更新于：2023-09-22

Arzoxifene Hydrochloride

盐酸阿佐昔芬

更新于：2023-09-22

概要

概要

基本信息

药物类型

小分子化药

别名

Arzoxifene、Arzoxifene hydrochloride (USAN)、SERM III

+ [4]

靶点

ER(雌激素受体家族)

作用机制

ERs调节剂(雌激素受体家族调节剂)

治疗领域

肿瘤、消化系统疾病、内分泌与代谢疾病+ [2]

在研适应症-

非在研适应症

乳腺癌、子宫内膜癌、骨质疏松症+ [3]

原研机构

Eli Lilly & Co.

在研机构-

非在研机构

Eli Lilly & Co.

最高研发状态(全球)终止临床3期

首次获批日期(全球)-

最高研发状态(中国)无进展

特殊审评-

结构

分子式C28H30ClNO4S

InChIKeyNHSNLUIMAQQXGR-UHFFFAOYSA-N

CAS号182133-27-3

关联

项与盐酸阿佐昔芬相关的临床试验

NCT00767299 / Completed临床2期

Effects of Arzoxifene on Bone Mineral Density in Korean Postmenopausal Women With Osteoporosis

The study is for Korean women who are postmenopausal and also suffer from osteoporosis.
The study will test if women who are given 20 mg of arzoxifene once a day for six months have a less severe level of osteoporosis than those women who do not take arzoxifene.
All patients will receive 500 mg of elemental calcium and 400 to 600 IU Vitamin D daily starting 4 weeks prior to study drug administration continuing through the 6 months of therapy.

开始日期2008-12-31

申办/合作机构

Eli Lilly & Co.

NCT00383422 / Completed临床3期

The Comparison of the Efficacy and Safety of Arzoxifene Versus Raloxifene in Postmenopausal Women With Osteoporosis

The purpose of this study is to compare the effect of arzoxifene to raloxifene on the bone mineral density (bone strength).

开始日期2006-10-31

申办/合作机构

Eli Lilly & Co.

EUCTR2006-001987-22-ES / Not yet recruiting临床3期

Comparación de la Eficacia y Seguridad de Arzoxifeno frente a Raloxifeno en mujeres posmenopáusicas con Osteoporosis”The Comparison of the Efficacy and Safety of Arzoxifene versus Raloxifene in Postmenopausal Women with Osteoporosis - GJAR

开始日期2006-09-28

申办/合作机构

Lilly SA

100 项与盐酸阿佐昔芬相关的专利（医药）

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124

项与盐酸阿佐昔芬相关的文献（医药）

2022-09-27·The Cochrane database of systematic reviews

Aromatase inhibitors (letrozole) for ovulation induction in infertile women with polycystic ovary syndrome.

Review

作者: Sebastian Franik ; Quang-Khoi Le ; Jan Am Kremer ; Ludwig Kiesel ; Cindy Farquhar

BACKGROUND:

Polycystic ovary syndrome (PCOS) is the most common cause of infrequent periods (oligomenorrhoea) and absence of periods (amenorrhoea). It affects about 5% to 20% of women worldwide and often leads to anovulatory infertility. Aromatase inhibitors (AIs) are a class of drugs that were introduced for ovulation induction in 2001. Since about 2001 clinical trials have reached differing conclusions as to whether the AI, letrozole, is at least as effective as the first-line treatment clomiphene citrate (CC), a selective oestrogen receptor modulator (SERM).

OBJECTIVES:

To evaluate the effectiveness and safety of AIs (letrozole) (with or without adjuncts) compared to SERMs (with or without adjuncts) for infertile women with anovulatory PCOS for ovulation induction followed by timed intercourse or intrauterine insemination.

SEARCH METHODS:

We searched the following sources, from their inception to 4 November 2021, to identify relevant randomised controlled trials (RCTs): the Cochrane Gynaecology and Fertility Group Specialised Register, CENTRAL, MEDLINE, Embase and PsycINFO. We also checked reference lists of relevant trials, searched the trial registers and contacted experts in the field for any additional trials. We did not restrict the searches by language or publication status.

