Products Nafarelin is commercially available as a nasal spray (Synrelina). It has been approved in many countries since 1992. Structure and properties Nafarelin (C66H83N17O13, Mr = 1322.5 g/mol) is an agonist derivative and analog of gonadotropin-releasing hormone (GnRH). It is present in the drug as nafarelin acetate. It is a decapeptide that is administered nasally … Nafarelin
Products Gonadorelin is commercially available as an injectable (Lutrelef). It has been approved in many countries since 1983. Structure and properties Gonadorelin is a decapeptide. It is chemically and biologically identical to GnRH, which is released pulsatile by the hypothalamus. It is present in drugs as gonadorelin acetate, a white to slightly yellowish powder that … Gonadorelin
Products Goserelin is commercially available as a solid depot (Zoladex, generic). It has been approved in many countries since 1990. Structure and properties Goserelin is an analog of gonadotropin-releasing hormone (GnRH) and is present in drugs as goserelin acetate, a decapeptide and white powder that is soluble in water. Goserelin: Pyr-Glu-His-Trp-Ser-Tyr-D-Ser(But)-Leu-Arg-Pro-Azgly. GnRH: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly Effects Goserelin … Goserelin
Products There are no human medicines containing buserelin on the market in many countries. Structure and properties Buserelin is a synthetic nonapeptide analogous to human gonadotropin-releasing hormone with agonistic activity for gonadorelin. Effects Buserelin (ATC L02AE01) is an analog of gonadotropin-releasing hormone (GnRH). Indications Endocrine treatment of advanced hormone-dependent prostate cancer, but not with prior … Buserelin
Products Peforelin is commercially available as a solution for injection for animals. It has been approved in many countries since 2009. Structure and properties Peforelin is a synthetic analog of gonadotropin-releasing hormone (GnRH) in which four amino acids have been exchanged. Effects Peforelin (ATCvet QH01CA) selectively stimulates the release of FSH and promotes follicular growth, … Peforelin
Products Follitropin alfa is commercially available as an injectable. It has been approved in many countries since 1995. Biosimilars are approved in some countries (Switzerland: Ovaleap, 2018). Structure and properties Follitropin alfa is a follicle-stimulating hormone (FSH) produced by biotechnological methods. It is a heterodimer and consists of two distinct glycoproteins, the α-subunit (92 amino … Follitropin Alfa
Products Follitropin beta is commercially available as a solution for injection (Puregon). It has been approved in many countries since 2001. Structure and properties Follitropin beta is a recombinant human follicle-stimulating hormone (FSH) produced by biotechnological methods. The amino acid sequence corresponds to human FSH. It differs from follitropin alfa in glycosylation. FSH is a … Follitropin Beta
Products GnRH analogs are commercially available in many countries in the form of injectables, implants, and nasal sprays, among others. The first agent to be approved was goserelin (Zoladex) in 1990. Structure and properties GnRH analogs are synthetically produced derivatives of gonadotropin-releasing hormone (GnRH, LHRH) produced in the hypothalamus. GnRH is a decapeptide and has … GnRH Analogs
Effects GnRH antagonists are competitive antagonists of GnRH at pituitary receptors, inhibiting the release of LH and FSH. Indications Suppression of premature LH peaks and prevention of premature ovulation in women undergoing assisted reproductive medicine. Prostate cancer in adult men (degarelix). Agents Cetrorelix (Cetrotide) Degarelix (Firmagon) Ganirelix (Orgalutran, out of trade)
Products Triptorelin is commercially available as an injectable. It has been approved in many countries since 1995. Structure and properties Triptorelin is a more potent derivative of gonadotropin-releasing hormone (GnRH). At position 6, the amino acid glycine has been replaced by D-tryptophan. It is a decapeptide. GnRH: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly. Triptorelin: Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly Effects Triptorelin (ATC L02AE04) is … Triptorelin
Products Enzalutamide was initially registered in capsule form (Xtandi). Film-coated tablets were approved in many countries in 2019. They are smaller and therefore easier to take. Enzalutamide was approved in the United States in 2012 and in many countries and the EU in 2013. Structure and properties Enzalutamide (C21H16F4N4O2S, Mr = 464.4 g/mol) is an … Enzalutamide
Products Leuprorelin is commercially available as an injectable and implant. It has been approved in many countries since 2004. Structure and properties Leuprorelin is present in drugs as leuprorelin acetate. The nonapeptide is a synthetic analog of the natural gonadotropin-releasing hormone GnRH. GnRH: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly. Leuprorelin: 5-oxo-Pro-His-Trp-Ser-Tyr-D-Leu-Arg-N-ethyl-L-prolinamide Effects Leuprorelin (ATC L02AE02) inhibits the secretion of LH … Leuprorelin
