Article
Oncology
Aditya Bardia, Ingrid Mayer, Eric Winer, Hannah M. Linden, Cynthia X. Ma, Barbara A. Parker, Meritxell Bellet, Carlos L. Arteaga, Sravanthi Cheeti, Mary Gates, Ching-Wei Chang, Jill Fredrickson, Jill M. Spoerke, Heather M. Moore, Jennifer Giltnane, Lori S. Friedman, Edna Chow Maneval, Iris Chan, Komal Jhaveri
Summary: This study evaluated the safety and efficacy of GDC-0810 in patients with ER+ advanced/MBC. The results showed that GDC-0810 was safe and tolerable, and had preliminary anti-tumor activity in these patients.
BREAST CANCER RESEARCH AND TREATMENT
(2023)
Article
Chemistry, Medicinal
Jianyu Lu, Chi-chung Chan, Deheng Sun, Guoping Hui, Huijun He, Jian Li, Jiaqiang Dong, Kai Liu, Liang Shen, Lihong Hu, Qingyang Gu, Shuhui Chen, Tielin Wang, Ting Gong, Wei Tang, Xiaoting Li, Xiaotong Zhu, Xu Zeng, Yingjie Zhu, Yuanfeng Xia, Yuanyuan Huang, Yusong Zhu, Zhenteng Liu, Charles Z. Ding
Summary: A novel compound, LX-039, was discovered as a potential treatment for ER positive breast cancer. LX-039 demonstrated significant anti-tumor activity, desirable ER antagonistic characteristics, and favorable pharmacokinetic and preliminary safety properties. This study highlights the clinical importance of LX-039 in the treatment of ER positive breast cancer.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Oncology
Aditya Bardia, Virginia Kaklamani, Sharon Wilks, Amy Weise, Donald Richards, Wael Harb, Cynthia Osborne, Robert Wesolowski, Meghan Karuturi, Paul Conkling, Rebecca G. Bagley, Yamei Wang, Maureen G. Conlan, Peter Kabos
Summary: This phase I study evaluated elacestrant in heavily pretreated women with estrogen receptor-positive metastatic breast cancer. The results showed that elacestrant 400 mg orally once daily has an acceptable safety profile and demonstrated single-agent activity, particularly in patients with ESR1 mutation. A phase III trial investigating elacestrant versus standard endocrine therapy is ongoing.
JOURNAL OF CLINICAL ONCOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Jinmin Miao, Jiajun Dong, Yiming Miao, Yunpeng Bai, Zihan Qu, Brenson A. Jassim, Bo Huang, Quyen Nguyen, Yuan Ma, Allison A. Murray, Jinyue Li, Philip S. Low, Zhong-Yin Zhang
Summary: In this study, researchers discovered the first highly potent and selective TC-PTP degrader called TP1L, which can induce degradation of TC-PTP and enhance T-cell signaling and tumor killing efficacy.
Article
Chemistry, Medicinal
Pengcheng Shao
Summary: The intense interest in developing orally bioavailable SERDs has been driven by the recent discovery of treatment-resistant ESR1 mutations. GDC-9545 (giredestrant) has been identified as a promising candidate with exceptional preclinical profile, showing potential for being a best-in-class oral SERD.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Geriatrics & Gerontology
Intira Sriprasert, Melissa Mert, Wendy J. Mack, Howard N. Hodis, Donna Shoupe
Summary: The study showed that oral estradiol plus vaginal progesterone leads to increased endometrial thickness and a higher risk of endometrial hyperplasia, suggesting the need for further investigation into alternative doses or frequencies of administration for adequate endometrial protection from estrogen therapy in postmenopausal women.
Article
Pharmacology & Pharmacy
Zhijie Dai, Pingfei Fang, Xiang Yan, Ronghua Zhu, Qiong Feng, Qiangyong Yan, Lingfeng Yang, Xiao Fan, Yuting Xie, Lihong Zhuang, Sheng Feng, Yantao Liu, Sheng Zhong, Zeyu Yang, Zhifeng Sheng, Zhiguang Zhou
Summary: SHR-1222, a humanized monoclonal antibody targeting sclerostin, was well tolerated at doses from 50 to 400 mg in this study, showing potential to promote bone formation and reduce bone resorption in individuals with low bone mass.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Oncology
Chuner Jiang, Peng Wu, Xiangming He, Jianfen Ni, Xiaowen Ding, Xiaohong Xu, Fangzheng Wang, Dehong Zou
Summary: This study investigated the relationship between serum reproductive hormone concentrations and patient characteristics and hormone receptor status among postmenopausal Chinese women with breast cancer. The results showed that decreased serum LH and FSH levels were associated with increased ER and PR expressions and decreased HER2 expression in postmenopausal patients with breast cancer.
