Cetrorelix Acetate

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

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..

Exenatide Acetate

A 39-amino acid peptide originally isolated from the salivary glands of the Gila monster (Heloderma suspectum), differs from exendin-3 only in two positions close to the N-terminus. Application of exenatide causes an increase in acinar cAMP without stimulating amylase release. As an incretin mimetic, exenatide acts as agonist of the glucagon-like peptide-1 (GLP-1) receptor.

Fertirelin Acetate

Fertirelin acetate is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.

Atosiban

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%.

Exenatide

Exendin-4 (exenatide), a 39-amino acid peptide originally isolated from the salivary glands of the Gila monster (Heloderma suspectum), differs from exendin-3 only in two positions close to the N-terminus. Application of exenatide causes an increase in acinar cAMP without stimulating amylase release. As an incretin mimetic, exenatide acts as agonist of the glucagon-like peptide-1 (GLP-1) receptor. As GLP-1, though with prolonged activity, exenatide augments the postprandial production of insulin and suppresses secretion of glucagon. For this reason, exenatide has found use as a medication of diabetes II.

Terlipressin

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.

Protirelin

Protirelin is a highly conserved neuropeptide that exerts the hormonal control of thyroid-stimulating hormone (TSH) levels as well as neuromodulatory functions.

Eptifibatide Acetate

Eptifibatide, is an antiplatelet drug of the glycoprotein IIb/IIIa inhibitor class. Eptifibatide is a cyclic heptapeptide derived from a protein found in the venom of the southeastern pygmy rattlesnake (Sistrurus miliarius barbouri). It belongs to the class of the so-called RGD (arginine-glycine-aspartate)-mimetics and reversibly binds to platelets.

Icatibant

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.