Tacrolimus chemical structure
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Tacrolimus

Tacrolimus (also FK-506 or Fujimycin) is a 23-membered macrolide lactone discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the fungus Streptomyces tsukubaensis. It is an immunosuppressive drug whose main use is after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. more...

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It has similar immunosuppressive properties to cyclosporine, but is much more potent in equal volumes. Also like cyclosporine it has a wide range of adverse interactions, including that with grapefruit which increases plasma-tacrolimus concentration.

It has been used in a topical preparation in the treatment of severe atopic dermatitis, as have cyclosporine and azathioprine with much less success. It has also been used after bone marrow transplants and for severe refractory uveitis.

The drug is owned by Astellas Pharma Inc. (Merging of Fujisawa Pharmaceutical Co.,Ltd. and Yamanouchi Pharmaceutical Co., Ltd as of April 1, 2005) and is sold under the tradename Prograf®. It is sometimes referred to as FK-506, an early name relating to its action. It was first approved by the FDA in 1994 for use in liver transplantation, this has been extended to include kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants.

Tacrolimus is a macrolide antibiotic. It acts by reducing peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This inhibits both T-lymphocyte signal transduction and IL-2 transcription. Although this activity is similar to cyclosporine studies have shown that the incidence of acute rejection is reduced by tacrolimus use over cyclosporine.

Side effects can be severe and include blurred vision, liver and kidney problems (it is nephrotoxic), seizures, tremors, hypertension, hypomagnesemia, diabetes mellitus, hyperkalemia, itching, insomnia, confusion, loss of appetite, hyperglycemia, weakness, depression, cramps, and neuropathy, as well as potentially increasing the severity of existing fungal or infectious conditions such as herpes zoster or polyoma viral infections.

Dermatological use

Protopic® or tacrolimus is a recent topical treatment of eczema, particularly atopic eczema. It suppresses inflammation in a similar way to steroids, but is not as powerful. An important dermatological advantage of tacrolimus is that it can be used directly on the face; topical steroids cannot be used on the face, as they thin the skin dramatically there. On other parts of the body, topical steroid are generally a better treatment. A common side effect of tacrolimus ointment, if used over a wide area, is to cause a burning or itching sensation on the first one or two applications.

Cancer risks

Tacrolimus and a related drug for eczema (pimecrolimus) are being suspected of carrying a cancer risk, though the matter is still a subject of controversy. Dermatologists agree that the drug should be used as a second-line remedy only after conventional methods of treatment have failed. The FDA issued a health warning in March 2005 for the drug, based on animal models and a small number of patients. Until further human studies yield more conclusive results, the FDA recommends that users be advised of the potential risks.

Read more at Wikipedia.org


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AD: tacrolimus treatment cheaper than steroids. (Third-Party Payers). : An article from: Skin & Allergy News $5.95 Tacrolimus may be safer for eyelid dermatitis. (No Glaucoma Risk, Eye Pressure Increase). : An article from: Skin & Allergy News $5.95
Pimecrolimus, tacrolimus black box challenged.(Dermatologic Therapy) : An article from: Skin & Allergy News $5.95 Tacrolimus relieves nickel dermatitis. (Nonsteroidal Ointment). : An article from: Family Practice News $5.95
Topical steroids still tops for atopic dermatitis: guidelines from dermatologists.(Clinical Rounds) : An article from: Internal Medicine News $5.95 Topical tacrolimus tops steroids for AD therapy: large study.(News)(atopic dermatitis) : An article from: Skin & Allergy News $5.95
New Tx Options Emerging for Pediatric Eczema. : An article from: Family Practice News $5.95 Tacrolimus bests pimecrolimus in atopic dermatitis therapy.(Clinical Rounds) : An article from: Pediatric News $5.95
Pimecrolimus, tacrolimus compared head to head: pediatric atopic dermatitis.(Dermatologic Therapy) : An article from: Skin & Allergy News $5.95 Black box recommended for Elidel and protopic.(Skin Disorders) : An article from: Family Practice News $5.95

What is the role of tacrolimus and pimecrolimus in atopic dermatitis?
EVIDENCE-BASED ANSWER When the standard therapies--mild topical corticosteroids and moisturizers--fail in the treatment of atopic dermatitis, patients ...
Are tacrolimus and pimecrolimus effective for psoriasis?
Clinical Question: Is tacrolimus ointment effective for the treatment of facial and intertriginous psoriasis? Setting: Outpatient (specialty) Study ...
Topical tacrolimus: a new therapy for atopic dermatitis - Clinical Pharmacology
Atopic dermatitis is a common problem affecting up to 10 percent of all children. The mainstays of therapy have been oral antihistamines, topical emollients, ...
Annular erythema responding to tacrolimus ointment - Case Reports
Abstract Annular erythema is an unusual, often idiopathic disorder that tends to respond poorly to topical therapy. Two patients with idiopathic, ...
Tacrolimus inhibits T-cell activation - Fk 506 - Washington Whispers - Brief Article
TACROLIMUS (FK 506) INHIBITS T-CELL ACTIVATION by inhibiting the production of IL-2, IL-3, IL-4, TNFa, and GM-CSF. Given the inflammatory basis of many ...
The immunomodulator tacrolimus has shown success in the treatment of psoriasis - Washington Whispers - Brief Article
THE IMMUNOMODULATOR TACROLIMUS HAS SHOWN success in the treatment of psoriasis. The newer immunomodulator pimecrolimus may also be a useful treatment ...
A multicentre, randomized, double-blind, controlled study of long-term treatment with 0.1% tacrolimus ointment in adults with moderate to severe atopic
A Multicentre, Randomized, Double-Blind, Controlled Study of Long-Term Treatment with 0.1% Tacrolimus Ointment in Adults with Moderate to Severe Atopic ...
Topical tacrolimus ointment combined with 6% salicylic acid gel for plaque psoriasis treatment
Topical Tacrolimus Ointment Combined with 6% Salicylic Acid Gel for Plaque Psoriasis Treatment Carroll CL, et al. Archives of Dermatology. 2005;141:43-46.

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