A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones

2002 ◽  
Vol 12 (16) ◽  
pp. 2073-2077 ◽  
Author(s):  
Satoshi Sasaki ◽  
Toshihiro Imaeda ◽  
Yoji Hayase ◽  
Yoshiaki Shimizu ◽  
Shizuo Kasai ◽  
...  
Keyword(s):  
Luteinizing Hormone ◽  
Luteinizing Hormone Releasing Hormone ◽  
Releasing Hormone ◽  
Design And Synthesis ◽  
New Class ◽  
Lhrh Antagonists

scholarly journals Luteinizing hormone-releasing hormone antagonists for urinary obstruction in prostate cancer

2013 ◽  
Vol 7 (9-10) ◽  
pp. 648 ◽  
Author(s):  
Patricia Tai ◽  
Asim Amjad ◽  
Rashmi Koul ◽  
Evgeny Sadikov ◽  
Arbind Dubey
Keyword(s):  
Prostate Cancer ◽  
Luteinizing Hormone ◽  
Serum Creatinine ◽  
Urinary Tract Obstruction ◽  
Specific Antigen ◽  
Pelvic Mass ◽  
Luteinizing Hormone Releasing Hormone ◽  
Releasing Hormone ◽  
Lhrh Agonists ◽  
Lhrh Antagonists

Luteinizing hormone-releasing hormone (LHRH) antagonists rapidly reduce testosterone and are preferred to LHRH agonists in situations when early response is important. The lack of flare reaction, as compared to LHRH agonists, is particularly desirable as it would not aggravate the problem. A 78-year-old man presented with symptoms of urinary tract obstruction. He had a prostate-specific antigen (PSA) of 91.3 ug/L and serum creatinine 146 umol/L. He had a large pelvic mass due to histologically confirmed prostate cancer, resulting in moderate left hydronephrosis and deteriorating renal function (serum creatinine of 163 umol/L). He was started on combined degarelix and bicalutamide on the day of consultation (day 0). The hydronephrosis resolved on the repeat computerized tomography scan performed on day 10. Serum creatinine normalized to under 130 umol/L on day 18. The PSA fell to 11 ug/L on day 18, 2.8 ug/L on day 28, and 0.5 ug/L on day 53. Therefore, LHRH antagonists are particularly useful in urgent situations. It is the preferred choice in these circumstances.

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