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Peptide based LHRH agonists and new generation antagonists

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05/28/2014

Peptide based LHRH agonists and new generation antagonists

Luteinizing hormone-releasing hormone (LH-RH or LHRH) agonists and gonadotropin-releasing hormone (GnRH) agonists are peptides or drugs that are used for hormone therapy. These drugs lower the production of testosterone in a human's body. The drop in testosterone levels usually slows or stops the growth of prostate cancer for some time. These agonist drugs cause the pituitary gland to release the hormones that tell the testicles and adrenal glands to produce testosterone. These drugs are usually given by injection or implanted under the skin or may be given once a month, once every 3 to 4 months, or once a year.
 
 
Peptide
Sequence
Indications
Agonists
 
 
Buserelin
 
Pyr-His-Trp-Ser-Tyr-D-Ser(OtBu)-Leu-Arg-Pro-NHEt
Prostate cancer
Gonadorelin
 
Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2
Cystic ovarian disease, agent for evaluating
hypothalamic-pituitary gonadotropic function
 
Goserelin
Pyr-His-Trp-Ser-Tyr-D-Ser(OtBu)-Leu-Arg-Pro-AzGly-NH2
Prostate cancer; breast cancer
Histrelin
 
Pyr-His-Trp-Ser-Tyr-D-His(N-benzyl)-Leu-Arg-Pro-NHEt
Prostate cancer; breast cancer
Leuprolide
 
Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt
Prostate cancer; breast cancer
Nafarelin
 
Pyr-His-Trp-Ser-Tyr-2Nal-Leu-Arg-Pro-Gly-NH2
Treat symptoms of endometriosis, central precocious
puberty
Triptorelin
 
Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2
Prostate cancer; breast cancer
Antagonists
 
 
Abarelix
Ac-D-2Nal-D-4-chloroPhe-D-3-(3’-pyridyl)Ala-Ser-(N-Me)Tyr-D-Asn-Leu-isopropylLys-Pro-DAla-NH2
Prostate cancer
 
Cetrorelix
Ac-D-2Nal-D-4-chloroPhe-D-3-(3’-pyridyl)Ala-Ser-Tyr-D-Cit-Leu-Arg-Pro-D-Ala-NH2
Prostate cancer; breast cancer
 
Degarelix
 
Ac-D-2Nal-D-4-chloroPhe-D-3-(3’-pyridyl)Ala-Ser-4-aminoPhe(L-hydroorotyl)- D-4-aminoPhe(carbamoyl)-Leu-isopropylLys-Pro-D-Ala-NH2
Prostate cancer
 
Ganirelix
 
Ac-D-2Nal-D-4-chloroPhe-D-3-(3’-pyridyl)
Ala-Ser-Tyr-D-(N9, N10-diethyl)-homoArg-Leu-(N9,
N10-diethyl)-homoArg-Pro-D-Ala-NH2
Fertility treatment
 
 

 
Reference
 
Thundimadathil J.; Cancer treatment using peptides: current therapies and future prospects. J Amino Acids. 2012;2012:967347. doi: 10.1155/2012/967347. Epub 2012 Dec 20.