Degarelix (BioDeep_00000615059)
代谢物信息卡片
(4R)-N-{4-[(2S)-2-{[(1R)-2-[4-(carbamoylamino)phenyl]-1-{[(1S)-1-{[(2S)-1-(2-{[(1R)-1-carbamoylethyl]carbamoyl}pyrrolidin-1-yl)-1-oxo-6-[(propan-2-yl)amino]hexan-2-yl]carbamoyl}-3-methylbutyl]carbamoyl}ethyl]carbamoyl}-2-[(2S)-2-[(2R)-2-[(2R)-3-(4-chlorophenyl)-2-[(2R)-2-acetamido-3-(naphthalen-2-yl)propanamido]propanamido]-3-(pyridin-3-yl)propanamido]-3-hydroxypropanamido]ethyl]phenyl}-2,6-dioxo-1,3-diazinane-4-carboxamide
化学式: C82H103ClN18O16 (1630.7487588000001)
中文名称: 地加瑞克
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC(C)CC(C(=O)NC(CCCCNC(C)C)C(=O)N1CCCC1C(=O)NC(C)C(=O)N)NC(=O)C(CC2=CC=C(C=C2)NC(=O)N)NC(=O)C(CC3=CC=C(C=C3)NC(=O)C4CC(=O)NC(=O)N4)NC(=O)C(CO)NC(=O)C(CC5=CN=CC=C5)NC(=O)C(CC6=CC=C(C=C6)Cl)NC(=O)C(CC7=CC8=CC=CC=C8C=C7)NC(=O)C
InChI: InChI=1S/C82H103ClN18O16/c1-45(2)35-60(72(107)92-59(16-9-10-33-87-46(3)4)80(115)101-34-12-17-68(101)79(114)88-47(5)70(84)105)93-74(109)63(38-51-23-30-58(31-24-51)91-81(85)116)95-76(111)64(39-50-21-28-57(29-22-50)90-71(106)66-42-69(104)100-82(117)99-66)97-78(113)67(44-102)98-77(112)65(41-53-13-11-32-86-43-53)96-75(110)62(37-49-19-26-56(83)27-20-49)94-73(108)61(89-48(6)103)40-52-18-25-54-14-7-8-15-55(54)36-52/h7-8,11,13-15,18-32,36,43,45-47,59-68,87,102H,9-10,12,16-17,33-35,37-42,44H2,1-6H3,(H2,84,105)(H,88,114)(H,89,103)(H,90,106)(H,92,107)(H,93,109)(H,94,108)(H,95,111)(H,96,110)(H,97,113)(H,98,112)(H3,85,91,116)(H2,99,100,104,117)/t47-,59+,60+,61-,62-,63-,64+,65-,66+,67+,68+/m1/s1
描述信息
L - Antineoplastic and immunomodulating agents > L02 - Endocrine therapy > L02B - Hormone antagonists and related agents
C147908 - Hormone Therapy Agent > C547 - Hormone Antagonist > C2092 - Gonadotropin Releasing Hormone Antagonist
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Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix can be used for prostate cancer research[1].
同义名列表
2 个代谢物同义名
Degarelix; (4R)-N-{4-[(2S)-2-{[(1R)-2-[4-(carbamoylamino)phenyl]-1-{[(1S)-1-{[(2S)-1-(2-{[(1R)-1-carbamoylethyl]carbamoyl}pyrrolidin-1-yl)-1-oxo-6-[(propan-2-yl)amino]hexan-2-yl]carbamoyl}-3-methylbutyl]carbamoyl}ethyl]carbamoyl}-2-[(2S)-2-[(2R)-2-[(2R)-3-(4-chlorophenyl)-2-[(2R)-2-acetamido-3-(naphthalen-2-yl)propanamido]propanamido]-3-(pyridin-3-yl)propanamido]-3-hydroxypropanamido]ethyl]phenyl}-2,6-dioxo-1,3-diazinane-4-carboxamide
数据库引用编号
8 个数据库交叉引用编号
- ChEBI: CHEBI:135961
- KEGGdrug: D08901
- PubChem: 16136245
- Metlin: METLIN85566
- DrugBank: DB06699
- ChEMBL: CHEMBL415606
- CAS: 214766-78-6
- medchemexpress: HY-16168A
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
文献列表
- Rebecka Amodei, Sonnet S Jonker, William Whitler, Charles T Estill, Charles E Roselli. The GnRH Antagonist Degarelix Suppresses Gonadotropin Secretion and Pituitary Sensitivity in Midgestation Sheep Fetuses.