SELECTION CRITERIA:

We included all RCTs of AIs used alone or with other medical therapies for ovulation induction in women of reproductive age with anovulatory PCOS.

DATA COLLECTION AND ANALYSIS:

Two review authors independently selected trials, extracted the data and assessed risks of bias using RoB 1. We pooled trials where appropriate using a fixed-effect model to calculate odds ratios (ORs) and 95% confidence intervals (CIs) for most outcomes, and risk differences (RDs) for ovarian hyperstimulation syndrome (OHSS). The primary outcomes were live birth rate and OHSS rate. Secondary outcomes were clinical pregnancy, miscarriage and multiple pregnancy rates. We assessed the certainty of the evidence for each comparison using GRADE methods.

MAIN RESULTS:

This is a substantive update of a previous review; of six previously included trials, we excluded four from this update and moved two to 'awaiting classification' due to concerns about validity of trial data. We included five additional trials for this update that now includes a total of 41 RCTs (6522 women). The AI, letrozole, was used in all trials. Letrozole compared to SERMs with or without adjuncts followed by timed intercourse Live birth rates were higher with letrozole (with or without adjuncts) compared to SERMs followed by timed intercourse (OR 1.72, 95% CI 1.40 to 2.11; I² = 0%; number needed to treat for an additional beneficial outcome (NNTB) = 10; 11 trials, 2060 participants; high-certainty evidence). This suggests that in women with a 20% chance of live birth using SERMs, the live birth rate in women using letrozole with or without adjuncts would be 27% to 35%. There is high-certainty evidence that OHSS rates are similar with letrozole or SERMs (0.5% in both arms: risk difference (RD) -0.00, 95% CI -0.01 to 0.01; I² = 0%; 10 trials, 1848 participants; high-certainty evidence). There is evidence for a higher pregnancy rate in favour of letrozole (OR 1.69, 95% CI 1.45 to 1.98; I² = 0%; NNTB = 10; 23 trials, 3321 participants; high-certainty evidence). This suggests that in women with a 24% chance of clinical pregnancy using SERMs, the clinical pregnancy rate in women using letrozole with or without adjuncts would be 32% to 39%. There is little or no difference between treatment groups in the rate of miscarriage per pregnancy (25% with SERMs versus 24% with letrozole: OR 0.94, 95% CI 0.66 to 1.32; I² = 0%; 15 trials, 736 participants; high-certainty evidence) and multiple pregnancy rate (2.2% with SERMs versus 1.6% with letrozole: OR 0.74, 95% CI 0.42 to 1.32; I² = 0%; 14 trials, 2247 participants; high-certainty evidence). However, a funnel plot showed mild asymmetry, indicating that some trials in favour of SERMs might be missing. Letrozole compared to laparoscopic ovarian drilling (LOD) One trial reported very low-certainty evidence that live birth rates may be higher with letrozole compared to LOD (OR 2.07, 95% CI 0.99 to 4.32; 1 trial, 141 participants; very low-certainty evidence). This suggests that in women with a 22% chance of live birth using LOD with or without adjuncts, the live birth rate in women using letrozole with or without adjuncts would be 24% to 47%. No trial reported OHSS rates. Due to the low-certainty evidence we are uncertain if letrozole improves pregnancy rates compared to LOD (OR 1.47, 95% CI 0.95 to 2.28; I² = 0%; 3 trials, 367 participants; low-certainty evidence). This suggests that in women with a 29% chance of clinical pregnancy using LOD with or without adjuncts, the clinical pregnancy rate in women using letrozole with or without adjuncts would be 28% to 45%. There seems to be no evidence of a difference in miscarriage rates per pregnancy comparing letrozole to LOD (OR 0.65, 95% CI 0.22 to 1.92; I² = 0%; 3 trials, 122 participants; low-certainty evidence). This also applies to multiple pregnancies (OR 3.00, 95% CI 0.12 to 74.90; 1 trial, 141 participants; very low-certainty evidence).

