Trenbolone is an anabolic steroid. It is used on livestock to increase muscle growth and appetite. Trenbolone compounds have a binding affinity for the androgen receptor three times as high as that of testosterone. Once metabolized, the drugs have the effect of increasing nitrogen uptake by muscles, leading to an increase in the rate of protein synthesis. It also has the secondary effects of stimulating appetite, reducing the amount of fat being deposited in the body, and decreasing the rate of catabolism. Short-term side effects include insomnia, high blood pressure, increased aggression, night sweats, and libido.

Isoflupredone is a veterinary drug used in cows, pigs and horses for the treatment of wide range of conditions: ketosis, musculoskeletal disorders, hypersensitivity, infections, inflammatory diseases, etc. The drug belongs to the class of corticosteroids and exerts its therapeutic effect by binding to glucocorticoid and mineralocorticoid receptors of animals.

Pralmorelin [GPA 748, GHRP 2, growth hormone-releasing peptide 2, KP-102 D, KP 102 LN] is an orally active, synthetic growth hormone-releasing peptide from a series of compounds that were developed by Polygen in Germany and Tulane University in the US. The use of pralmorelin as a diagnostic agent for GH deficiency is based on its ability to markedly increase plasma levels of GH in healthy subjects irrespectively of gender, obesity or age. However, in patients with GH deficiency, the effect of pralmorelin on GH levels is significantly lower compared with healthy controls. Pralmorelin is marketed under the brand name GHRP in Japan. It is used as a diagnostic agent in a single-dose formulation for the assessment of growth hormone deficiency (GHD). Pralmorelin (GHRP-2) acts to endogenously increase growth hormone release from the pituitary. With the increase of serum growth hormone, downstream effects occur. A notable hormone that is commonly used as a surrogate for growth hormone therapy, insulin like growth factor 1 (IGF-1), is known to increase with the infusion of GHRP-2. Administration of GHRP-2 results in amplification of the naturally occurring growth hormone secretion peaks, regulated by the hypothalamus and pituitary. After the release of growth hormone, a cascade of signaling events occurs in many body tissues, continuous exposure to growth hormone elicits long-term physiological changes. Of particular interest, especially in the case of the use of GHRP-2 as an alternative growth hormone therapy, hepatic production of IGF-1 occurs as result of endogenously released growth hormone from GHRP-2. GHRP-2 acts on the growth hormone secretagogue receptor (GHSR1a) in pituitary and hypothalamic tissues. The growth hormone secretagogue receptor (GHSR) is the natural receptor for the endogenous hormone Ghrelin, a stress hormone produced mainly by the lining of the stomach. This receptor among many other functions, controls and growth hormone release.

Vapreotide (Sanvar) is cyclic octapeptide analog of somatostatin with higher metabolic stability than the parent hormone and developed by Debiopharm Group for the treatment of esophageal variceal bleeding in patients with cirrhotic liver disease and AIDS-related diarrhea. Somatostatin inhibits the secretion of vasodilatory peptides from the gastrointestinal tract, including glucagon, which has been shown to contribute to the maintenance of portal hypertension. While natural somatostatin has a very short half-life (3 min), the elimination half-life of vapreotide is reported to be approximately 10 times longer than that of its parent compound. Pharmacodynamic studies of healthy volunteers demonstrated suppression of gastric acid secretion and inhibition of the secretion of pancreatic enzyme, which is similar to somatostatin. Vapreotide has demonstrated efficacy in the early management of acute variceal hemorrhage but only based on combined primary endpoints of hemostasis and survival after 5 days. In addition, vapreotide’s efficacy is limited to only one major study performed in Europe and not yet in the United States. Although it did not show a significant reduction in mortality, vapreotide’s observed the effect on hemostasis, as well as its favorable safety profile. Adverse effects that occurred in the vapreotide trials were generally mild and primarily included gastrointestinal symptoms and alterations of the gastrointestinal hormonal system. Vapreotide not recommended for approval by an FDA Advisory Panel due to Insufficient evidence that the drug provided a benefit in the treatment for acute esophageal variceal bleeding.

Buserelin is a synthetic peptide analog of the luteinizing hormone-releasing hormone (LHRH) agonist, which stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). Buserelin is used for palliative treatment of prostate cancer, and for treatment of endometriosis. Buserelin is also used for infertility treatment to prepare the pituitary gland before starting treatment with gonadotrophins (FSH and LH) to artificially stimulate ovulation.

Subarachnoid haemorrhage (SAH) following cerebral aneurysm rupture or trauma can result in the induction of secondary ischaemic brain damage via a decrease in microvascular perfusion, a disruption of the blood-brain barrier and consequent vasogenic oedema, and the delayed spasm of the major cerebral arteries (i.e. vasospasm). It is increasingly apparent that oxygen radical-induced, iron-catalyzed lipid peroxidation (LP) within the subarachnoid blood and vascular wall plays a key role in the occurrence of these secondary events. Tirilazad mesylate, is a nonglucocorticoid, 21-aminosteroid, is a potent cytoprotective inhibitor of LP that works by a combination of radical scavenging and membrane stabilizing properties. It has been demonstrated to attenuate the acute and delayed vascular consequences of SAH and to protect the brain against ischaemic insults. Tirilazad mesylate has been proposed to treat acute ischaemic stroke. When tested on animal models, tirilazad protects brain tissue, and reduces brain damage. However, the drug fails to treat, and even worsens a stroke when studied on a human being.

Taltirelin (TA-0910), a synthetic thyrotropin-releasing hormone (TRH) analog, has been developed by Tanabe Seiyaku for the treatment of neurodegenerative diseases. Taltirelin mimics the physiological actions of TRH, but with a much longer half-life and duration of effects, and little development of tolerance following prolonged dosing. Taltirelin has nootropic, neuroprotective and analgesic effects. Taltirelin is primarily being researched for the treatment of spinocerebellar ataxia; limited research has also been carried out with regard to other neurodegenerative disorders, e.g., spinal muscular atrophy.

Quingestanol is a metabolite of the quingestanol acetate, oral contraceptive, which was studied for therapy of menopausal diabetic women. Quingestanol is also a prodrug of norethisterone, which is used in birth control.

Nomegestrol acetate (NOMAC) is a 19-norprogesterone derivative with high biological activity at the progesterone receptor, a weak anti-androgenic effect, but with no binding to estrogen, glucocorticoid or mineralocorticoid receptors. Nomegestrol has been developed by the Monaco-based company Théramex SAM (a Teva subsidiary). Nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea, premenstrual syndrome) and as a component of hormone replacement therapy in combination with estradiol for the relief of menopausal symptoms; it has been approved in Europe as monotherapy for the treatment of the menopausal syndrome, uterine diseases and menorrhagia, and in combination with an estrogen for the treatment of menopausal symptoms. Nomegestrol acetate in combination with estradiol is used as an oral contraceptive.