Endocrinology.
2022 02; 163(2):. doi:
10.1210/endocr/bqab262. [PMID: 34958103] - Hiroshi Sasaki, Kenta Miki, Kojiro Tashiro, Keiichiro Mori, Fumihiko Urabe, Wataru Fukuokaya, Takahiro Kimura, Shun Sato, Hiroyuki Takahashi, Manabu Aoki, Shin Egawa. Differences in sex hormone recovery profile after cessation of 12-week gonadotropin-releasing hormone antagonist versus agonist therapy.
Andrology.
2022 02; 10(2):270-278. doi:
10.1111/andr.13107. [PMID: 34510814] - Jeremy Yuen-Chun Teoh, Xiao-Yu Tian, Christine Yim-Ping Wong, Chi-Wai Lau, Chak-Kwong Cheng, Victor Wai-Lun Tang, Ronald Cheong-Kin Chan, Yu Huang, Chi-Fai Ng. Endothelial dysfunction after androgen deprivation therapy and the possible underlying mechanisms.
The Prostate.
2022 01; 82(1):13-25. doi:
10.1002/pros.24244. [PMID: 34570375] - Carlotta Palumbo, Alessandro Antonelli, Luca Triggiani, Alberto Dalla Volta, Filippo Maffezzoni, Stefania Zamboni, Paolo Borghetti, Luca Rinaudo, Francesca Valcamonico, Roberto Maroldi, Stefano Maria Magrini, Claudio Simeone, Alfredo Berruti. Changes in body composition and lipid profile in prostate cancer patients without bone metastases given Degarelix treatment: the BLADE prospective cohort study.
Prostate cancer and prostatic diseases.
2021 09; 24(3):852-859. doi:
10.1038/s41391-021-00345-0. [PMID: 33723362] - Nicholas G Nickols, Matthew B Goetz, Christopher J Graber, Debika Bhattacharya, Guy Soo Hoo, Matthew Might, David B Goldstein, Xinchen Wang, Rachel Ramoni, Kenute Myrie, Samantha Tran, Leila Ghayouri, Sonny Tsai, Michelle Geelhoed, Danil Makarov, Daniel J Becker, Jun-Chieh Tsay, Melissa Diamond, Asha George, Mohammad Al-Ajam, Pooja Belligund, R Bruce Montgomery, Elahe A Mostaghel, Carlie Sulpizio, Zhibao Mi, Ellen Dematt, Joseph Tadalan, Leslie E Norman, Daniel Briones, Christina E Clise, Zachary W Taylor, Jeffrey R Huminik, Kousick Biswas, Matthew B Rettig. Hormonal intervention for the treatment of veterans with COVID-19 requiring hospitalization (HITCH): a multicenter, phase 2 randomized controlled trial of best supportive care vs best supportive care plus degarelix: study protocol for a randomized controlled trial.
Trials.
2021 Jul; 22(1):431. doi:
10.1186/s13063-021-05389-0. [PMID: 34225789] - Wilhelmina C M Duivenvoorden, Magda Naeim, Sarah N Hopmans, Sadiya Yousef, Geoff H Werstuck, Shawn Dason, Jehonathan H Pinthus. Protective effect of pharmacological castration on metabolic perturbations and cardiovascular disease in the hyperglycemic male ApoE-/-:Ins2+/Akita mouse model.
Prostate cancer and prostatic diseases.
2021 06; 24(2):389-397. doi:
10.1038/s41391-020-00288-y. [PMID: 32989260] - Yi-Fu Liu, Sheng-Qiang Fu, Yu-Chang Yan, Bin-Bin Gong, Wen-Jie Xie, Xiao-Rong Yang, Ting Sun, Ming Ma. Progress in Clinical Research on Gonadotropin-Releasing Hormone Receptor Antagonists for the Treatment of Prostate Cancer.
Drug design, development and therapy.
2021; 15(?):639-649. doi:
10.2147/dddt.s291369. [PMID: 33623372] - Noritoshi Kawate, Ryota Kanuki, M A Hannan, Weerakoon W P N Weerakoon. Inhibitory effects of long-term repeated treatments of a sustainable GnRH antagonist, degarelix acetate, on caprine testicular functions.
The Journal of reproduction and development.