AUTHORS' CONCLUSIONS:

Letrozole appears to improve live birth rates and pregnancy rates in infertile women with anovulatory PCOS, compared to SERMs, when used for ovulation induction, followed by intercourse. There is high-certainty evidence that OHSS rates are similar with letrozole or SERMs. There was high-certainty evidence of no difference in miscarriage rate and multiple pregnancy rate. We are uncertain if letrozole increases live birth rates compared to LOD. In this update, we added good quality trials and removed trials with concerns over data validity, thereby upgrading the certainty of the evidence base.

2022-01-01·Frontiers in endocrinology3区 · 医学

27-Hydroxycholesterol, The Estrogen Receptor Modulator, Alters DNA Methylation in Breast Cancer.

3区 · 医学

ArticleOA

作者: Ravindran Vini ; Arumugam Rajavelu ; Sreeja Sreeharshan

27-hydroxycholesterol (27-HC) is the first known endogenous selective estrogen receptor modulator (SERM), and its elevation from normal levels is closely associated with breast cancer. A plethora of evidence suggests that aberrant epigenetic signatures in breast cancer cells can result in differential responses to various chemotherapeutics and often leads to the development of resistant cancer cells. Such aberrant epigenetic changes are mostly dictated by the microenvironment. The local concentration of oxygen and metabolites in the microenvironment of breast cancer are known to influence the development of breast cancer. Hence, we hypothesized that 27-HC, an oxysterol, which has been shown to induce breast cancer progression via estrogen receptor alpha (ERα) and liver X receptor (LXR) and by modulating immune cells, may also induce epigenetic changes. For deciphering the same, we treated the estrogen receptor-positive cells with 27-HC and identified DNA hypermethylation on a subset of genes by performing DNA bisulfite sequencing. The genes that showed significant DNA hypermethylation were phosphatidylserine synthase 2 (PTDSS2), MIR613, indoleamine 2,3-dioxygenase 1 (IDO1), thyroid hormone receptor alpha (THRA), dystrotelin (DTYN), and mesoderm induction early response 1, family member 3 (MIER). Furthermore, we found that 27-HC weakens the DNMT3B association with the ERα in MCF-7 cells. This study reports that 27-HC induces aberrant DNA methylation changes on the promoters of a subset of genes through modulation of ERα and DNMT3B complexes to induce the local DNA methylation changes, which may dictate drug responses and breast cancer development.

2022-01-01·Frontiers in endocrinology3区 · 医学

Water Extract of Rhizoma Drynaria Selectively Exerts Estrogenic Activities in Ovariectomized Rats and Estrogen Receptor-Positive Cells.

3区 · 医学

ArticleOA

作者: Liping Zhou ; Ka-Ying Wong ; Christina Chui-Wa Poon ; Wenxuan Yu ; Huihui Xiao ; Chi-On Chan ; Daniel Kam-Wah Mok ; Man-Sau Wong

Our previous study demonstrated that the bone protective actions of herbal medicine Rhizoma Drynariae (Gusuibu, RD) were mainly mediated by flavonoid phytoestrogens via estrogen receptors, raising concerns about the safety of using RD as it may induce estrogen-like risk-benefit profile and interact with other ER ligands, such as selective estrogen receptor modulators (SERMs), when coadministered. The present study evaluated the estrogenic activities of RD and its potential interaction with tamoxifen, a SERM, in estrogen-sensitive tissues by using mature ovariectomized (OVX) rats and ER-positive cells. Similar to but weaker than tamoxifen, RD at its clinical dose dramatically ameliorated OVX-induced changes in bone and dopamine metabolism-related markers in OVX rats. However, tamoxifen, but not RD, induced uterotrophic effects. No significant alteration in mammary gland was observed in OVX rats treated with RD, which was different from the inhibitory actions of tamoxifen. The two-way ANOVA results indicated the interactions between RD and tamoxifen in the bone, brain, and uterus of OVX rats while RD did not alter their responses to tamoxifen. Our results demonstrate that RD selectively exerts estrogenic actions in a different manner from tamoxifen. Moreover, RD interacts with tamoxifen without altering its effects in OVX rats.

