Review
Oncology
Mathieu Roumiguie, Xavier Paoletti, Yann Neuzillet, Romain Mathieu, Sebastien Vincendeau, Francois Kleinclauss, Arnaud Mejean, Laurent Guy, Marc Olivier Timsit, Thierry Lebret
Summary: The study compared the efficacy, safety, and health-related quality of life of apalutamide, enzalutamide, and darolutamide in patients with nonmetastatic castration-resistant prostate cancer. Results showed that all three drugs significantly prolonged survival compared to placebo and were generally well tolerated. Therefore, drug selection in clinical practice should be based on individual patient factors such as tolerability, drug interactions, and comorbidities.
Review
Oncology
Carlo Cattrini, Orazio Caffo, Ugo De Giorgi, Alessia Mennitto, Alessandra Gennari, David Olmos, Elena Castro
Summary: This review discusses the use of apalutamide, darolutamide, and enzalutamide in patients with nmCRPC and the clinical implications of novel imaging techniques for treatment selection.
Article
Oncology
Christos Kakouratos, Dimitra Kalamida, Ioannis Lamprou, Erasmia Xanthopoulou, Christos Nanos, Alexandra Giatromanolaki, Michael Koukourakis
Summary: In vitro and in vivo experiments showed that apalutamide has superior radio-sensitising activity compared to bicalutamide in combination with radiotherapy for prostate cancer. Clinical studies are encouraged to determine whether replacing bicalutamide with apalutamide can improve curability rates.
BRITISH JOURNAL OF CANCER
(2021)
Article
Urology & Nephrology
Susan Halabi, Shan Jiang, Emi Terasawa, Viviana Garcia-Horton, Rajeev Ayyagari, A. Reginald Waldeck, Neal Shore
Summary: This study compared the safety and efficacy of darolutamide vs apalutamide, and darolutamide vs enzalutamide in nonmetastatic castration-resistant prostate cancer through matching-adjusted indirect comparisons. While there were no differences in metastasis-free survival, darolutamide showed lower rates of certain adverse events compared to apalutamide and enzalutamide, suggesting a more favorable safety and tolerability profile.
JOURNAL OF UROLOGY
(2021)
Article
Oncology
Tie Zhou, Shengfei Qin, Weidong Xu, Shouyan Tang, Guanghua Chen, Song Li, Jianguo Hou, Xu Gao, Guowei Shi, Zhongquan Sun, Jie Jin, Lijun Chen, Weibing Sun, Ben Liu, Jingen Wang, Qinggui Meng, Dongwen Wang, Zhiquan Hu, Dalin He, Yong Yang, Xishuang Song, Cheng Fu, Yinhuai Wang, Dingwei Ye, Wei Zhang
Summary: This study assessed the safety and efficacy of proxalutamide, a novel androgen receptor antagonist, in men with metastatic castration-resistant prostate cancer (mCRPC). By evaluating various endpoints, it was found that the 200 mg dose group showed the best antitumor activity with manageable safety. Therefore, a daily dose of 200 mg proxalutamide is recommended for future phase 3 trials.
INTERNATIONAL JOURNAL OF CANCER
(2023)
Article
Oncology
Saizo Fujmoto, Kazutoshi Fujita, Mitsuhisa Nishimoto, Mamoru Hamaguchi, Ken Kuwahara, Mamoru Hashimoto, Shogo Adomi, Takafumi Minami, Masahiro Nozawa, Kazuhiro Yoshimura, Hirotsugu Uemura
Summary: Switching from enzalutamide or apalutamide to darolutamide may be an effective therapeutic option for patients with non-metastatic castration-resistant prostate cancer. This retrospective study demonstrated that approximately 55.5% of patients had a PSA decline >50% after switching to darolutamide, with an average PSA decline of 73%.
Article
Pharmacology & Pharmacy
Valeria Emma Palmieri, Giandomenico Roviello, Alberto D'Angelo, Chiara Casadei, Ugo De Giorgi, Roberta Giorgione
Summary: Important changes have occurred in prostate cancer treatment in recent years, particularly regarding non-metastatic castration-resistant prostate cancer (nmCRPC). Three drugs have been approved for high-risk disease - apalutamide, enzalutamide, and darolutamide. While clinical efficacy is comparable, darolutamide has a different toxicity profile and greater tolerance. Further trials and clinical experience are needed to determine personalized treatments for patients.