2020 Dec; 66(6):587-592. doi:
10.1262/jrd.2020-035. [PMID: 32830151] - Jesse Ory, Thiago Fernandes Nigres Lima, Maxwell Towe, Fabio Stefano Frech, Jordan C Best, Bruce R Kava, Ranjith Ramasamy. Understanding the Complex Relationship Between Androgens and SARS-CoV2.
Urology.
2020 10; 144(?):1-3. doi:
10.1016/j.urology.2020.06.048. [PMID: 32653566] - Andrei Cristian Dan Gheorghe, Ana Ciobanu, Andreea Simona Hodorogea, George Daniel Radavoi, Viorel Jinga, Ioan Tiberiu Nanea, Gabriela Silvia Gheorghe. Evolution of Electrocardiographic Repolarization Parameters During Antiandrogen Therapy in Patients with Prostate Cancer and Hypogonadism.
Cardiovascular toxicology.
2020 08; 20(4):390-400. doi:
10.1007/s12012-020-09566-6. [PMID: 32152959] - Harutake Sawazaki, Daiji Araki, Yosuke Kitamura, Kota Yagi. Metabolic changes with degarelix vs leuprolide plus bicalutamide in patients with prostate cancer: a randomized clinical study.
World journal of urology.
2020 Jun; 38(6):1465-1471. doi:
10.1007/s00345-019-02937-x. [PMID: 31482294] - Conrad Leitsmann, Paul Thelen, Marianne Schmid, Johannes Meller, Carsten-Oliver Sahlmann, Birgit Meller, Lutz Trojan, Arne Strauss. Enhancing PSMA-uptake with androgen deprivation therapy - a new way to detect prostate cancer metastases?.
International braz j urol : official journal of the Brazilian Society of Urology.
2019 May; 45(3):459-467. doi:
10.1590/s1677-5538.ibju.2018.0305. [PMID: 30901173] - Indunil N Pathirana, Chandana Rajapaksa, Noritoshi Kawate, Anuradha Wimalarathne, Lakshitha Fonseka, Priyangika Nilmini Weerakoon, Minhaj A Hannan, Basil Alexander, Anil Pushpakumara, Siril Ariyaratne, Hiromichi Tamada. EFFECTS OF GONADOTROPIN-RELEASING HORMONE ANTAGONIST DEGARELIX ON MUSTH AND SERUM TESTOSTERONE CONCENTRATIONS IN ASIAN ELEPHANTS ( ELEPHAS MAXIMUS).
Journal of zoo and wildlife medicine : official publication of the American Association of Zoo Veterinarians.
2018 Sep; 49(3):779-783. doi:
10.1638/2018-0019.1. [PMID: 30212355] - Laurence Klotz, Andrew Loblaw, Robert Siemens, Paul Ouellette, Anil Kapoor, Marlene Kebabdjian, Liying Zhang, Fred Saad. A Phase II, Randomized, Multicenter Study Comparing 10 Months versus 4 Months of Degarelix Therapy in Prolonging the Off Treatment Interval in Men with Localized Prostate Cancer Receiving Intermittent Androgen Deprivation Therapy for Biochemical Recurrence following Radical Local Therapy.
The Journal of urology.
2018 08; 200(2):335-343. doi:
10.1016/j.juro.2018.03.010. [PMID: 29534997] - Lorenzo Tosco, Annouschka Laenen, Thomas Gevaert, Isabelle Salmon, Christine Decaestecker, Elai Davicioni, Christine Buerki, Frank Claessens, Johan Swinnen, Karolien Goffin, Raymond Oyen, Wouter Everaerts, Lisa Moris, Gert De Meerleer, Karin Haustermans, Steven Joniau. Neoadjuvant degarelix with or without apalutamide followed by radical prostatectomy for intermediate and high-risk prostate cancer: ARNEO, a randomized, double blind, placebo-controlled trial.
BMC cancer.
2018 04; 18(1):354. doi:
10.1186/s12885-018-4275-z. [PMID: 29606109] - Jun-Ichi Hori, Daisuke Koga, Hidehiro Kakizaki, Tsuyoshi Watanabe. Differential effects of depot formulations of GnRH agonist leuprorelin and antagonist degarelix on the seminiferous epithelium of the rat testis.
Biomedical research (Tokyo, Japan).
