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Tacrolimus
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DRUG INFO
Tacrolimus
Drug Name:
Tacrolimus
Indication: Tacrolimus is indicated for the prophylaxis of organ rejection in patients receiving allogeneic liver or kidney transplants. Used in a topical preparation in the treatment of severe atopic dermatitis, also used after bone marrow transplants and for severe refractory uveitis.
Pharmacology: Tacrolimus, a macrolide immunosuppressant produced by Streptomyces tsukubaensis, is an immunosuppressive agent indicated for the treatment of patients receiving kidney and/or liver transplants. Tacrolimus has been demonstrated to suppress humoral immunity and, to a greater extent, cell-mediated reactions such as allograft rejection, delayed type hypersensitivity, collagen- induced arthritis, experimental allergic encephalomyelitis, and graft versus host disease. It has similar immunosuppressive properties to cyclosporine, but is much more potent in equal volumes.
Mechanism Of Action: Tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. A complex of Tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This prevents the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines. Tacrolimus also inhibits the transcription for genes which encode IL-3, IL-4, IL-5, GM-CSF, and TNF-, all of which are involved in the early stages of T-cell activation. Additionally, Tacrolimus has been shown to inhibit the release of pre-formed mediators from skin mast cells and basophils, and to downregulate the expression of FceRI on Langerhans cells.
Drug Category: Immunosuppressive Agents; ATC:D11AX14; ATC:L04AA05
Brand Names/Synonyms: FK 506; FK-506; FK5; K506; Prograf; Protopic; Tacarolimus; Tacrolimus
Dosage Forms: CAPSULE; OINTMENT; SOLUTION
Absorption: Generally incomplete with absolute bioavailability of 17-22%
Interactions:
DrugBank: Interactions for Tacrolimus
Interactions for Tacrolimus:
Formal topical drug interaction studies with PROTOPIC Ointment have not been conducted. Based on its minimal
extent of absorption, interactions of PROTOPIC Ointment with systemically administered drugs are unlikely to occur
but cannot be ruled out. The concomitant administration of known CYP3A4 inhibitors in patients with widespread and/or
erythrodermic disease should be done with caution. Some examples of such drugs are erythromycin, itraconazole,
ketoconazole, fluconazole, calcium channel blockers and cimetidine.
Chemical IUPAC Name: [3S-[3R*[E(1S*,3S*,4S*)],4S*,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26aR*]]-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5, 19-dihydroxy-3- [2-(4-hydroxy-3-methoxycyclohexyl) -1-methylethenyl]-14, 16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-15, 19-epoxy-3H-pyrido[2,1-c][1,4] oxaazacyclotricosine-1,7,20, 21(4H,23H)-tetrone, monohydrate
Chemical Formula: C44H69NO12
Half Life: 11.3 hours (range from 3.5 to 40.6 hrs)
Drug Type: Approved Drug
# Accession No: APRD00276
CAS Registry Number: 104987-11-3
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Tacrolimus News
(When available)
EFI Proofing Solutions Jan 13, 2006
R9005 Designportal, EFI participated with three systems composed of Colorproof XF and Canon Image Prograf 6400PG, Epson Stylus Pro 4800 and HP DesignJet 90 respectively. ...
NDA for Immunosuppressant FK506 Modified Release Formulation ... Dec 27, 2005
PharmaLive.com (press release), It is marketed as an agent to suppress rejection after organ transplantations under the brand name of Prograf in over 70 countries in the world. ...
Inhaled Cyclosporine Boosts Survival of Lung Recipients Jan 12, 2006
MedPage Today, All patients also received conventional immunosuppression with Prograf (tacrolimus) at 0.06 mg/kg/day, Imuran (azathioprine) at 2 mg/kg/day, and prednisone at ...
Astellas Pharma Submits NDA for FK506 Immunosuppressant to FDA Dec 26, 2005
Japan Corporate News (press release), FK 506 (tacrolimus), which was discovered by Astellas Pharma, is now prescribed in about 70 countries worldwide under the trade name of Prograf. ...
Moisture loss leads to dry, itchy skin woes Jan 9, 2006
Newark Star Ledger, ...or reverse the process. The use of prescription immunomodulators like Protopic and Elidel are effective treatment. Both of these ...
Elements Home Spa Announces Promotional Pricing on its Very ... Jan 5, 2006
PR Web (press release), ...advisory to inform healthcare providers and patients about a potential cancer risk from the use of Elidel (pimecrolimus) and Protopic (tacrolimus), products ...
Bird Flu, Cloning, Katrina: Top Health Stories of 2005 Dec 27, 2005
FOX News ...concerns. Eczema skin creams Elidel and Protopic, because of fears they may increase the risk of skin cancer and lymphoma. Abortion ...
Drug firm investing up to $5M on WNY operations Dec 19, 2005
MSNBC The plant makes and packages a proprietary skin ointment named Protopic, a prescription medication used to treat moderate to severe cases of eczema in adults ...
Consumer Reports Examines Weaknesses of Current Drug-safety System Dec 27, 2005
Kansas City infoZine, Tegaserod (Zelnorm) for irritable bowel syndrome with constipation; and topical immunosuppressants pimecrolimus (Elidel) and tacrolimus (Protopic) for eczema. ...
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