EXPERT REVIEW OF CLINICAL PHARMACOLOGY
(2021)
Article
Oncology
Hanfang Jiang, Quchang Ouyang, Yongmei Yin, Zhongshen Tong, Kunwei Shen, Zhongyu Yuan, Cuizhi Geng, Yaxin Liu, Guohong Song, Ran Ran, Wei Li, Qing Qu, Meiyu Wang, Luping Meng, Youzhi Tong, Huiping Li
Summary: The study evaluated the efficacy and safety of a novel non-steroidal androgen receptor antagonist, Proxalutamide, in patients with AR-positive metastatic breast cancer. The results showed promising anti-tumor activity and tolerability of Proxalutamide, supporting further investigation of this drug.
EUROPEAN JOURNAL OF CANCER
(2022)
Article
Biochemistry & Molecular Biology
Yue Gu, Mengxia Xue, Qizhi Wang, Xiaodan Hong, Xinyu Wang, Fang Zhou, Jianguo Sun, Guangji Wang, Ying Peng
Summary: This study evaluated the potential efficacy of proxalutamide as a novel therapy strategy for prostate cancer. Proxalutamide demonstrated superior inhibitory effects on proliferation and migration of PCa cells, induced apoptosis, reduced lipid accumulation, inhibited de novo lipogenesis, and decreased AR expression. By co-targeting the AR axis and endogenous adipogenesis, proxalutamide offers a promising approach to combat drug resistance and prolong the clinical service life of AR-targeted therapy for PCa.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Medicine, General & Internal
Cheng-Kuang Yang, Tai -Lung Cha, Yen-Hwa Chang, Shu-Pin Huang, Jen-Tai Lin, Shian-Shiang Wang, Chao-Yuan Huang, See-Tong Pang
Summary: Darolutamide, a second-generation androgen receptor inhibitor, has been shown to improve metastasis-free survival and overall survival in men with non-metastatic castration-resistant prostate cancer. It has a unique chemical structure that potentially offers advantages in terms of efficacy and safety compared to other similar drugs. Indirect evidence suggests that darolutamide is preferred due to its good adverse event profile.
JOURNAL OF THE FORMOSAN MEDICAL ASSOCIATION
(2023)
Article
Biochemistry & Molecular Biology
Qian Xu, Zixiong Zhang, Chenchao Huang, Qiqi Bao, Rongyu Zhang, Meng Wu, Xiaohui Xiao, Xiaoli Han, Xiaoyu Li, Jinming Zhou
Summary: The androgen signaling pathway is crucial in prostate cancer (PCa), and the anti-androgen drug Darolutamide (ODM-201) shows promising activity against the androgen receptor. This study synthesized 37 analogues of ODM-201 with half of them exhibiting similar or better anti-AR transcriptional activity, and compound 28t showed superior inhibitory activity against resistant mutants.
BIOORGANIC CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Wing Lam, Mohammad Arammash, Wei Cai, Fulan Guan, Zaoli Jiang, Shwu-Huey Liu, Peikwen Cheng, Yung-Chi Cheng
Summary: In this study, the drug YIV-818-A and its active compounds RA-V and RA-VII were found to have potential in addressing drug resistance in castration-resistant prostate cancer (CRPC) by targeting both the androgen receptor (AR) and the glucocorticoid receptor (GR) and modulating important epigenetic markers. These compounds showed synergistic effects with established CRPC drugs in both in vitro and in vivo experiments. These findings suggest that YIV-818-A could be a safe chemopreventive agent and a strong anti-prostate cancer drug.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Oncology
Yara Rodriguez, Kenji Unno, Mihai I. Truica, Zachary R. Chalmers, Young A. Yoo, Rajita Vatapalli, Vinay Sagar, Jindan Yu, Barbara Lysy, Maha Hussain, Huiying Han, Sarki A. Abdulkadir
Summary: This study identifies PRRX2 as a driver of enzalutamide resistance in prostate cancer. PRRX2 expression is highest in double-negative prostate cancer cases and its associated gene signature can serve as a biomarker for enzalutamide resistance, which can be reversed with CDK4/6 and BCL2 inhibitors.