2018; 39(4):197-214. doi:
10.2220/biomedres.39.197. [PMID: 30101840] - Håkan Olsson, Niclas Petri, Lars Erichsen, Anders Malmberg, Lars Grundemar. Effect of Degarelix, a Gonadotropin-Releasing Hormone Receptor Antagonist for the Treatment of Prostate Cancer, on Cardiac Repolarisation in a Randomised, Placebo and Active Comparator Controlled Thorough QT/QTc Trial in Healthy Men.
Clinical drug investigation.
2017 Sep; 37(9):873-879. doi:
10.1007/s40261-017-0547-7. [PMID: 28660498] - Yoshiyuki Miyazawa, Yoshitaka Sekine, Takahiro Syuto, Masashi Nomura, Hidekazu Koike, Hiroshi Matsui, Yasuhiro Shibata, Kazuto Ito, Kazuhiro Suzuki. A gonadotropin-releasing hormone antagonist reduces serum adrenal androgen levels in prostate cancer patients.
BMC urology.
2017 Aug; 17(1):70. doi:
10.1186/s12894-017-0261-z. [PMID: 28851333] - Michael Backofen, Gregoire Schwach, Wolfgang Koechling, Torsten Weiss, Achim Goepferich. Polyanion based controlled release system for the GnRH-receptor antagonist degarelix.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.
2017 Jun; 104(?):65-71. doi:
10.1016/j.ejps.2017.03.036. [PMID: 28347774] - Seiichiro Ozono, Taiji Tsukamoto, Seiji Naito, Yasuo Ohashi, Takeshi Ueda, Tsutomu Nishiyama, Hideki Maeda, Hidehito Kusuoka, Rio Akazawa, Mototsugu Ito, Hideyuki Akaza. Efficacy and safety of a 3-month dosing regimen of degarelix in Japanese patients with prostate cancer: a phase II maintenance-dose-finding study.
Japanese journal of clinical oncology.
2017 May; 47(5):438-446. doi:
10.1093/jjco/hyx011. [PMID: 28334771] - M A Hannan, N Kawate, Y Fukami, W W P N Weerakoon, E E Büllesbach, T Inaba, H Tamada. Effects of long-acting GnRH antagonist, degarelix acetate, on plasma insulin-like peptide 3, testosterone and luteinizing hormone concentrations, and scrotal circumference in male goats.
Theriogenology.
2017 Jan; 88(?):228-235. doi:
10.1016/j.theriogenology.2016.09.032. [PMID: 27793455] - J Morote, L Regis, A Celma, J Planas. Measurement of serum testosterone during androgenic suppression in patients with prostate cancer: A systematic review.
Actas urologicas espanolas.
2016 Oct; 40(8):477-84. doi:
10.1016/j.acuro.2016.01.006. [PMID: 26899928] - H Taniguchi, T Katano, K Nishida, H Kinoshita, T Matsuda, S Ito. Elucidation of the mechanism of suppressed steroidogenesis during androgen deprivation therapy of prostate cancer patients using a mouse model.
Andrology.
2016 09; 4(5):964-71. doi:
10.1111/andr.12213. [PMID: 27230983] - Kenta Miki, Hiroshi Sasaki, Masahito Kido, Hiroyuki Takahashi, Manabu Aoki, Shin Egawa. A comparative study on the efficacies of gonadotropin-releasing hormone (GnRH) agonist and GnRH antagonist in neoadjuvant androgen deprivation therapy combined with transperineal prostate brachytherapy for localized prostate cancer.
BMC cancer.
2016 09; 16(?):708. doi:
10.1186/s12885-016-2737-8. [PMID: 27586506] - Greg L Shaw, Hayley Whitaker, Marie Corcoran, Mark J Dunning, Hayley Luxton, Jonathan Kay, Charlie E Massie, Jodi L Miller, Alastair D Lamb, Helen Ross-Adams, Roslin Russell, Adam W Nelson, Matthew D Eldridge, Andrew G Lynch, Antonio Ramos-Montoya, Ian G Mills, Angela E Taylor, Wiebke Arlt, Nimish Shah, Anne Y Warren, David E Neal. The Early Effects of Rapid Androgen Deprivation on Human Prostate Cancer.
European urology.
2016 08; 70(2):214-8. doi:
10.1016/j.eururo.2015.10.042. [PMID: 26572708] - Junichi Hori, Naoki Wada, Gaku Tamaki, Makoto Azumi, Masafumi Kita, Tatsuya Iwata, Seiji Matsumoto, Hidehiro Kakizaki. Combination of GnRH Antagonist Degarelix and Antiandrogen Is Effective in PSA Reduction and Bone Management in Patients with Prostate Cancer.
