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Review

Galeterone for the treatment of advanced prostate cancer: the evidence to date

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Pages 2289-2297 | Published online: 15 Jul 2016

Keep up to date with the latest research on this topic with citation updates for this article.

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Bhrugesh Pravinchandra Joshi, Vishwambhar Vishnu Bhandare, Mahima Vankawala, Prittesh Patel, Rajesh Patel, Bhavin Vyas & Ramar Krishnamurty. (2023) Friedelin, a novel inhibitor of CYP17A1 in prostate cancer from Cassia tora. Journal of Biomolecular Structure and Dynamics 41:19, pages 9695-9720.
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Nadia A. Khalil, Eman M. Ahmed, Ashraf F. Zaher, Eman A. Sobh, Samiha A. El-Sebaey & Mona S. El-Zoghbi. (2021) New benzothieno[2,3-c]pyridines as non-steroidal CYP17 inhibitors: design, synthesis, anticancer screening, apoptosis induction, and in silico ADME profile studies. Journal of Enzyme Inhibition and Medicinal Chemistry 36:1, pages 1839-1859.
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Marcello Tucci, Clizia Zichi, Consuelo Buttigliero, Francesca Vignani, Giorgio V Scagliotti & Massimo Di Maio. (2018) Enzalutamide-resistant castration-resistant prostate cancer: challenges and solutions. OncoTargets and Therapy 11, pages 7353-7368.
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Diogo A. Bastos & Emmanuel S. Antonarakis. (2018) CTC-derived AR-V7 detection as a prognostic and predictive biomarker in advanced prostate cancer. Expert Review of Molecular Diagnostics 18:2, pages 155-163.
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Fable Zustovich & Davide Pastorelli. (2016) Therapeutic management of bone metastasis in prostate cancer: an update. Expert Review of Anticancer Therapy 16:11, pages 1199-1211.
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Retheesh S. Thankan, Elizabeth Thomas, Puranik Purushottamachar, David J. Weber & Vincent C.O. Njar. (2023) Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which Outperform Docetaxel and Enzalutamide in CRPC CWR22Rv1 Xenograft Mouse Model. Bioorganic Chemistry 139, pages 106700.
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Edris Choupani, Mohammad Mahmoudi Gomari, Saeed Zanganeh, Sherko Nasseri, Kaveh Haji-allahverdipoor, Neda Rostami, Yaeren Hernandez, Safa Najafi, Neda Saraygord-Afshari & Arshad Hosseini. (2023) Newly Developed Targeted Therapies Against the Androgen Receptor in Triple-Negative Breast Cancer: A Review. Pharmacological Reviews 75:2, pages 309-327.
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Si Ha, Guoshun Luo & Hua Xiang. (2022) A Comprehensive Overview of Small-Molecule Androgen Receptor Degraders: Recent Progress and Future Perspectives. Journal of Medicinal Chemistry 65:24, pages 16128-16154.
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Maria Adamaki & Vassilios Zoumpourlis. (2021) Prostate Cancer Biomarkers: From diagnosis to prognosis and precision-guided therapeutics. Pharmacology & Therapeutics 228, pages 107932.
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Joan Font-Díaz, Alba Jiménez-Panizo, Carme Caelles, María dM Vivanco, Paloma Pérez, Ana Aranda, Eva Estébanez-Perpiñá, Antonio Castrillo, Mercedes Ricote & Annabel F. Valledor. (2021) Nuclear receptors: Lipid and hormone sensors with essential roles in the control of cancer development. Seminars in Cancer Biology 73, pages 58-75.
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Rami A. Masamrekh, Tatiana A. Filippova, Kirill A. Sherbakov, Alexander V. Veselovsky, Victoria V. Shumyantseva & Alexey V. Kuzikov. (2020) Interactions of galeterone and its 3‐keto‐Δ4 metabolite (D4G) with one of the key enzymes of corticosteroid biosynthesis – steroid 21‐monooxygenase (CYP21A2). Fundamental & Clinical Pharmacology 35:2, pages 423-431.