项与盐酸阿佐昔芬相关的新闻（医药）

2022-09-14

·BioSpace

Sermonix Pharmaceuticals Shares Details of First-Ever Known Durable Complete Clinical Response in a Metastatic ER+/HER2- Breast Cancer Patient With an ESR1 Mutation After Prior CDK4/6 Inhibitor Treatment

Presentation delivered at the ninth-annual Metastatic Breast Cancer Research Conference in Park City, Utah Case was reported during Phase 2 study investigating efficacy of lasofoxifene, Sermonix’s lead investigational drug COLUMBUS, Ohio, Sept. 14, 2022 (GLOBE NEWSWIRE) -- Sermonix Pharmaceuticals LLC, a privately held biopharmaceutical company developing innovative therapeutics to specifically treat ESR1-mutated metastatic breast and gynecological cancers, broadly shared a case report detailing the first-ever known finding of a durable complete response that could be characterized as complete clinical remission in a metastatic estrogen receptor-positive (ER+)/HER2- breast cancer patient with an ESR1 mutation after prior CDK4/6 inhibitor treatment upon participation in any single-agent hormonally based therapy. The case report, “Durable Complete Remission of Metastatic ER+/HER2- Breast Cancer After Lasofoxifene Therapy,” was initially shared Sept. 9 at the ninth-annual Metastatic Breast Cancer Research Conference in Park City, Utah. Lasofoxifene is Sermonix’s lead investigational drug. The durable complete response (CR) was reported during Sermonix’s Phase 2 Evaluation of Lasofoxifene in ESR1 Mutations (ELAINE 1, NCT03781063) study. The open-label, randomized study evaluated the efficacy of oral lasofoxifene versus intramuscular fulvestrant for the treatment of postmenopausal women with locally advanced or metastatic ER+/HER2- breast cancer with an ESR1 mutation and progression-free survival as the primary endpoint. Top-line ELAINE 1 data was presented Sept. 10 during the European Society for Medical Oncology (ESMO) Congress 2022 in Paris. Although not statistically significant, the results of the study numerically favored lasofoxifene. The patient was recruited to the ELAINE 1 study and started treatment on Dec. 16, 2020. Her first radiological assessment, eight weeks after lasofoxifene initiation via PET-FDG scan, revealed no pathological uptake in her pleural lesions, a sum diameter of 14 mm (55% reduction) and significant reduction of the bony lesion in the ilium with no new pathological findings. Scans at Week 16 revealed further improvement up to complete radiological disappearance of all measurable and non-measurable lesions. Radiological complete response was maintained at 80 weeks (June 29, 2022). “Achieving a complete response in metastatic breast cancer with endocrine treatment post CDK4/6 inhibitor is exceedingly uncommon, particularly with single-agent endocrine therapy,” said Dr. Einav Nili Gal-Yam, M.D., Ph.D., ELAINE 1 principal investigator and head of the Breast Oncology Institute at Chaim Sheba Medical Center in Ramat Gan, Israel. “This is a very gratifying result, pointing to lasofoxifene’s potentially significant role in addressing the unmet needs of patients with ESR1 mutations. We look forward to the continued clinical development of this drug.” About Lasofoxifene Lasofoxifene is an investigational, nonsteroidal selective estrogen receptor modulator (SERM), which Sermonix licensed globally from Ligand Pharmaceuticals Inc. (NASDAQ: LGND) and has been studied in previous comprehensive Phase 1-3 non-oncology clinical trials in more than 15,000 postmenopausal women worldwide. Lasofoxifene’s bioavailability and activity in mutations of the estrogen receptor could potentially hold promise for patients who have acquired endocrine resistance due to ESR1 mutations, a common finding in the metastatic setting and an area of high unmet medical need. Lasofoxifene’s novel activity in ESR1 mutations was discovered at Duke University and Sermonix has exclusive rights to develop and commercialize the product in this area. Lasofoxifene, a potent, oral SERM could, if approved, play a critical role in the targeted precision medicine treatment of advanced ER+ breast cancer. About Sermonix Sermonix Pharmaceuticals Inc. is a privately held biopharmaceutical company focused on the development of female-specific oncology products and is currently undertaking two Phase 2 clinical studies of lasofoxifene, its lead investigational drug. Sermonix Pharmaceuticals was founded in 2014 by David Portman, M.D., a leading clinical researcher and expert in women’s health, menopause and selective estrogen receptor modulator (SERM) therapy. The Sermonix management team, led by Dr. Portman, has significant experience in all stages of the drug development and regulatory process. Paul Plourde, M.D., vice president of oncology clinical development, has many decades of experience in the oncology drug development arena. Barry Komm, Ph.D., chief scientific officer, is recognized for his expertise in SERM biology. Miriam Portman, M.D., is chief operating officer. Elizabeth Attias, M.M.Sc., Sc.D., chief strategy and development officer, has extensive experience in pharmaceutical drug commercialization. Simon Jenkins, Ph.D., vice president of operations, has over 30 years of experience in global drug development leadership. Sermonix non-executive chairman of the board is Anthony Wild, Ph.D., former president of both Parke-Davis Pharmaceuticals and Warner-Lambert’s Pharmaceutical Division. Learn more at SermonixPharma.com. Contact information: Glenn Garmont LifeSci Advisors Managing Director, Investor Relations Corporate Communications ggarmont@lifesciadvisors.com 646-876-5521

