TACROLIMUS

Overview
Tacrolimus is a drug that suppresses the immune system and is mainly used to prevent rejection of transplanted organs. Tacrolimus accomplishes its immune-suppressing effecting by inhibiting an enzyme (calcineurin) crucial for the multiplication of T-cells, cells that are vital to the immune process.


Uses:
Tacrolimus is mainly used after an organ transplant, to lower the risk of organ rejection by reducing the activity of the patient's immune system.The use of Tacrolimus allows transplantation specialists to reduce the dose of steroids, which are also used to prevent rejection. This "steroid-sparing effect" is important because of the many side effects that can occur when larger doses of steroids are used for a long period of time.

It is also used in a topical preparation to treat Atopic dermatitis (eczema), severe refractory uveitis after bone marrow transplants, Psoriasis, and the skin condition Vitiligo. It is equally as effective as a mid-potency steroid. An important advantage of Tacrolimus is that, unlike steroids, it does not cause skin thinning (atrophy) or other steroid related side effects. It may therefore be used continuously on the body and applied to the thinner skin over the face and eyelids.


Mode of Action:
Tacrolimus reduces peptidyl-prolylisomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription. The action of transcription factors requiring dephosphorylation is thus inhibited, leading to the blockade of interleukin-2 gene transcription, an early event in the immunological cascade.

Tacrolimus is also known to suppress the early stage T-cell activation by inhibiting the transcription for genes which encode IL-3, IL-4, IL-5, GM-CSF, and TNF.

Although this immuno-suppressant activity is similar to cyclosporine, studies have shown that the incidence of acute rejection during organ transplants is reduced by Tacrolimus in comparison to the use of cyclosporin


Production:
We produce Tacrolimus from the fungal culture Streptomyces tukkugudaensis, which was identified in a remote village in India and carefully cultivated through years of hard work at our R&D department.

The raw bulk is produced using our proprietary process in a sterile fermentation facility, and is followed by the appropriate downstream purification protocols. All of this is performed under strict cGMP conditions. The final purified bulk drug emerges in dry crystalline form.

Our Quality Control Department undertakes rigorous assay procedures at every step, from production until final dispatch of each consignment. Every gram of Tacrolimus at Transgene conforms to a detailed and specified series of quality control assays.


Sales
Tacrolimus can be supplied in Gram or Kilogram quantities. If you are interested in buying our product, please contact us.

Sample Certificate of Analysis
 
 
 

ORLISTAT

Overview:
The World Health Organization estimates that by the year 2015, approximately 2.3 billion adults worldwide will be overweight, and more than 700 million will be obese. In most developed countries, obesity has become an epidemic of alarming proportions and a leading public health concern.

Obesity is a leading cause of death and is associated with many of the top 10 diseases with the highest mortality rates, including diabetes, heart disease, stroke, and cancer. For these reasons, effective interventions to treat overweight and obesity are much needed, including those with only modest effects. Research has shown that even small losses in weight, such as 5%–10% of baseline weight, may have clinical importance and may reduce blood pressure, glucose, cholesterol and triglycerides levels, potentially moderating cardiovascular diseases and diabetes.

Orlistat currently is the most studied anti-obesity drug in the world, and is associated with the least-severe adverse effects. Pharmacological treatment of obesity has become widely used in most countries, although the number of available drugs is still very limited. Till recently, there were two drugs, orlistat and sibutramine, approved by the US Food and Drug Administration (FDA) and European Medical Agency (EMEA) for the long-term treatment of obesity and overweight in the European Union and the United States. However, since sibutramine was banned due to severe adverse effects, Orlistat has come to be the only drug of choice for long term treatment of obesity.

Orlistat (tetrahydrolipstatin) is a lipase inhibitor that blocks about one-third of intestinal fat absorption. Orlistat is the saturated derivative of lipstatin—a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. The empirical chemical formula for Orlistat is C29H53NO5.


Uses:
Because of its effects on the absorption of fats, Orlistat is mainly used in the treatment of obesity. It was approved by the U.S. Food and Drug Administration (FDA) in 1999, and is recommended for obese people with a body mass index (BMI) of more than 30 kilograms per square meter. It is also recommended when peoples’ BMI is between 27 and 30 kilograms per square meter and other heath considerations such as high blood pressure, elevated blood cholesterol, or diabetes are detrimental to their lives. Medical studies found that when taken for six months, adults lost 12.4 to 13.4 pounds on average.

Orlistat was introduced into the marketplace primarily because of the increasing number of overweight or obese people in the United States and other countries around the world. According to the National Institutes of Health (NIH), as of 2007, about 65% of all U.S. adults are overweight or obese. NIH scientists have shown that being overweight or obese can lead to increased risk of developing health issues such as high blood pressure, heart disease, arterial disease, and type-2 diabetes. According to the World Health Organization (WHO), over one billion adults are overweight in the world, and at least 300 million of them are considered obese.

It is also increasingly being used in the management of type 2 diabetes and hyperlipidemia.


Mode of Action
Orlistat prevents the digestion and absorption of dietary fats into the bloodstream so that, instead, they pass through bowel movements within the feces, reducing the amount of calories that go into the human body. Inside the human body, Orlistat diminishes the production of pancreatic lipase, which is an enzyme that decomposes triglycerides within the intestines. When pancreatic lipase is not present, triglycerides that are ingested within foods are stopped from being hydrolyzed into free fatty acids. They are, instead, excreted through bowel movements within feces without being digested. Orlistat, itself, is only slightly absorbed into the body. Most of it is taken into the gastrointestinal tract and eventually removed through the feces.


Technology
Development of Orlistat at Transgene is a result of intensive research for several years. Our scientists have optimized the production of a key metabolite, Lipstatin, through a complex biochemical process using Streptomyces toxitricini strain for fermentation and employing further purification steps. A series of chemical synthesis steps follow this for the final production of tetra-hydro-lipstatin (Orlistat), a derivative of lipstatin.
 
 
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