Article
Materials Science, Biomaterials
Ze Gao, Jun Huang, Zhaoxiang Xie, Peikun Xin, Hao Huang, Tao Du, Jun Wu, Hai Huang
Summary: This article proposes a strategy of using a biocompatible nanoparticle drug delivery system to improve the bioavailability and therapeutic performance of enzalutamide. The system has been shown to enhance drug delivery efficiency, increase drug cytotoxicity, and reduce the half-inhibitory concentration of the drug, thus demonstrating great potential for the treatment of prostate cancer.
BIOMATERIALS SCIENCE
(2022)
Article
Chemistry, Medicinal
Ao Wang, Xianggang Luo, Xin Meng, Zhengyu Lu, Kaixian Chen, Yushe Yang
Summary: This study designed, synthesized, and identified a series of steroid analogs, among which YXG-158 (23-h) was a selective androgen receptor degrader with dual functions of AR degradation and CYP17A1 inhibition, showing promising therapeutic potential for enzalutamide-resistant prostate cancer.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Mohamed Abou Chakra, Athanasios E. Dellis, Athanasios G. Papatsoris, Mohamad Moussa
EXPERT OPINION ON PHARMACOTHERAPY
(2020)
Article
Emergency Medicine
Mohamad Moussa, Athanasios G. Papatsoris, Mohamed Abou Chakra
Summary: This study found that ISWI and diclofenac were equally effective in relieving the pain of acute renal colic, and both were more effective compared to placebo.
AMERICAN JOURNAL OF EMERGENCY MEDICINE
(2021)
Editorial Material
Emergency Medicine
Mohamad Moussa, Athanasios G. Papatsoris, Mohamed Abou Chakra
AMERICAN JOURNAL OF EMERGENCY MEDICINE
(2021)
Article
Urology & Nephrology
Kimon Tsirkas, Anna Zygogianni, Andromachi Kougioumtzopoulou, Vasileios Kouloulias, Zoi Liakouli, Athanasios Papatsoris, John Georgakopoulos, Christos Antypas, Christina Armpillia, Athanasios Dellis
Summary: This prospective study suggests that the selective use of alpha-blockers can prevent acute urinary retention in patients undergoing EBRT for localized prostate cancer, while also relieving patient-reported symptoms. However, there are currently no established independent predictive factors to distinguish which patients may benefit from alpha-blocker therapy.
WORLD JOURNAL OF UROLOGY
(2021)
Article
Urology & Nephrology
Mohamad Moussa, Mohamed Abou Chakra, Athanasios G. Papatsoris, Athanasios Dellis, Baraa Dabboucy, Youssef Fares
Summary: Daily intravesical PI instillation significantly reduces symptomatic UTIs, emergency department visits, and hospitalizations in NLUTD patients performing CIC. Moreover, it also decreases multidrug resistance in UTI organisms.
NEUROUROLOGY AND URODYNAMICS
(2021)
Article
Urology & Nephrology
I. Glykas, Ch Fragkoulis, D. D. Mitsikostas, A. Papatsoris, I. Mitsogiannis, G. Papadopoulos, A. Skolarikos, I. Gkialas, K. Ntoumas, A. Dellis
Summary: The study evaluated and compared the efficacy and safety of treating MS patients with LUTD using a b3 agonist (mirabegron) or anticholinergics. Both treatments showed improvement in LUTD symptoms without statistical differences between the two groups.