小分子药物

2022-09-13

·BioSpace

Sermonix Pharmaceuticals Announces Results of Phase 2 Study of Lasofoxifene vs. Fulvestrant in Postmenopausal Women With Locally Advanced or Metastatic ER+/HER2- Breast Cancer and an ESR1 Mutation

COLUMBUS, Ohio, Sept. 13, 2022 (GLOBE NEWSWIRE) -- Sermonix Pharmaceuticals LLC, a privately held biopharmaceutical company developing innovative therapeutics to specifically treat ESR1-mutated metastatic breast and gynecological cancers, today announced results of its signal-seeking Evaluation of Lasofoxifene in ESR1 Mutations (ELAINE 1) Phase 2 study. The results were initially shared Sept. 10 during a late-breaking oral presentation at the European Society for Medical Oncology (ESMO) Congress 2022 in Paris. The open-label ELAINE 1 (NCT03781063) study began U.S. enrollment in September 2019, assessing the efficacy and safety of oral lasofoxifene versus intramuscular fulvestrant, a selective estrogen receptor degrader (SERD), in 103 patients. All participants were post-CDK4/6 inhibitor/aromatase inhibitor therapy and had an ESR1 mutation. Progression-free survival was the primary endpoint. Top-line data included: Median progression-free survival (PFS) was 6.04 mos. (95% CI, 2.82–8.04) for lasofoxifene vs. 4.04 mos. (95% CI, 2.93–6.04) for fulvestrant, P=0.138 (HR, 0.699 [95% CI, 0.445–1.125]) Clinical benefit rate (CBR) was 36.5% for lasofoxifene vs. 21.6% for fulvestrant, P=0.12. CBR is defined as the percentage of all subjects with a complete or partial response; or stable disease for >/= 24 weeks Objective response rate was 13.2% for lasofoxifene vs. 2.9% for fulvestrant, P=0.12, with 1 confirmed complete response (CR) (72-week duration) and 4 confirmed partial responses (PR) in the lasofoxifene arm vs. 1 PR in the fulvestrant arm PFS was numerically and consistently greater with lasofoxifene vs. fulvestrant when visceral metastasis and/or Y537S ESR1 mutation subgroups were analyzed While not reaching statistical significance in this 103-patient study, all endpoints numerically favored lasofoxifene Exploratory endpoints included: PFS at 6 mos. for lasofoxifene was 53.4% vs. 37.9% for fulvestrant; PFS at 12 mos. was 30.7% for lasofoxifene vs. 14.1% for fulvestrant Clearance of ctDNA also favored lasofoxifene over fulvestrant Most common adverse events were fatigue, nausea, arthralgias and hot flashes; most were Grade 1/2. No thrombotic events occurred ELAINE 1 is the first clinical trial comparing lasofoxifene with fulvestrant in ESR1-mutated metastatic breast cancer patients with progression on an aromatase inhibitor (Al) in combination with a CDK4/6 inhibitor, and the first to demonstrate anti-tumor activity and target engagement of a novel selective estrogen receptor modulator (SERM) in this setting. ELAINE 2, a Phase 2 single-arm trial of lasofoxifene in combination with the CDK4/6 inhibitor abemaciclib, showed efficacy in heavily pretreated patients with ESR1-mutated mBC post-CDK4/6i (ASCO 2022). “Sermonix is pleased with the outcomes reported in our ELAINE 1 trial comparing lasofoxifene with fulvestrant, suggesting lasofoxifene’s anti-tumor activity and potential to play a critical role in the targeted precision medicine treatment of ESR1-mutated advanced ER+ breast cancer,” said Dr. David Portman, Sermonix founder and chief executive officer. “Lasofoxifene following endocrine/CDK4/6 inhibitor