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Authors: Vanessa Ngan, Staff Writer, 2004. Updated: Dr Kelvin Truong, Dermatology Research Fellow, Westmead Hospital, Sydney, Australia; Dr Martin Keefe, Dermatologist, Christchurch, New Zealand. Copy edited by Gus Mitchell. September 2021.
Tacrolimus is a macrolide calcineurin inhibitor immunosuppressant drug available as a topical ointment, oral capsule, and intravenous injection. It was initially isolated from the soil fungus Streptomyces tsukabaenis.
Tacrolimus may be used to treat these skin conditions
Topical tacrolimus may be used to treat these skin conditions
Tacrolimus is a lipophilic molecule; for topical use it is formulated as an ointment. Percutaneous absorption is minimal except where there is an epidermal barrier defect such as in active atopic dermatitis. As disease activity settles, absorption through the skin reduces.
Tacrolimus is metabolised by cytochrome P450 in the liver. Tacrolimus is not metabolised in the skin.
Polymorphisms in the CYP3A5 gene affect the bioavailability of systemic tacrolimus with CYP3A5 non-expressors requiring a higher dose of systemic tacrolimus post-transplant.
Tacrolimus suppresses the cell-mediated immune response.
The Food and Drug Administration (FDA) has a black box warning for a possible increase in cancer risk including skin cancers and lymphoma. Evidence is conflicting with topical use so the risk, if any, is probably very small.
If you are not based in New Zealand, we suggest you refer to your national drug approval agency for further information about medicines (eg, the Australian Therapeutic Goods Administration and the US Food and Drug Administration) or a national or state-approved formulary (eg, the New Zealand Formulary and New Zealand Formulary for Children and the British National Formulary and British National Formulary for Children).
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