximately 40% of HR-positive metastatic breast cancers and is associated with a poor prognosis. Historically, the use of PI3K targeted therapy in the first-line advanced setting has been limited and therefore testing for PIK3CA mutations is not common at the time of diagnosis. Early biomarker testing with an FDA-approved test, such as Foundation Medicine’s FoundationOne®Liquid CDx, before first-line treatment is crucial to help identify people who may benefit from targeted therapy, such as Itovebi. Itovebi is currently being investigated in three company-sponsored Phase III clinical studies (INAVO120, INAVO121, INAVO122) in PIK3CA-mutated locally advanced or metastatic breast cancer in various combinations. We are exploring additional studies in breast cancer and other tumor types with the hope of bringing the benefit of this targeted therapy to more people with PIK3CA mutations and addressing patient unmet needs. About the INAVO120 study INAVO120 study [NCT04191499] is a Phase III, randomized, double-blind, placebo-controlled study evaluating the efficacy and safety of Itovebi (inavolisib) in combination with palbociclib and fulvestrant versus placebo plus palbociclib and fulvestrant in people with PIK3CA-mutated, hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer whose disease progressed during treatment or within 12 months of completing adjuvant endocrine therapy and who have not received prior systemic therapy for metastatic disease. The study included 325 patients, who were randomly assigned to either the investigational or control treatment arm. The primary endpoint is progression-free survival, as assessed by investigators, defined as the time from randomization in the clinical trial to the time when the disease progresses, or a patient dies from any cause. Secondary endpoints include overall survival, objective response rate, and clinical benefit rate. Beyond INAVO120, Itovebi is currently being investigated in two additional company-sponsored Phase III clinical studies in PIK3CA-mutated locally advanced or metastatic breast cancer in various combinations: in combination with fulvestrant versus alpelisib plus fulvestrant in HR-positive/HER2-negative breast cancer post cyclin-dependent kinase 4/6 inhibitor and endocrine combination therapy (INAVO121; NCT05646862), and in combination with dual HER2 blockade versus dual HER2 blockade and optional physician's choice of endocrine therapy as a maintenance treatment in HER2-positive disease (INAVO122; NCT05894239). About hormone receptor (HR)-positive breast cancer HR-positive breast cancer is the most prevalent type of all breast cancers, accounting for approximately 70% of cases. A defining feature of HR-positive breast cancer is that its tumor cells have receptors that attach to one or both hormones – estrogen or progesterone – which can contribute to tumor growth. People diagnosed with HR-positive metastatic breast cancer often face the risk of disease progression and treatment side effects, creating a need for additional treatment options. The PI3K signaling pathway is commonly dysregulated in HR-positive breast cancer, often due to activating PIK3CA mutations, which have been identified as a potential mechanism of intrinsic resistance to standard of care endocrine therapy in combination with cyclin-dependent kinase 4/6 inhibitors. What is Itovebi? Itovebi (inavolisib) is a prescription medicine used in combination with the medicines palbociclib and fulvestrant to treat adults who have hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer that has an abnormal phosphatidylinositol-3-kinase catalytic subunit alpha (PIK3CA) gene, and has spread to nearby tissue or lymph nodes (locally advanced), or to other parts of the body (metastatic), and has come back after hormone (endocrine) therapy. Your healthcare provider will test your cancer for abnormal PIK3CA genes to make sure that Itovebi is right for you. It is not known if Itovebi is safe and effective in children. Important Safety Information What are the possible side effects of Itovebi? Itovebi may cause serious side effects, including: High blood sugar levels (hyperglycemia). High blood sugar is common with Itovebi and may be severe. Your healthcare provider will monitor your blood sugar levels before you start and during treatment with Itovebi. Your blood sugar levels may be monitored more often if you have a history of Type 2 diabetes. Your healthcare provider may also ask you to self-monitor and report your blood sugar levels at home. This will be required more frequently in the first 4 weeks of treatment. If you are not sure how to test your blood sugar levels, talk to your healthcare