therapies continues to be studied and we anticipate efficacy will be confirmed in a larger clinical study. Sermonix is planning a Phase 3 registrational combination study based on these results as well as encouraging efficacy and safety demonstrated in the ELAINE 2 study of lasofoxifene and abemaciclib reported at this year’s ASCO annual meeting.” “ELAINE 1 suggested lasofoxifene's activity in patients with metastatic breast cancer post-CDK4/6i and an ESR1 mutation,” said Dr. Paul Plourde, Sermonix vice president for clinical oncology development. “While not reaching statistical significance in our modestly powered study, all efficacy parameters numerically favored lasofoxifene over fulvestrant. Moreover, the safety pro lasofoxifene was well tolerated with few Grades 3 and 4 adverse events and a differentiated pro injectable and oral SERDs. Lasofoxifene trials may offer new hope for patients with mutated ESR1 metastatic breast cancer.” About Lasofoxifene Lasofoxifene is an investigational, nonsteroidal selective estrogen receptor modulator (SERM), which Sermonix licensed globally from Ligand Pharmaceuticals Inc. (NASDAQ: LGND) and has been studied in previous comprehensive Phase 1-3 non-oncology clinical trials in more than 15,000 postmenopausal women worldwide. Lasofoxifene’s bioavailability and activity in mutations of the estrogen receptor could potentially hold promise for patients who have acquired endocrine resistance due to ESR1 mutations, a common finding in the metastatic setting and an area of high unmet medical need. Lasofoxifene’s novel activity in ESR1 mutations was discovered at Duke University and Sermonix has exclusive rights to develop and commercialize the product in this area. Lasofoxifene, a potent, oral SERM could, if approved, play a critical role in the targeted precision medicine treatment of advanced ER+ breast cancer. About Sermonix Sermonix Pharmaceuticals Inc. is a privately held biopharmaceutical company focused on the development of female-specific oncology products and is currently undertaking two Phase 2 clinical studies of lasofoxifene, its lead investigational drug. Sermonix Pharmaceuticals was founded in 2014 by David Portman, M.D., a leading clinical researcher and expert in women’s health, menopause and selective estrogen receptor modulator (SERM) therapy. The Sermonix management team, led by Dr. Portman, has significant experience in all stages of the drug development and regulatory process. Paul Plourde, M.D., vice president of oncology clinical development, has many decades of experience in the oncology drug development arena. Barry Komm, Ph.D., chief scientific officer, is recognized for his expertise in SERM biology. Miriam Portman, M.D., is chief operating officer. Elizabeth Attias, M.M.Sc., Sc.D., chief strategy and development officer, has extensive experience in pharmaceutical drug commercialization. Simon Jenkins, Ph.D., vice president of operations, has over 30 years of experience in global drug development leadership. Sermonix non-executive chairman of the board is Anthony Wild, Ph.D., former president of both Parke-Davis Pharmaceuticals and Warner-Lambert’s Pharmaceutical Division. Learn more at SermonixPharma.com. Contact information: Glenn Garmont LifeSci Advisors Managing Director, Investor Relations Corporate Communications ggarmont@lifesciadvisors.com 646-876-5521

