Drugs profiles

Raloxifene hydrochloride is a second generation selective estrogen receptor modulator (SERM) of the benzothiophene family. This drug is similar in its effects to the drug tamoxifen (nolvadex), exhibiting estrogen receptor antagonist properties in some tissues while acting as an estrogen receptor agonist in others. The main point of variation between the two drugs is their tissue selectivity. While raloxifene hydrochloride is a strong anti-estrogen in breat and uterine tissues, it appears to be estrogenic in bone. This allows it to protect bone density, mimicking the effects of endogenous estradiol. This is quite different than nolvadex, which is anti estrogenic in both breast and bone. In a role that novel for an anti-estrogen, raloxifene was approved by the FDA for the prevention and treatment of osteoporosis in post menopausal women. It is also being investigated for several other potential uses, including the treatment and prevention of cardiovascular disease. Raloxifene was developed by Eli Lilly & Company, and the FDA approved for U.S sale in 1997. Its first indictated use was as that of an osteoporosis treatment, owing to its ability to increase bone density. In 2007, the FDA expanded the indicated uses for the drug to include reducing the risk of invasive breast cancer in two  populations. Today, the drug is a fairly popular drug in clinical medicine, and is approved for sale in over 50 countries. The most common brand name is Evista and dominates the global market.

Toremifene citrate is an anti-estrogenic drug, specifically classified as a selective estrogen receptor modulator (SERM) with mixed agonist and antagonist properties. It is a non steroidal triphenylethylene derivative, similar in structure to both the drugs nolvadex and clomid. Toremifen citrate is used for the treatment of breast cancer in postmenopausal women with the estrogen receptor positive or estrogenic receptor unknown tumors. It works by attaching to the estrogen receptor in various tissues in a competitive manner, blocking endogenous estrogen from exerting biological activity. Toremifene citrate was first approved by the FDA as a prescription drug in 1997. It is sold in the U.S under the Fareston brand name, which is made by the pharmaceutical company Gtx Inc. Fareston is also available in over 25 other countries worldwide. Fareston is most commonly supplied in tablets of 88.4mg, which are labeled and equate to 60mg of toremifene base.

Fulvestrant is a highly selective estrogen receptor antagonist. It exerts its action in the body not by targeting the production of estrogen, but by preventing it from exerting activity on the body. It does this by binding available estrogen receptors in a competitive manner, making them unavailable for circulating estrogens. This mode of action is very similar to Nolvadex and Clomid, although unlike these two agent fulvestrant does not have mixed agonist/antagonist properties. It is a pure estrogen receptor antagonist. This agent also stands out as the first inject able estrogen antagonist to catch the attention of the athletic and bodybuilding world. Although not widely used here, when applied it may be effective drug for mitigating the side effects of excess estrogen caused by anabolic/androgenic steroid use such as gynecomastia, fat buildup, and increased water retention. Fulvestrant was developed by the pharmaceutical company AstraZeneca. It was approved as a prescription drug in the U.S in 2002, and is sold under the brand name of Faslodex. The drug is indicated for the treatment of estrogen receptor positive breast cancer with disease progression following traditional anti estrogen treatment with drugs  such as nolvadex. The company has since expanded  its market for Faslodex to include over a dozen countries worldwide.

Letrozole is a non steroidal selective third generation aromatse inhibitor. The structure and activity of this compound are very similar to that of Arimidex, and is prescribed for similar medical reasons. More specifically, United States prescribing guidelines for leptosome recommend it to be used for the treatment of postmenopausal women with estrogen receptor positive or estrogen receptor unkown brest cancer. It is typically used as a second line of treatment after an estrogen receptor antagonist like tamoxifen has failed to elicit a deseribale response, although it is sometimes initiated as the first course of therapy depending on the circumstances. Male bodybuilders and athletes find value in leptosome for its ability to mitigatge the estrogenic side effects associated with the use of aromatically anabolic/androgenic steroids, such as gynecomastia, fat buildup, and visible water retention. The U.S FDA approved leptosome for prescription sale in 1997, where it is sold by  the pharmaceutical company Novartis under the brand name of Femera. The company also markets the drug in over 70 nations worldwide. The drug is most commonly supplied in dosages of 2.5mg.

Tamoxifen citrate is a non steroidal anti estrogenic drug, used widely in clinical medicine. It is specifically a selective estrogen receptor modulator of the triphenylethylene family, and posses both estrogen agonist and antagonist properties. As such, it may act as an estrogen in some tissues while acting as an anti-estrogen in others. In breast tissue the drug is a strong anti estrogen and as a result is commonly used in the treatment of estrogen related breast cancer in women. Tamoxifen citrate was first developed in 1962 by the pharmaceutical company ICI. It was made commercially available in the United States not long after, but its initial use was for the treatment of female infertility, a purpose for which the drug does not seem ideally suited for. It was not until 1977 that the FDA approved the drug for use in the United States for the treatment of breast cancer. The drug has been sold by ICI in a number of worldwide markets under the brand name of Nolvadex. The drug is most commonly supplied in tablets containing either 10mg of 20mg of the drug.

