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.