小分子药物ASCO会议

2022-08-25

·BioSpace

Sermonix Pharmaceuticals Announces Top-Line Data From ELAINE 1 Phase 2 Study of Lasofoxifene Versus Fulvestrant Is Accepted for a Late-Breaking Oral Presentation at ESMO Congress 2022

COLUMBUS, Ohio, Aug. 25, 2022 (GLOBE NEWSWIRE) -- Sermonix Pharmaceuticals LLC, a privately held biopharmaceutical company developing innovative therapeutics to specifically treat ESR1-mutated metastatic breast and gynecological cancers, today announced that top-line data from its Phase 2 study of lasofoxifene, its lead investigational drug, versus fulvestrant was accepted for a late-breaking oral presentation at the European Society for Medical Oncology (ESMO) Congress 2022, which is being held September 9-13, 2022, in Paris. The open-label, randomized Evaluation of Lasofoxifene in ESR1 Mutations (ELAINE 1, NCT03781063) study, which began U.S. enrollment in September 2019, assessed the efficacy of oral lasofoxifene versus intramuscular fulvestrant for the treatment of postmenopausal women with locally advanced or metastatic estrogen receptor-positive (ER+)/HER2- breast cancer with an ESR1 mutation and progression-free survival as the primary endpoint. Details of the presentation are as follows: Title: Open-label, randomized study of lasofoxifene (LAS) vs fulvestrant (Fulv) for women with locally advanced/metastatic ER+/HER2- breast cancer (mBC), an estrogen receptor 1 (ESR1) mutation, and disease progression on aromatase (AI) and cyclin-dependent kinase 4/6 (CDK4/6i) inhibitors Presenter: Matthew P. Goetz Date, Time and Location: September 10 at 3:05 p.m. CEST, 7.2.E - Évry Auditorium Session: Mini Oral Session: breast cancer, metastatic Presentation Number: LBA20 About Lasofoxifene Lasofoxifene is an investigational, nonsteroidal selective estrogen receptor modulator (SERM), which Sermonix licensed globally from Ligand Pharmaceuticals Inc. (NASDAQ: LGND) and has been studied in previous comprehensive Phase 1-3 non-oncology clinical trials in more than 15,000 postmenopausal women worldwide. Lasofoxifene’s bioavailability and activity in mutations of the estrogen receptor could potentially hold promise for patients who have acquired endocrine resistance due to ESR1 mutations, a common finding in the metastatic setting and an area of high unmet medical need. Lasofoxifene’s novel activity in ESR1 mutations was discovered at Duke University and Sermonix has exclusive rights to develop and commercialize the product in this area. Lasofoxifene, a potent, oral SERM could, if approved, play a critical role in the targeted precision medicine treatment of advanced ER+ breast cancer. About Sermonix Sermonix Pharmaceuticals Inc. is a privately held biopharmaceutical company focused on the development of female-specific oncology products and is currently undertaking two Phase 2 clinical studies of lasofoxifene, its lead investigational drug. Sermonix Pharmaceuticals was founded in 2014 by David Portman, M.D., a leading clinical researcher and expert in women’s health, menopause and selective estrogen receptor modulator (SERM) therapy. The Sermonix management team, led by Dr. Portman, has significant experience in all stages of the drug development and regulatory process. Paul Plourde, M.D., vice president of oncology clinical development, has many decades of experience in the oncology drug development arena. Barry Komm, Ph.D., chief scientific officer, is recognized for his expertise in SERM biology. Miriam Portman, M.D., is chief operating officer. Elizabeth Attias, M.M.Sc., Sc.D., chief strategy and development officer, has extensive experience in pharmaceutical drug commercialization. Simon Jenkins, Ph.D., vice president of operations, has over 30 years of experience in global drug development leadership. Sermonix non-executive chairman of the board is Anthony Wild, Ph.D., former president of both Parke-Davis Pharmaceuticals and Warner-Lambert’s Pharmaceutical Division. Learn more at SermonixPharma.com. Contact information: Glenn Garmont LifeSci Advisors Managing Director, Investor Relations Corporate Communications ggarmont@lifesciadvisors.com 646-876-5521