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Keith T. Schmidt, Alwin D. R. Huitema, Cindy H. Chau & William D. Figg. (2021) Resistance to second-generation androgen receptor antagonists in prostate cancer. Nature Reviews Urology 18:4, pages 209-226.
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Maojun Zhou, Hao Zheng, Yubin Li, Huichao Huang, Xiaoli Min, Shuyan Dai, Wenqiang Zhou, Zhuchu Chen, Guangyu Xu & Yongheng Chen. (2021) Discovery of a novel AR/HDAC6 dual inhibitor for prostate cancer treatment. Aging 13:5, pages 6982-6998.
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Susana M. M. Lopes, Joana R. C. Santos & Teresa M. V. D. Pinho e Melo. (2021) Reactivity of steroidal 1-azadienes toward enamines: an approach to novel chiral penta- and hexacyclic steroids. Organic & Biomolecular Chemistry 19:5, pages 1122-1132.
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Eva Estébanez-Perpiñá, Charlotte L. Bevan & Iain J. McEwan. (2021) Eighty Years of Targeting Androgen Receptor Activity in Prostate Cancer: The Fight Goes on. Cancers 13:3, pages 509.
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Yulin Xu, Shichong Liao, Lijun Wang, Yuan Wang, Wen Wei, Ke Su, Yi Tu & Shan Zhu. (2020) Galeterone sensitizes breast cancer to chemotherapy via targeting MNK/eIF4E and β-catenin. Cancer Chemotherapy and Pharmacology 87:1, pages 85-93.
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P. Thelen, H. Taubert, S. Duensing, G. Kristiansen, A. S. Merseburger & M. V. Cronauer. (2018) Bedeutung der Androgenrezeptor-Spleißvariante AR-V7 für Prognose und Therapie des fortgeschrittenen Prostatakarzinoms. Aktuelle Urologie 51:06, pages 582-592.
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S. Wach, H. Taubert & M. Cronauer. (2019) Role of androgen receptor splice variants, their clinical relevance and treatment options. World Journal of Urology 38:3, pages 647-656.
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Claudia Ferroni & Greta Varchi. (2019) Non-Steroidal Androgen Receptor Antagonists and Prostate Cancer: A Survey on Chemical Structures Binding this Fast-Mutating Target. Current Medicinal Chemistry 26:33, pages 6053-6073.
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Andrew K. Kwegyir-Afful, Senthilmurugan Ramalingam, Vidya P. Ramamurthy, Puranik Purushottamachar, Francis N. Murigi, Tadas S. Vasaitis, Weiliang Huang, Maureen A. Kane, Yuji Zhang, Nicholas Ambulos, Sudhir Tiwari, Pratima Srivastava, Ivo P. Nnane, Arif Hussain, Yun Qiu, David J. Weber & Vincent C. O. Njar. (2019) Galeterone and The Next Generation Galeterone Analogs, VNPP414 and VNPP433-3β Exert Potent Therapeutic Effects in Castration-/Drug-Resistant Prostate Cancer Preclinical Models In Vitro and In Vivo. Cancers 11:11, pages 1637.
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Radek Jorda, Eva Řezníčková, Urszula Kiełczewska, Jadwiga Maj, Jacek W. Morzycki, Leszek Siergiejczyk, Václav Bazgier, Karel Berka, Lucie Rárová & Agnieszka Wojtkielewicz. (2019) Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines. European Journal of Medicinal Chemistry 179, pages 483-492.
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N. G. R. Dayan Elshan, Matthew B. Rettig & Michael E. Jung. (2018) Molecules targeting the androgen receptor (AR) signaling axis beyond the AR‐Ligand binding domain. Medicinal Research Reviews 39:3, pages 910-960.