Gan to kagaku ryoho. Cancer & chemotherapy.
2016 Jun; 43(6):727-31. doi:
NULL. [PMID: 27306809] - Monica Sakai, Daniel B Martinez-Arguelles, Nathan H Patterson, Pierre Chaurand, Vassilios Papadopoulos. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonist degarelix on human prostate cell growth.
PloS one.
2015; 10(3):e0120670. doi:
10.1371/journal.pone.0120670. [PMID: 25811175] - Sarah N Hopmans, Wilhelmina C M Duivenvoorden, Geoff H Werstuck, Laurence Klotz, Jehonathan H Pinthus. GnRH antagonist associates with less adiposity and reduced characteristics of metabolic syndrome and atherosclerosis compared with orchiectomy and GnRH agonist in a preclinical mouse model.
Urologic oncology.
2014 Nov; 32(8):1126-34. doi:
10.1016/j.urolonc.2014.06.018. [PMID: 25242517] - Jack M Zuckerman, Gregg Eure, John Malcolm, Lilian Currie, Robert Given. Prospective evaluation of testosterone fluctuations during a transition of therapy from degarelix to leuprolide in patients on androgen deprivation therapy.
Urology.
2014 Mar; 83(3):670-4. doi:
10.1016/j.urology.2013.10.036. [PMID: 24360065] - Anders Sonesson, Birgitte Buur Rasmussen. In vitro and in vivo human metabolism of degarelix, a gonadotropin-releasing hormone receptor blocker.
Drug metabolism and disposition: the biological fate of chemicals.
2013 Jul; 41(7):1339-46. doi:
10.1124/dmd.113.051706. [PMID: 23589543] - Karol Axcrona, Sirpa Aaltomaa, Carlos Martins da Silva, Haluk Ozen, Jan-Erik Damber, László B Tankó, Enrico Colli, Peter Klarskov. Androgen deprivation therapy for volume reduction, lower urinary tract symptom relief and quality of life improvement in patients with prostate cancer: degarelix vs goserelin plus bicalutamide.
BJU international.
2012 Dec; 110(11):1721-8. doi:
10.1111/j.1464-410x.2012.11107.x. [PMID: 22500884] - Juan Antonio García-Velasco, Sanja Kupesic, Antonio Pellicer, Claire Bourgain, Carlos Simón, Milan Mrazek, Paul Devroey, Joan-Carles Arce. Follicular and endocrine profiles associated with different GnRH-antagonist regimens: a randomized controlled trial.
Reproductive biomedicine online.
2012 Feb; 24(2):153-62. doi:
10.1016/j.rbmo.2011.10.016. [PMID: 22197127] - Anders Sonesson, Wolfgang Koechling, Jacek Stalewski, László B Tankó, Birgitte Buur Rasmussen. Metabolite profiles of degarelix, a new gonadotropin-releasing hormone receptor antagonist, in rat, dog, and monkey.
Drug metabolism and disposition: the biological fate of chemicals.
2011 Oct; 39(10):1895-903. doi:
10.1124/dmd.111.039883. [PMID: 21768273] - J de la Rosette, R Davis, D Frankel, T Kold Olesen. Efficacy and safety of androgen deprivation therapy after switching from monthly leuprolide to monthly degarelix in patients with prostate cancer.
International journal of clinical practice.
2011 May; 65(5):559-66. doi:
10.1111/j.1742-1241.2011.02637.x. [PMID: 21342376] - Ryan S Raddin, Christine M Walko, Young E Whang. Response to degarelix after resistance to luteinizing hormone-releasing hormone agonist therapy for metastatic prostate cancer.
Anti-cancer drugs.
2011 Mar; 22(3):299-302. doi:
10.1097/cad.0b013e328342d54b. [PMID: 21360851] - Fritz H Schröder, Bertrand Tombal, Kurt Miller, Laurent Boccon-Gibod, Neal D Shore, E David Crawford, Judd Moul, Tine Kold Olesen, Bo-Eric Persson. Changes in alkaline phosphatase levels in patients with prostate cancer receiving degarelix or leuprolide: results from a 12-month, comparative, phase III study.
BJU international.
