Tacrolimus, CAS number 104987-11-3, was the second macrolide immunosuppressant discovered, second only to discovery of rapamycin (sirolimus) on Rapa Nui (Easter Island) in 1975. Discovered in 1984, tacrolimus, also known as FK-506 or Fujimycin, is an immunosuppressant drug, often given to organ transplant recipients. Tacrolimus is effective in helping to prevent transplant patients from experiencing organ rejection after a transplant surgery. By working in close collaboration with manufacturers worldwide, LGM Pharma is a preferred supplier of the API tacrolimus for research and development programs.
Anyone who is allergic to hydrogenated castor oil or tacrolimus itself must inform their doctor. Additionally, if patients have used a cyclosporine such as Neoral, Sandimmune or Gengraf they should notify their medical provider as well. Tacrolimus was initially approved by the FDA in 1994 for use in liver transplant patients. Since then this reliable drug has also been approved for use in transplants of the kidney, small bowel, lung, heart, pancreas, skin, cornea, bone marrow, trachea and also limb transplants in patients. Tacrolimus has also shown efficacy in preventing graft-versus-host disease in patients receiving stem cell donations.
Owned by Astellas Pharma Inc. and sold under the trade name Prograf®, tacrolimus is a twice daily regimen under the Prograf brand. Advagraf® is the brand name for the once a day dosing of tacrolimus, and is sold in 0. 5, 1, 3 and 5 milligram strength capsules. Typical doses for once a day treatment of tacrolimus are 0.15 to 0.20 mgs/kgs, and are usually prescribed alongside other post transplant drugs, such as mycophenolate, IL-2 receptor inhibitors and steroids. There is a topical ointment available as well, Protopic, which is used to treat conditions unrelated to post organ transplants, like eczema and atopic dermatitis. Burning and itching are common side effects of Protopia, and it’s use should be avoided for people with malignant skin lesions.
Typical side effects for patients using tacrolimus, both orally and intravenously for post transplant surgery includes nausea, stomach pain, headache, weakness, insomnia and swelling, particularly in the hands and feet. Serious adverse effects are also possible with treatment of tacrolimus, including cardiac, liver and kidney damage, along with a risk of seizures, hyperglycemia, and an increase of existing fungal infections such as herpes zoster.
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