provider. You should stay well-hydrated during treatment with Itovebi. Tell your healthcare provider right away if you develop symptoms of high blood sugar, including: difficulty breathing blurred vision nausea and vomiting (lasting more than 2 hours) unusually increased appetite stomach pain weight loss excessive thirst fruity-smelling breath dry mouth flushed face and dry skin more frequent urination than usual or a higher amount of urine than normal feeling unusually sleepy or tired confusion Mouth sores (stomatitis). Mouth sores are common with Itovebi and may be severe. Tell your healthcare provider if you develop any of the following in your mouth: pain swelling redness ulcers Diarrhea. Diarrhea is common with Itovebi and may be severe. Severe diarrhea can lead to the loss of too much body water (dehydration) and kidney injury. Tell your healthcare provider right away if you develop diarrhea, stomach-area (abdominal pain), or see mucus or blood in your stool during treatment with Itovebi. Your healthcare provider may tell you to drink more fluids or take medicines to treat your diarrhea. Your healthcare provider may tell you to decrease your dose, temporarily stop your treatment, or completely stop your treatment with Itovebi if you develop certain serious side effects. The most common side effects and abnormal blood test results of Itovebi when used in combination with palbociclib and fulvestrant include: decreased white blood cell counts, red blood cell counts, and platelet counts decreased blood levels of calcium, potassium, sodium, and magnesium increased creatinine blood levels tiredness increased blood levels of the liver enzyme alanine transaminase (ALT) nausea rash loss of appetite COVID-19 infection headache Itovebi may affect fertility in males and in females who are able to become pregnant. Talk to your healthcare provider if this is a concern for you. These are not all the possible side effects of Itovebi. Call your healthcare provider for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or http://www.fda.gov/medwatch. You may also report side effects to Genentech at (877) 436-3683. Before you take Itovebi, tell your healthcare provider about all of your medical conditions, including if you: have a history of diabetes or high blood sugar have kidney problems are pregnant or plan to become pregnant. Itovebi can harm your unborn baby. Females who are able to become pregnant: Your healthcare provider will check to see if you are pregnant before you start treatment with Itovebi. You should use effective non-hormonal birth control (contraception) during treatment and for 1 week after your last dose of Itovebi. Talk to your healthcare provider about what birth control method is right for you during this time. Tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with Itovebi. Males with female partners who are able to become pregnant: You should use effective birth control (contraception) during treatment with Itovebi and for 1 week after your last dose. are breastfeeding or plan to breastfeed. It is not known if Itovebi passes into your breastmilk. Do not breastfeed during treatment with Itovebi and for 1 week after your last dose. Talk to your healthcare provider about the best way to feed your baby during treatment with Itovebi. Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Please see additional Important Safety Information in the full Itovebi Prescribing Information or visit https://www.itovebi.com. About Genentech in Breast Cancer Genentech has been advancing breast cancer research for more than 30 years with the goal of helping as many people with the disease as possible. Our medicines, along with companion diagnostic tests, have contributed to bringing breakthrough outcomes in HER2-positive and triple-negative breast cancers. As our understanding of breast cancer biology rapidly improves, we are working to identify new biomarkers and approaches to treatment for other subtypes of the disease, including estrogen receptor-positive breast cancer, which is a form of hormone receptor-positive breast cancer, the most prevalent type of all breast cancers. About Genentech Founded more than 40 years ago, Genentech is a leading biotechnology company that discovers, develops, manufactures and commercializes medicines to treat patients with serious and life-threatening medical conditions. The company, a member of the Roche Group, has headquarters in South San Francisco, California. For additional information about the company, please visit http://www.gene.com. Dr. Jhaveri has financial interests related to Roche and Genentech. All trademarks used or mentioned in this release are protected by law. ###