2010 Jul; 106(2):182-7. doi:
10.1111/j.1464-410x.2009.08981.x. [PMID: 19912212] - James E Frampton, Katherine A Lyseng-Williamson. Degarelix.
Drugs.
2009 Oct; 69(14):1967-76. doi:
10.2165/10484080-000000000-00000. [PMID: 19747011] - Bo-Eric Persson, Tine Kold Olesen, Jens-Kristian Jensen. Degarelix: a new approach for the treatment of prostate cancer.
Neuroendocrinology.
2009; 90(3):235-44. doi:
10.1159/000228832. [PMID: 19602868] - Michael Steinberg. Degarelix: a gonadotropin-releasing hormone antagonist for the management of prostate cancer.
Clinical therapeutics.
2009; 31 Pt 2(?):2312-31. doi:
10.1016/j.clinthera.2009.11.009. [PMID: 20110043] - Marc Gittelman, Peter J Pommerville, Bo-Eric Persson, Jens-Kristian Jensen, Tine Kold Olesen. A 1-year, open label, randomized phase II dose finding study of degarelix for the treatment of prostate cancer in North America.
The Journal of urology.
2008 Nov; 180(5):1986-92. doi:
10.1016/j.juro.2008.07.033. [PMID: 18801505] - Hendrik Van Poppel, Bertrand Tombal, Jean J de la Rosette, Bo-Eric Persson, Jens-Kristian Jensen, Tine Kold Olesen. Degarelix: a novel gonadotropin-releasing hormone (GnRH) receptor blocker--results from a 1-yr, multicentre, randomised, phase 2 dosage-finding study in the treatment of prostate cancer.
European urology.
2008 Oct; 54(4):805-13. doi:
10.1016/j.eururo.2008.04.065. [PMID: 18538469] - Hendrik van Poppel, Sten Nilsson. Testosterone surge: rationale for gonadotropin-releasing hormone blockers?.
Urology.
2008 Jun; 71(6):1001-6. doi:
10.1016/j.urology.2007.12.070. [PMID: 18407326] - John Anderson, Per-Anders Abrahamsson, David Crawford, Kurt Miller, Bertrand Tombal. Management of advanced prostate cancer: can we improve on androgen deprivation therapy?.
BJU international.
2008 Jun; 101(12):1497-501. doi:
10.1111/j.1464-410x.2008.07590.x. [PMID: 18336613] - Marc Princivalle, Pierre Broqua, Richard White, Jessica Meyer, Gaell Mayer, Lucy Elliott, Ketil Bjarnason, Robert Haigh, Christopher Yea. Rapid suppression of plasma testosterone levels and tumor growth in the dunning rat model treated with degarelix, a new gonadotropin-releasing hormone antagonist.
The Journal of pharmacology and experimental therapeutics.
2007 Mar; 320(3):1113-8. doi:
10.1124/jpet.106.112326. [PMID: 17179469] - Pravin R Jadhav, Henrik Agersø, Christoffer W Tornøe, Jogarao V S Gobburu. Semi-mechanistic pharmacodynamic modeling for degarelix, a novel gonadotropin releasing hormone (GnRH) blocker.
Journal of pharmacokinetics and pharmacodynamics.
2006 Oct; 33(5):609-34. doi:
10.1007/s10928-006-9025-1. [PMID: 16967346] - Henrik Agersø, Wolfgang Koechling, Magnus Knutsson, Rolf Hjortkjaer, Mats O Karlsson. The dosing solution influence on the pharmacokinetics of degarelix, a new GnRH antagonist, after s.c. administration to beagle dogs.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.
2003 Nov; 20(3):335-40. doi:
10.1016/j.ejps.2003.08.001. [PMID: 14592699] - Pierre Broqua, Pierre J-M Riviere, P Michael Conn, Jean E Rivier, Michel L Aubert, Jean-Louis Junien. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: degarelix.
The Journal of pharmacology and experimental therapeutics.
2002 Apr; 301(1):95-102. doi:
10.1124/jpet.301.1.95. [PMID: 11907162] - G Jiang, J Stalewski, R Galyean, J Dykert, C Schteingart, P Broqua, A Aebi, M L Aubert, G Semple, P Robson, K Akinsanya, R Haigh, P Riviere, J Trojnar, J L Junien, J E Rivier. GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.
Journal of medicinal chemistry.
2001 Feb; 44(3):453-67. doi:
10.1021/jm0003900. [PMID: 11462984]