FRONTIERS IN ONCOLOGY
(2022)
Article
Multidisciplinary Sciences
Soo-Min Kim, Sung Eun Kim, Dong-Yun Lee, DooSeok Choi
Summary: The study evaluated serum estradiol levels in postmenopausal women using different doses and formulations of oral menopausal hormone therapy. It found that serum estradiol levels were not directly proportional to estrogen dose, with estradiol 2 mg showing significantly higher levels compared to estradiol 1 mg and conjugated estrogen 0.45 mg.
SCIENTIFIC REPORTS
(2021)
Article
Substance Abuse
Hu Chen, Yunlong Lu, Rui Xiong, Carlo I. Rosales, Cassandre Coles, Kana Hamada, Nuria Asad, Gregory R. J. Thatcher, Amy W. Lasek
Summary: This study found that the use of a brain-penetrant selective estrogen receptor degrader could reduce binge-like ethanol drinking in female mice, providing a novel strategy to reduce binge drinking in women. Additionally, binge-like ethanol drinking increased Esr1 transcript in specific brain regions in both males and females.
ALCOHOL-CLINICAL AND EXPERIMENTAL RESEARCH
(2022)
Article
Medicine, General & Internal
Jaroslaw Pinkas, Iwona Bojar, Mariusz Gujski, Beata Sarecka-Hujar, Alfred Owoc, Dorota Raczkiewicz
Summary: The study found that interactions between APOE and ESR1 gene polymorphisms can impact cognitive functions in postmenopausal women. Women carrying specific genotypes showed better cognitive functions, while carrying specific genotypes simultaneously may lead to decreased cognitive functioning.
ARCHIVES OF MEDICAL SCIENCE
(2021)
Review
Biochemistry & Molecular Biology
Swati Sucharita Mohanty, Prafulla Kumar Mohanty
Summary: Breast cancer is the second most prevalent cancer globally, with a significant relationship between obesity and increased risk of developing the disease. Premature menopause and premenopausal obesity decrease the risk, while postmenopausal obesity amplifies it due to adipose tissue being a major reservoir for estrogen biosynthesis. High estrogen levels in overweight postmenopausal women are seen as a major factor in breast cancer development.
Article
Endocrinology & Metabolism
Bo Mi Kim, Sung Eun Kim, Dong-Yun Lee, DooSeok Choi
Summary: In this study, 40 postmenopausal Korean women underwent 12 months of TSEC treatment, showing a significant increase in total hip bone mineral density and specific changes in the parameters of HSA. The findings suggest that TSEC treatment could potentially improve bone geometry in postmenopausal women, providing a promising option for fracture prevention and osteoporosis.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Article
Biology
Meng Wu, Rongyu Zhang, Zixiong Zhang, Ning Zhang, Chenfan Li, Yongli Xie, Haoran Xia, Fangjiao Huang, Ruoying Zhang, Ming Liu, Xiaoyu Li, Shan Cen, Jinming Zhou
Summary: A bifunctional small molecule called Z15 was discovered and identified as an effective and selective androgen receptor (AR) antagonist and degrader. It interacts with the ligand-binding domain (LBD) and activation function-1 region of AR, promoting its degradation through the proteasome pathway. In vitro and in vivo studies showed that Z15 successfully suppressed AR, AR mutants, and AR splice variants (ARVs) transcription activity, overcoming resistance to second-generation antiandrogens (SGAs) induced by AR LBD mutations, amplification, and ARVs. This highlights the synergistic importance of AR antagonism and degradation in advanced prostate cancer treatment.
Review
Chemistry, Medicinal
Teesha Downton, Fiona Zhou, Davendra Segara, Rinath Jeselsohn, Elgene Lim
Summary: The translated article discusses the limitations of current endocrine therapies for ER-positive breast cancer and the mechanisms of drug resistance, focusing on ESR1 mutations. It also provides an overview of the development and research progress of oral SERDs in improving treatment outcomes.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)
Review
Radiology, Nuclear Medicine & Medical Imaging
Alfred O. Ankrah, Ismaheel O. Lawal, Rudi A. J. O. Dierckx, Mike M. Sathekge, Andor W. J. M. Glaudemans
Summary: The population at risk for invasive fungal disease has increased due to medical therapy advances and diseases compromising the immune system. Non-invasive and indirect evidence, such as serology and imaging, has been used for early diagnosis of fungal infection. Imaging serves as a non-invasive biomarker for early diagnosis and monitoring of infection during treatment.
