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Icatibant (Firazyr) is a synthetic peptidomimetic drug consisting of ten amino acids, and acts as an effective and specific antagonist of bradykinin B2 receptors. It has been approved in the EU for use in hereditary angioedema, and is under investigation for a number of other conditions in which bradykinin is thought to play a significant role.
Terlipressin is a synthetic triglycyllysine derivative of vasopressin with vasoconstrictive, antihemorrhagic, and antidiuretic properties. Upon intravenous administration, terlipressin, an inactive prodrug, is biotransformed to its active moiety, lysine vasopressin (LVP), a nonselective vasopressin analogue with affinity for vasopressin receptors V1 (V1a), V2 and V3 (V1b). As a V1 agonist, terlipressin increases systemic vascular resistance, particularly in the splanchnic area, resulting in a decrease of portal pressure. V1 binding also promotes platelet aggregation and glycogenolysis, while V3 binding induces adrenocorticotropic hormone (ACTH) secretion. Compared to vasopressin, terlipressin has a minimal effect on V2 receptors, which are responsible for promotion of water reabsorption in the collecting ducts of the kidney via stimulation of cyclic AMP production.
Pramlintide is an analogue of amylin, a small peptide hormone that is released into the bloodstream by the β-cells of the pancreas along with insulin, after a meal. Like insulin, amylin is completely absent in individuals with Type I diabetes.
Angiotensin II human (Angiotensin II) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis.
Abarelix is a synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It directly and competitively binds and blocks the gonadotropin releasing hormone receptors in the anterior pituitary, which inhibits the secretion and release of the luteinizing hormone (LH) and follicle stimulating hormone (FSH). For men, the inhibition of LH secretion prevents the release of testosterone. Therefore, it can relieve symptoms associated with prostate hypertrophy or prostate cancer.
Cetrorelix Acetate is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 1.21 nM). It can suppress production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland which inhibits ovulation, exhibit antiproliferative effects and display efficacy against hormone-sensitive cancers in vivo. It is often used to treat hormone-sensitive cancers of the prostate and breast.
Degarelix (INN) or degarelix acetate (USAN) (trade name Firmagon) has an immediate onset of action, binding to gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland and blocking their interaction with GnRH. This induces a fast and profound reduction in luteinising hormone (LH), follicle-stimulating hormone (FSH) and in turn, testosterone suppression. Testosterone is a male hormone that promotes growth of many prostate tumours..
Deslorelin acetate is an injectable gonadotropin releasing hormone super-agonist (GnRH agonist) also known as an LHRH agonist. It stops the production of sex hormones (testosterone and oestrogen).
Teriparatide(recombinant human parathyroid hormone) /PTH (1-34) (human) corresponds to the N-terminal part of human parathyroid hormone, a peptide consisting of 84 amino acids.
Atosiban is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban is indicated to delay imminent pre-term birth in pregnant adult women. Atosiban is useful in improving the pregnancy outcome of in vitro fertilization-embryo transfer (IVF-ET) in patients with repeated implantation failure (RIF). The pregnancy rate improved from zero to 43.7%.