WORLD JOURNAL OF UROLOGY
(2021)
Article
Oncology
Aristotelis Bamias, Kimon Tzannis, Roubini Zakopoulou, Minas Sakellakis, John Dimitriadis, Alkistis Papatheodoridi, Loukianos Rallidis, Panagiotis Halvatsiotis, Anna Tsiara, Maria Kaparelou, Efthymios Kostouros, Despina Barbarousi, Konstantinos Koutsoukos, Evangelos Fragiadis, Athanasios E. Dellis, Ioannis Anastasiou, Konstantinos Stravodimos, Alexandros Pinitas, Athanasios Papatsoris, Ioannis Adamakis, Ioannis Varkarakis, Charalampos Fragoulis, Stamatina Pagoni, Charis Matsouka, Andreas Skolarikos, Dionysios Mitropoulos, Konstantinos Doumas, Charalampos Deliveliotis, Constantinos Constantinides, Meletios-Athanasios Dimopoulos
Summary: This study investigated the incidence of arterial thromboembolic events (ATEs) in patients with advanced urinary tract cancer (aUTC) who received cytotoxic chemotherapy. The results showed that ATEs occurred in 4.6% of these patients, with ischemic stroke being the most common ATE. Perioperative chemotherapy, tumors other than urinary tract cancer, and pure non-transitional cell carcinoma histology were identified as independent risk factors for ATE.
Review
Chemistry, Medicinal
Mohamad Moussa, Athanasios Papatsoris, Mohamed Abou Chakra, Athanasios Dellis
Summary: The therapeutic landscape for advanced and metastatic urothelial carcinoma is evolving, with the recent approval of enfortumab vedotin showing favorable antitumor effectiveness and an acceptable safety profile in heavily pretreated patients.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2021)
Review
Urology & Nephrology
Dominic Brown, Georgios Tsampoukas, Elenko Petkov Popov, Zaid Aldin, Mohamad Moussa, Athanasios Papatsoris, Noor N. P. Buchholz
Summary: Radiological surveillance of incidental small testicular masses is safe for select patient groups due to the high probability of benign disease, although optimal patient selection criteria and a well-defined protocol are lacking. This approach could be considered for patients with incidental, impalpable testicular masses of <= 5 mm in diameter displaying no significant size increase or internal vascularity on US.
ARAB JOURNAL OF UROLOGY
(2021)
Article
Pharmacology & Pharmacy
Mohamad Moussa, Lazaros Lazarou, Athanasios Dellis, Mohamed Abou Chakra, Athanasios Papatsoris
Summary: The drug darolutamide has been evaluated for its clinical development, efficacy, and safety in the treatment of nonmetastatic castration-resistant prostate cancer. Its unique structure with high affinity for androgen receptors and retaining antagonist activity in mutant isoforms make it exceptional in terms of safety and efficacy compared to other drugs in this category. Darolutamide is considered to have the lowest probability for adverse events compared to apalutamide and enzalutamide, making it a promising option for personalized treatment strategies and sequencing treatment between approved novel drugs.
EXPERT OPINION ON PHARMACOTHERAPY
(2021)
Review
Urology & Nephrology
Mohamad Moussa, Athanasios Papatsoris, Mohamed Abou Chakra, Yousef Fares, Athanasios Dellis
TURKISH JOURNAL OF UROLOGY
(2020)
Review
Surgery
Mohamad Moussa, Mohamed Abou Chakra, Athanasios Papatsoris, Athanasios Dellis, Wajih Saad, Nazih Bou Chahine
INTERNATIONAL JOURNAL OF SURGERY CASE REPORTS
(2020)
Review
Urology & Nephrology
Georgios Tsampoukas, Muhammad Faisal Khan, Antigoni Katsouri, Waseem Akhter, Mohamad Moussa, Konstantinos Deliveliotis, Athanasios Papatsoris, Noor Buchholz
ARCHIVIO ITALIANO DI UROLOGIA E ANDROLOGIA
(2020)
Review
Urology & Nephrology
Athanasios Dellis, Panagiotis Kallidonis, Constantinos Adamou, Nikolaos Kostakopoulos, Dimitrios Kotsiris, Panteleeimon Ntasiotis, Athanasios G. Papatsoris
MINERVA UROLOGICA E NEFROLOGICA
(2020)
Review
Urology & Nephrology
Konstantinos Deliveliotis, Athanasios G. Papatsoris, Andreas Skolarikos, Iraklis Mitsogiannis, Kimon Tzannis, Athanasios E. Dellis
ARAB JOURNAL OF UROLOGY
(2020)