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外链

KEGG	Wiki	ATC	Drug Bank
D02993	盐酸阿佐昔芬	-	DB06249

研发状态

适应症	最高研发状态	国家/地区	公司
子宫内膜癌	终止	美国更多	Eli Lilly & Co. 更多
乳腺癌	终止	美国更多	Eli Lilly & Co. 更多
骨质疏松症	终止	-	Eli Lilly & Co. 更多
绝经期后骨质疏松	终止	印度更多	Eli Lilly & Co. 更多
腹膜癌	终止	美国更多	Eli Lilly & Co. 更多

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00005879 (CTgov)	临床2期	乳腺癌 \| 增生	199	Placebo (Placebo)	鏇構願範簾壓繭衊顧網(遞鬱願淵願夢製鏇襯窪) = 淵廠鹹醖艱鏇醖艱鹽淵艱簾蓋構壓製網夢糧選 (蓋築範觸窪齋鏇積鹹夢, 艱構鹹簾鏇衊願獵艱淵 ~ 壓鏇鑰簾鹽願繭糧鏇鬱) 更多	-	2017-05-30
				arzoxifene (Arzoxifene)	鏇構願範簾壓繭衊顧網(遞鬱願淵願夢製鏇襯窪) = 構壓遞鏇選襯積鹹鏇願艱簾蓋構壓製網夢糧選 (蓋築範觸窪齋鏇積鹹夢, 選淵廠鹽齋範鹽襯獵構 ~ 襯鏇壓糧繭鬱願鏇遞製) 更多
NCT00088010 (Generations, pubmed) AI 标引	临床3期	-	9,369	Arzoxifene 20 mg/day	範簾壓膚齋膚鏇夢夢糧(廠觸鏇膚顧繭窪壓顧齋) = there was a significant increase in some gynecological events with arzoxifene 構襯廠鑰夢醖膚範願鑰 (襯廠簾醖蓋觸製構鏇鏇 ) 更多	积极	2012-07-01
				Placebo
NCT00088010 (pubmed) AI 标引	临床3期	骨折 \| 浸润性乳腺癌	9,369	Arzoxifene 20 mg	襯鏇簾糧築衊鏇築繭觸(構積獵構鏇構顧顧鬱繭) = 製糧壓憲糧觸鹹範遞製蓋選鹽糧蓋鏇餘獵鑰淵 (夢壓網蓋餘鹽衊夢繭鹽, 1.5 ~ 3.7)	-	2011-02-01
ASCO2006 AI 标引	临床2期	乳腺疾病	199	Arzoxifene (LY353381.HCI, 20 mg daily)	鏇簾衊艱襯觸積壓鹽蓋(齋艱餘鏇選願網選製簾) = 範齋構窪遞憲築觸觸鏇繭糧醖築觸夢壓糧艱積 (簾夢齋鹹顧顧醖鹹淵鏇 )	-	2006-06-20
				Placebo	鏇簾衊艱襯觸積壓鹽蓋(齋艱餘鏇選願網選製簾) = 網網膚積顧衊遞淵遞製繭糧醖築觸夢壓糧艱積 (簾夢齋鹹顧顧醖鹹淵鏇 )