SEMINARS IN NUCLEAR MEDICINE
(2023)
Review
Radiology, Nuclear Medicine & Medical Imaging
Nick D. van Rijsewijk, Frank F. A. IJpma, Marjan Wouthuyzen-Bakker, Andor W. J. M. Glaudemans
Summary: F-18-FDG PET/CT has good diagnostic accuracy and value in the diagnosis of fever of unknown origin, providing reliable results in various patient groups. Compared to 67Ga-citrate and WBC scintigraphy, F-18-FDG PET/CT has been more extensively researched and is preferred due to its advantages and shorter procedural duration.
SEMINARS IN NUCLEAR MEDICINE
(2023)
Review
Clinical Neurology
Chris W. J. van der Weijden, Emma Biondetti, Ingomar W. Gutmann, Hildebrand Dijkstra, Rory McKerchar, Daniele de Paula Faria, Erik F. J. de Vries, Jan F. Meilof, Rudi A. J. O. Dierckx, Valentin H. Prevost, Alexander Rauscher
Summary: Myelin is a protective sheath made of phospholipid bilayer and water that wraps around axons. Non-invasive quantitative myelin imaging methods are needed for evaluating myelin damage, assessing the efficacy of remyelination therapies, and monitoring brain maturation in children. Different MRI and PET techniques have been developed for myelin imaging based on various biophysical principles. This review provides an overview of these techniques, including image acquisition, data analysis, and validation status, and concludes that quantitative susceptibility mapping, inhomogeneous magnetization transfer for MRI, and C-11-MeDAS for PET are the most promising techniques.
Review
Radiology, Nuclear Medicine & Medical Imaging
Daniel Aaron Vazquez-Matias, Erik F. J. de Vries, Rudi A. J. O. Dierckx, Janine Doorduin
Summary: Major depressive disorder is a growing and poorly understood pathology that requires research in animal paradigms due to technical and ethical limitations. PET imaging has been used in preclinical studies to investigate glucose metabolism, neuroreceptor populations, and the inflammatory response associated with depressive phenotypes. This review summarizes the findings in animal models and discusses the relevance of PET imaging for understanding depression and developing new therapies.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)
Review
Radiology, Nuclear Medicine & Medical Imaging
Chris W. J. van der Weijden, Pascalle Mossel, Anna L. Bartels, Rudi A. J. O. Dierckx, Gert Luurtsema, Adriaan A. Lammertsma, Antoon T. M. Willemsen, Erik F. J. de Vries
Summary: Pharmacokinetic modelling with arterial sampling is the gold standard for analyzing dynamic PET data of the brain, but it has limited clinical application due to its invasive nature. Non-invasive methods, such as population based input function (PBIF), image derived input function (IDIF), and simultaneous estimation of the input function (SIME), have been proposed as alternatives. This systematic review assesses the correspondence of these non-invasive methods with the gold standard and highlights the need for validation before clinical implementation.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)
Article
Infectious Diseases
Marjan Wouthuyzen-Bakker, Marleen van Oosten, Wouter Bierman, Rik Winter, Andor Glaudemans, Riemer Slart, Marlous Toren-Wielema, Ignace Tielliu, Clark J. Zeebregts, Niek H. J. Prakken, Jean Paul de Vries, Ben R. Saleem
Summary: Vascular graft or endograft infection (VGEI) is a serious complication of vascular surgery, which has high morbidity and mortality rates. To diagnose and treat VGEI effectively, a multidisciplinary team of vascular surgeons, infectious disease specialists, medical microbiologists, radiologists, nuclear medicine specialists, and hospital pharmacists is required. A structured diagnostic, antibiotic, and surgical treatment algorithm can help guide clinical decision-making and improve the clinical outcome of patients with VGEI.
INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES
(2023)
Review
Radiology, Nuclear Medicine & Medical Imaging
Bram van Leer, Nick D. van Rijsewijk, Maarten W. N. Nijsten, Riemer H. J. A. Start, Janesh Pillay, Andor W. J. M. Glaudemans
Summary: The use of F-18-FDG-PET/CT in ICU patients is limited but feasible and safe. It has been shown to be effective in studying the pathophysiology of conditions such as acute respiratory distress syndrome and traumatic brain injury, and has the potential to improve outcomes in cases of infection with unknown origin.