Clinical ResultPhase 3Drug Approval

25 Oct 2024

·www.globenewswire.com

ANI Pharmaceuticals Announces the FDA Approval and Launch of Estradiol Gel, 0.06%

PRINCETON, N.J., Oct. 25, 2024 (GLOBE NEWSWIRE) -- ANI Pharmaceuticals, Inc. (ANI or the Company) (Nasdaq: ANIP) today announced that following final approval from the U.S. Food and Drug Administration (FDA) for its Abbreviated New Drug Application (ANDA), the Company launched Estradiol Gel, 0.06%. ANI’s Estradiol Gel, 0.06% is the generic version of the reference listed drug (RLD) EstroGel® Gel, 0.06%. "With the FDA approval and commercialization of Estradiol Gel, 0.06%, we are pleased to bring another limited-competition product to market and ensure that customers and patients in need have ready access,” stated Nikhil Lalwani, President and Chief Executive Officer of ANI. U.S. annual sales for Estradiol Gel, 0.06% total approximately $16.7 million, based on August 2024 moving annual total (MAT) IQVIA data. About ANI Pharmaceuticals, Inc. ANI Pharmaceuticals, Inc. (Nasdaq: ANIP) is a diversified biopharmaceutical company serving patients in need by developing, manufacturing, and marketing high-quality branded and generic prescription pharmaceutical products, including for diseases with high unmet medical need. The Company is focused on delivering sustainable growth by scaling up its Rare Disease business through its lead asset Purified Cortrophin® Gel, strengthening its Generics business with enhanced research and development capabilities, delivering innovation in Established Brands, and leveraging its U.S. based manufacturing footprint. For more information, visit www.anipharmaceuticals.com. Forward-Looking Statements This press release contains not only historical information, but also forward-looking statements made pursuant to the safe-harbor provisions of the Private Securities Litigation Reform Act of 1995. These forward-looking statements represent the Company’s expectations or beliefs concerning future events, including statements regarding the benefits of the acquisition of Alimera Sciences. These forward-looking statements generally are identified by the words “believe,” “project,” “expect,” “anticipate,” “estimate,” “intend,” “continue,” “strategy,” “future,” “opportunity,” “plan,” “may,” “should,” “will,” “shall,” “would” other words of similar meaning, derivations of such words and the use of future dates. Forward-looking statements are predictions, projections and other statements about future events that are based on current expectations and assumptions and, as a result, are subject to risks and uncertainties. The following factors, among others, could cause actual results to differ materially from those described in these forward-looking statements: (i) the ability to implement business plans, forecasts, and other expectations in connection with the acquisition and integration of Alimera Sciences, Inc. (“Alimera”) and identify and realize additional opportunities and, in particular, the possibility that the Company is unable to achieve anticipated synergies, (ii) costs and regulatory requirements relating to contract manufacturing arrangements, (iii) costs or delays associated with manufacturing (including the sources and any changes in sources thereof) of the Company’s products, (iv) delays or failures in retaining and obtaining continuing and future product approvals from the FDA, and other regulatory issues relating to the Company's business and products, (v) market trends for the Company’s products, including but not limited to, ILUVIEN, YUTIQ and Cortrophin Gel, and the ability to achieve anticipated sales for such products, (vi) risks that the acquisition of Alimera may disrupt current plans and operations of the Company and potential difficulties of the Company in retaining employees of Alimera and/or maintaining business relationships of Alimera, (vii) the impact of any litigation to which the Company is, or may become, a party, including in connection with the acquisition and integration thereof, (viii) volatility in the Company’s stock price, including as a result of the acquisition, (ix) changes in competitive and regulated industries in which the Company operates, variations in operating performance across competitors, changes in laws and regulations affecting the Company’s business, and changes in the Company’s capital structure as a result of the acquisition, (x) regulatory and other approvals relating to product development and manufacturing, (xi) the Company’s ability, and that of its suppliers, development partners, and manufacturing partners, to comply with laws, regulations and standards that govern or affect the pharmaceutical and biotechnology industries and/or the Company and its products, (xii) costs incurred in connection with the acquisition of Alimera and the possibility that the Company is unable to realize anticipated benefits of the acquisition or to realize estimated pro forma results and underlying assumptions, (xiii) delays in production, increased costs and potential loss of revenues if there is a change in manufacturers or manufacturing processes due to the limited number of suppliers for the Company’s raw materials, active pharmaceutical ingredients, excipients and other materials, (xiv) the Company’s reliance on single source third-party contract manufacturing supply for certain of its key products, including ILUVIEN, YUTIQ and Cortrophin Gel, (xv) changes in policy or actions that may be taken by the FDA, United States Drug Enforcement Administration, and other regulatory agencies, including among other things, drug recalls, regulatory approvals, facility inspections and potential enforcement actions, (xvi) the impact of legislative or regulatory reform on the pricing for the Company’s products, (xvii) the Company’ ability to maintain the services of its key executives and other personnel, and (xviii) general business and economic conditions, such as inflationary pressures, geopolitical conditions including, but not limited to, the conflict between Russia and the Ukraine, the conflict between Israel and Gaza, conflicts related to the attacks on cargo ships in the Red Sea, and the effects and duration of outbreaks of public health emergencies. More detailed information on these and additional factors that could affect the Company’s actual results are described in the Company’s filings with the Securities and Exchange Commission (“SEC”), including its most recent annual report on Form 10-K and quarterly reports on Form 10-Q, as well as other filings with the SEC. All forward-looking statements in this news release speak only as of the date of this news release and are based on the Company’s current beliefs, assumptions, and expectations. The Company undertakes no obligation to update or revise any forward-looking statement, whether as a result of new information, future events or otherwise. Investor Relations:Lisa M. Wilson, In-Site Communications, Inc.T: 212-452-2793E: lwilson@insitecony.com Source: ANI Pharmaceuticals, Inc.