Testolactone is a first generation non selective steroidal aromatase inhibitor, used clinically to treat estrogen dependant breast cancer. Its exact mode of funciton is unkown, but it is believed to inhibit the aromatase enzyme in a noncompetitive and irreversible manner. If so, this would be an activity that is very similar to that of Lentaron. This might also explain why cessation of the drug does not provide an immediate restoration of normal estrogen production. Like formestane, it takes several days after ceasing use for the body to replenish its enzyme levels. Testolactone was first approved by the FDA as a prescription drug back in 1970. It was an early anti estrogenic drug, exhibiting a moderately pronounced effect but failing to reach levels of high clinical success. As other more successful medications began to surface for the treatment of breast cancer, testolactone would not see the success that had been planned for it. Currently, the United States is the only country where the product has not been discontinued. Testolactone is most commonly supplied in tablets of 50mg.

GH-releasing hexapeptide (GHRP-6) is a secratogue that stimulates the release of growth hormone (GH) by acting at both hypothalamic and pituitary sites which has been clinically documented in a wide variety of species in vivo and in vitro. GHRP-6 duplicates the way the growth hormone works in the body. In studies it not only has shown to enhance growth hormone levels, but also increased the pulsatile secretory bursts of GH. Another remarkable trait of GHRP-6 is its increase in normal pulsatile physiological secretion by its hypothalamic action. Initial studies with GHRP-6 suggested that this compound acted primarily on the pituitary gland and was absolutely specific for GH release. More recent studies have qualified both of these assumptions. This peptide has been clinically verified to increase GH levels, increase appetite, raise IGF-1 levels, help sleep cycles and more.

Human growth hormone is an important mediator of the human growth process. This hormone is produced endogenously by the anterior pituitary gland, and exist at especially high levels during child hood. Its growth supporting effects  are broad and can be separated into three main categories which are bone, skeletal muscle, and internal organs. It also supports protein, carbohydrate, lipid, and mineral metabolism, and can stimulate the growth of connective tissues. Although vital to the roles of early development, human growth hormone is produced throughout adulthood. Its production and biological role decline significantly with age however, but continue to support metabolism and muscle and tissue growth throughout life. In a medical setting this drug  is used to treat a number of distinct health conditions. It is most notably associated with pituitary deficient dwarfism, a disease in which growth is hindered due to the body’s lack of natural growth hormone production. The first human growth hormone medications were made from pituitary extracts of human origin. These were commonly referred to as cadaver growth hormone preparations. It was later determined that using these preparations was causing patients to develop the fatal brain disorder CJD. Because of this, the FDA banned the cadaver made preparations of this drug. Years later, synthetic methods of producing human growth hormone were developed and the FDA approved them in 1985 for medical use.

Insulin like growth factor-1 (IGF-1) is a substance which in manufactured by recombinant DNA technology. IGF-1 is the primary mediator of the growth promoting effects of human growth hormone. As such, the substance also can stimulate the growth of bone, muscle, and internal organs. Its effects on skeletal muscle are also highly hyperplasic, meaning it causes an increase in cell number. Unlike human growth hormone, however, this substance has very strong insulin like effects. It can support growth by increasing the uptake of amino acids, glucose, and fatty acids, but lowers blood sugar levels so efficiently that it can induce severe hypoglycemia if to high of a dose is taken. The increased uptake of fatty acids may also mean that the drug can increase the amount of body fat that is stored by the users. The United States FDA approved the medical use of IGF-1 in 2005. It is sold under the brand  name of Increlex manufactured by the pharmaceutical company Tercica Inc. Tercica licenses this technology from Genentech, which was the first company to sell synthetic human growth hormone in the United States.

Somatrem is a synthetically manufactured form of human growth hormone. It is actually a variant of endogenous human growth hormone protein, containing the same sequence of 191 amino acids, but with the addition of an extra amino acid, methionine. For this reason somatrem is commonly described as methionyl human growth hormone. As an human growth hormone medication, somatrem supports the growth of bone, skeletal muscle, connective tissues, and internal organs. It also plays a role in protein, carbohydrate, lipid, and mineral metabolism. In a medical setting, somatrem is used to treat childen with growth failure caused by endogenous growth hormone deficiency. When administered as a long term treatment before linear growth is stopped due to closed growth plates, the drug may impart a significant positive effect on linear  growth. Somatrem is considered to be therapeutically equivalent to growth hormone or pituitary origin. As an human growth hormone drug, somatrem is valued by bodybuilders and athletes for its ability to promote fat loss and muscle and connective tissue growth. Somatrem was approved for sale by the FDA in the United States in 1985. It was the first synthetic growth hormone medication available worldwide, produced via a manufacturing process called Inclusion Body Technology. The technology involves inserting the DNA encoding for the human growth hormone protein into Escherichia coli bacteria, which assemble and synthesize the pure protein. Prior to the advent of synthetic growth hormone, HGH was made into a medication only by extracting the natural protein from human cadavers. Biological or cadaver HGH, as it was called, was banned in the U.S in 1985 due to the high prevalence of a rare neurological disease known as CJD in patients. Somatrem was approved for sale that same year, giving the company that produced it a short monopoly on the growth hormone market. Somatrem is most commonly supplied in multi dosed vials containing a while lyophilized powder that requires reconstitution with sterile or bacteriostatic water before use.