SEMINARS IN NUCLEAR MEDICINE
(2023)
Article
Medicine, General & Internal
Andor W. J. M. Glaudemans, Olivier Gheysens
Summary: Nuclear medicine imaging techniques have gained widespread acceptance in diagnosing and monitoring infectious and inflammatory diseases. PET imaging has been incorporated into diagnostic flowcharts in recent clinical guidelines. This perspective paper discusses current guidelines, limitations, and future research goals for achieving the differentiation between infection, inflammation, and malignancy in nuclear medicine.
FRONTIERS IN MEDICINE
(2023)
Article
Behavioral Sciences
Cyprien G. J. Guerrin, Erik F. J. de Vries, Kavya Prasad, Daniel A. Vazquez-Matias, Lesley E. Manusiwa, Lara Barazzuol, Janine Doorduin
Summary: Prenatal immune activation and postnatal immune challenge had a significant impact on behavior in female rats. The combination of maternal immune activation and immune challenge during adolescence resulted in long-lasting changes in social behavior and locomotion. These findings highlight the importance of immune activation and challenge during critical periods of development.
BEHAVIOURAL BRAIN RESEARCH
(2023)
Review
Oncology
Mostafa Roya, Samaneh Mostafapour, Philipp Mohr, Laura Providencia, Zekai Li, Johannes H. van Snick, Adrienne H. Brouwers, Walter Noordzij, Antoon T. M. Willemsen, Rudi A. J. O. Dierckx, Adriaan A. Lammertsma, Andor W. J. M. Glaudemans, Charalampos Tsoumpas, Riemer H. J. A. Slart, Joyce van Sluis
Summary: Recently, a new type of PET scanner with long axial field-of-view (LAFOV) has been introduced in clinical practice. Compared to conventional PET scanners, LAFOV scanners have a larger coverage and higher sensitivity, providing new opportunities for clinical applications, such as reducing scan time, decreasing the amount of radiotracer used, and using dynamic or parametric imaging. Emerging technologies like artificial intelligence and imaging with multiple radiotracers can further enhance the clinical application of LAFOV PET.
Review
Oncology
Jasper J. L. van Geel, Erik F. J. de Vries, Michel van Kruchten, Geke A. P. Hospers, Andor W. J. M. Glaudemans, Carolina P. Schroder
Summary: Molecular imaging, such as PET, is being used more frequently as a biomarker to predict and assess treatment response in breast cancer. Specific tracers are used to measure metabolic activity, estrogen receptor expression, and human epidermal growth factor receptor 2 expression. These biomarkers have potential in predicting treatment response and outcome, but more studies are needed before implementation in clinical practice.
THERAPEUTIC ADVANCES IN MEDICAL ONCOLOGY
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Bram van Leer, Johannes H. van Snick, Mark Londema, Maarten W. N. Nijsten, Oemer Kasalak, Riemer H. J. A. Slart, Andor W. J. M. Glaudemans, Janesh Pillay
Summary: We report the findings of four critically ill patients with persistent inflammation during late phase of COVID-19 who underwent [F-18]FDG-PET/CT imaging. PET/CT findings showed that bilateral lung anomalies could explain the increased CRP and leukocytes in all patients. Based on PET/CT results, secondary infection/inflammatory focus was suspected in two patients (pancreatitis and gastritis). Lymphadenopathy was present in patients with detectable SARS-CoV-2 viral load. Muscle uptake around the hips or shoulders was observed in all patients, possibly due to the process of heterotopic ossification.
CLINICAL AND TRANSLATIONAL IMAGING
(2023)
Article
Toxicology
Didima M. G. de Groot, Louisa Linders, Reinier Kayser, Rianne Nederlof, Celine de Esch, Roderick C. Slieker, C. Frieke Kuper, Andre Wolterbeek, V. Jeroen de Groot, Andor Veltien, Arend Heerschap, Aren van Waarde, Rudi A. J. O. Dierckx, Erik F. J. de Vries
Summary: This study investigated the impact of environmental chemicals on brain development and found that di-n-octyltin dichloride (DOTC) can affect both structural and functional brain development. The study also revealed the involvement of immune system development and functioning in the impairment of the nervous system. These findings support the close connection between the immune and nervous systems in brain development.
TOXICOLOGY MECHANISMS AND METHODS
(2023)