Drug ApprovalAcquisition

24 Oct 2024

·www.biospace.com

Havah Therapeutics Announces Formation of Clinical Advisory Board to Advance Its New Breast Cancer Treatment Approach

Chaired by founder Stephen Birrell, MD PhD, group includes experts in breast cancer biology, endocrine signaling and biomarker-driven risk reduction strategies BOULDER, Colo.--(BUSINESS WIRE)--Havah Therapeutics, a clinical stage biopharmaceutical company developing innovative, proprietary hormonal implant therapies for prevention and treatment of breast cancers, announced the formation of their Clinical Advisory Board Chaired by Havah Therapeutics founder Stephen Birrell, MD, PhD. “The scientific and clinical guidance of this esteemed group will be invaluable as we advance our androgen targeted therapy into late-stage clinical studies for Ductal Carcinoma In-Situ (DCIS) and investigator-sponsored combination studies in more advanced disease,” said, Matthew Brewer, CEO of Havah Therapeutics. Shelley Hwang, MD, MPH, Breast Cancer Research Foundation (BCRF) Investigator and internationally recognized expert in pre-invasive disease and DCIS, added: “I am thrilled to be involved with Havah Therapeutics at this critical stage of their development. Insights gained from their ongoing Phase 2 study ( RECAST DCIS ), coupled with my experience as the principal investigator of the COMET Study , will potentially enable the company’s androgen receptor targeting therapy to provide a much needed treatment alternative to invasive surgery and radiation treatment.” The members of Havah Therapeutics’ Clinical Advisory Board include: Stephen Birrell, MD, PhD (Chair), is founder of Havah Therapeutics and Chief Medical Officer of Wellend Health, an Australia-wide clinic that specializes in breast hormone-health, women at high-risk breast cancer and clinical trials. He is a Clinical Affiliate academic at the University of Adelaide Dame Roma Mitchell Cancer Research Laboratories. Shelley Hwang, MD, MPH is the Mary and Deryl Hart Distinguished Professor of Surgical Oncology and Radiology, Vice Chair of Research and Disease Group Leader for the Breast Cancer Program at Duke University Comprehensive Cancer Center. Her research focus includes breast cancer prevention, identifying less invasive treatments for early-stage breast cancers including DCIS and addressing and mitigating health care disparities in breast cancer. Seema A. Khan, MD is Professor of Surgery in the Feinberg School of Medicine at Northwestern University, and the Bluhm Family Professor of Cancer Research. She is the Co-Leader of the Cancer Prevention Research Program at the Robert H. Lurie Comprehensive Cancer Center. Her research focuses on applying biomarker knowledge to improve breast cancer risk stratification and develop preventive interventions for high-risk women. Her research is funded by the National Institutes of Health, The Breast Cancer Research Foundation, the Avon Foundation, and the Susan G. Komen Foundation Professor Wayne Tilley, PhD is the Inaugural Director of the Dame Roma Mitchell Cancer Research Laboratories, University of Adelaide. He completed a Fellowship at UT Southwestern in Dallas Texas in the late 1980s where he was one of the first to clone the human androgen receptor (AR) with Professor Jean Wilson, MD. A current major research focus of Professor Tilley’s lab is the development of new treatments for breast cancer that stimulate the tumor suppressive activity of the AR in the breast (Nature Medicine 2021; Lancet Oncology 2024) to counter the proliferative effects of estrogen. Additional background information on the CAB members can be found on the company’s website: About RECAST DCIS Havah Therapeutics is currently participating in the Re-Evaluating Conditions for Active Surveillance Suitability as Treatment: Ductal Carcinoma In Situ (RECAST DCIS), a Phase 2 platform study aimed at preventing the progression of DCIS to breast cancer. Havah Therapeutics’ HAVAH T+Ai™, a proprietary combination of testosterone (T) and anastrozole (Ai) that targets the androgen and estrogen receptor pathways, is being evaluated alongside two other endocrine therapy arms. About Havah Therapeutics Havah Therapeutics is developing a novel therapeutic implant for treating hormonally sensitive cancers and other breast conditions. This groundbreaking method relies on stimulating (agonizing) the androgen receptor in breast tissue, utilizing natural hormonal mechanisms to treat patients safely and with greatly reduced side effects. The product is a combination of two registered agents (testosterone and anastrozole, a low dose aromatase inhibitor) that when dosed, provides three months of continuous medication enabling a superior product pro compliance, safety and efficacy. For more information, visit . Contacts Media Contacts: Matthew Brewer mb@havahtx.com Danielle Clark-Brown dcb@havahtx.com