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Štěpán Veselý. (2019) Current clinical utility of prostate cancer markers. Onkologie 13:2, pages 78-82.
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Meng Wu, Yongli Xie, Xiangling Cui, Chenchao Huang, Rongyu Zhang, Yang He, Xiaoyu Li, Mingliang Liu, Shan Cen & Jinming Zhou. (2019) Rational drug design for androgen receptor and glucocorticoids receptor dual antagonist. European Journal of Medicinal Chemistry 166, pages 232-242.
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Cameron M. Armstrong & Allen C. Gao. (2019) Current strategies for targeting the activity of androgen receptor variants. Asian Journal of Urology 6:1, pages 42-49.
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Mohamad Akbar Ali, ChrisTina Okolo, Zakeyah A. Alsharif, Jedidiah Whitt, Steven A. Chambers, Rajender S. Varma & Mohammad A. Alam. (2018) Benign Synthesis of Thiazolo-androstenone Derivatives as Potent Anticancer Agents. Organic Letters 20:18, pages 5927-5932.
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Jane Kim Nguyen & Cristina Magi-Galluzzi. (2018) Unfavorable Pathology, Tissue Biomarkers and Genomic Tests With Clinical Implications in Prostate Cancer Management. Advances in Anatomic Pathology 25:5, pages 293-303.
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Christof Bernemann, Julie Steinestel, Verena Humberg, Martin Bögemann, Andres Jan Schrader & Jochen K. Lennerz. (2018) Performance comparison of two androgen receptor splice variant 7 (AR‐V7) detection methods. BJU International 122:2, pages 219-226.
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Susana M. M. Lopes, Clara S. B. Gomes & Teresa M. V. D. Pinho e Melo. (2018) Reactivity of Steroidal 1-Azadienes toward Carbonyl Compounds under Enamine Catalysis: Chiral Penta- and Hexacyclic Steroids. Organic Letters 20:14, pages 4332-4336.
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K.A. Shcherbakov, D.S. Shcherbinin, V.A. Kostin, V.A. Zolottsev, A.Yu. Misharin & A.V. Veselovsky. (2018) Investigation in silico the interaction of oxazolinyl derivatives of [17(20)E]-21-norpregnene with androgen receptor. Biomedical Chemistry: Research and Methods 1:1, pages e00008.
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Alexander Kretschmer & Derya Tilki. (2017) Biomarkers in prostate cancer – Current clinical utility and future perspectives. Critical Reviews in Oncology/Hematology 120, pages 180-193.
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Eleni Efstathiou. (2017) Attaining precision therapy in prostate cancer: A tall order. European Journal of Cancer 81, pages 226-227.
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Julie Steinestel, Christof Bernemann, Andres J. Schrader & Jochen K. Lennerz. (2017) Reply to Marcus V. Cronauer, Axel S. Merseburger, and M. Raschid Hoda's Letter to the Editor re: Christof Bernemann, Thomas J. Schnoeller, Manuel Luedeke, et al. Expression of AR-V7 in Circulating Tumour Cells Does Not Preclude Response to Next Generation Androgen Deprivation Therapy in Patients with Castration Resistant Prostate Cancer. Eur Urol 2017;71:1–3. European Urology 71:4, pages e107-e108.
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Julie Steinestel, Christof Bernemann, Andres J. Schrader & Jochen K. Lennerz. (2017) Reply from Authors re: Emmanuel S. Antonarakis, Howard I. Scher. Do Patients With AR-V7–Positive Prostate Cancer Benefit from Novel Hormonal Therapies? It All Depends on Definitions. Eur Urol 2017;71:4–6. European Urology 71:1, pages 6-7.
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Isabel Coutinho, Tanya K Day, Wayne D Tilley & Luke A Selth. (2016) Androgen receptor signaling in castration-resistant prostate cancer: a lesson in persistence. Endocrine-Related Cancer 23:12, pages T179-T197.
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