Phase 2Radiation Therapy

100 Deals associated with Estradiol

External Link

KEGG	Wiki	ATC	Drug Bank
D00105	Estradiol	G03CA03	DB00783

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Infertility	JP	Fuji Pharma Co., Ltd.	11 Mar 2022
Ovarian Stimulations	JP	Bayer Yakuhin Ltd.	11 Mar 2022
Dyspareunia	US	Mayne Pharma Ltd.	29 May 2018
Oestrogen deficiency	JP	Orion Corp	21 Sep 2007
Female Urogenital Diseases	JP	Hisamitsu Pharmaceutical Co., Inc.	01 Oct 1999
Hot Flashes	JP	Hisamitsu Pharmaceutical Co., Inc.	01 Oct 1999
Hypogonadism	JP	Hisamitsu Pharmaceutical Co., Inc.	01 Oct 1999
Atrophic Vaginitis	US	Novo Nordisk, Inc.	26 Mar 1999
Osteoporosis, Postmenopausal	US	AbbVie, Inc.	20 Dec 1996
Urogenital Diseases	US	Pfizer Inc.	26 Apr 1996
Hypoestrogenism	US	Bayer HealthCare	22 Dec 1994
Uterine Hemorrhage	US	Bayer HealthCare	22 Dec 1994
Vulvovaginal atrophy	US	Bayer HealthCare	22 Dec 1994
Vasomotor symptom	US	Bayer HealthCare	22 Dec 1994

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Postmenopausal atrophic vaginitis	Phase 3	US	Novo Nordisk A/S	01 Mar 2005
Postmenopausal atrophic vaginitis	Phase 3	CA	Novo Nordisk A/S	01 Mar 2005
Menopausal symptoms	Phase 3	AT	Novo Nordisk A/S	28 May 2004
Menopausal symptoms	Phase 3	BE	Novo Nordisk A/S	28 May 2004
Menopausal symptoms	Phase 3	DK	Novo Nordisk A/S	28 May 2004
Menopausal symptoms	Phase 3	FI	Novo Nordisk A/S	28 May 2004
Menopausal symptoms	Phase 3	FR	Novo Nordisk A/S	28 May 2004
Menopausal symptoms	Phase 3	DE	Novo Nordisk A/S	28 May 2004
Menopausal symptoms	Phase 3	NO	Novo Nordisk A/S	28 May 2004
Menopausal symptoms	Phase 3	SE	Novo Nordisk A/S	28 May 2004

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03332303 (CTgov)	Phase 3	Vulvovaginal atrophy	540	Estradiol Vaginal Cream (Experimental: Estradiol Vaginal Cream, USP, 0.01% (Prasco LLC))	yliohrjcbg(mebqkphwfl) = uajoudgcpd eequnuoaqm (xbcsrqznpr, bisxiglkqm - zdmtaoqvsw) View more	-	30 May 2024
				Estrace® Cream (Active Comparator: Estrace® Cream)	yliohrjcbg(mebqkphwfl) = ychgemhiwt eequnuoaqm (xbcsrqznpr, mkxivmsckk - ojbywocbwv) View more
NCT00268476 \| NCT00303784 (PATCH and STAMPEDE, Pubmed)	Phase 3	Prostatic Cancer testosterone \| oestrogen	-	Transdermal oestrogen (tE2) patches	fziwasruhy(qocepuqqhn) = Rates of androgen suppression with tE2 were equivalent to LHRHa takvaxhhya (boxckrxjom ) View more	Positive	01 Jan 2024
				Luteinising hormone releasing hormone analogues (LHRHa)
NCT04051320 (CTgov)	Phase 2	Depression, Postpartum \| Irritable Mood	23	Micronized progesterone+Leuprolide Acetate 3.75 MG/ML+Estradiol 2 Mg tablet (Hormone Sensitive Women (HS+))	icvnbnuwcq(zuvkmwkwyg) = fbrujvpcxf dlpkboqxyx (wdteyermkk, lihchdaocw - rrfdzurubv) View more	-	25 Aug 2023
				Micronized progesterone+Leuprolide Acetate 3.75 MG/ML+Estradiol 2 Mg tablet (Hormone Insensitive Women (HS-))	icvnbnuwcq(zuvkmwkwyg) = wxoagnapec dlpkboqxyx (wdteyermkk, kybywwmjvv - yrxcfnjntk) View more
ARVO2023	Not Applicable	17-β estradiol	-	17-β estradiol	pycxysoklq(vckpdcfvxq) = kvonmjjwqg jbviimxphn (iohdpkngin, 17.8)	-	01 Jun 2023
NCT03943823 (CTgov)	Phase 4	Vaginal Discharge \| Bacterial Vaginosis	4	Premarin+Estrace (Estrogen Vaginal Cream)	aruqasmymq(dgcoukwxxb) = pjwwtrozpw aipjfxkdbv (hetqsnzuiw, kcuihaknow - ydcdsxamcv) View more	-	01 Mar 2023
				Trimo-San vaginal gel (Trimo-San Vaginal Gel)	aruqasmymq(dgcoukwxxb) = oruovugtzd aipjfxkdbv (hetqsnzuiw, htuoiafstf - vfhubccwwa) View more
ChiCTR1900022110 (Pubmed)	Phase 4	Intrauterine adhesions	78	Transdermal gel	uvqworosht(hadyquerct) = wnopwyfkrd efzaypbdxl (hqjmrvvsql )	-	01 Jan 2023
				Estradiol valerate oral tablet	uvqworosht(hadyquerct) = wpcrbiyswo efzaypbdxl (hqjmrvvsql )
NCT02516202 (Pubmed)	Phase 3	Menopausal symptoms \| Vaginal Diseases \| Dyspareunia	174	Vaginal estradiol tablet (10 μg/d for 2 weeks and then twice weekly)	fuozpmhule(vkmdmuhwbh) = ryxsarhpgk lznouwhyii (fsoknbqqov, 2.2)	-	01 Nov 2022
				Dual placebo	fuozpmhule(vkmdmuhwbh) = dfakehocgp lznouwhyii (fsoknbqqov, 2.1)
NCT03498313 (CLEAR-2, CTgov)	Phase 4	Suicidal Ideation	60	Placebo+estradiol (Transdermal Estradiol + Placebo)	ysaxevfdiv(foueqktugk) = sfjhxgmrgh nomvletpjy (krcunfmiwh, epcvpkcrqi - optwqjdvmw) View more	-	14 Sep 2022
				Oral Micronized Progesterone + Placebo (Oral Micronized Progesterone + Placebo)	ysaxevfdiv(foueqktugk) = rotsoegkjb nomvletpjy (krcunfmiwh, odpwacvypq - heviwcxtxu) View more
NCT01418209 (Pubmed)	Not Applicable	Vasomotor symptom	171	Low-dose oral estradiol	isnslznegb(ivktqootcs) = oqfehtvmwy gajnahxwgf (btbhopxspv ) View more	-	16 Aug 2022

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