Tacrolimus Formulations
Tacrolimus is available as a topical ointment in 0.03% and 0.1% concentrations for dermatologic use, and as oral capsules (0.5 mg, 1 mg, 5 mg) and intravenous solution for transplant rejection prophylaxis. 1
Topical Formulations for Lupus Skin Flares
For patients with lupus skin manifestations, topical tacrolimus ointment 0.1% is the appropriate formulation and has demonstrated efficacy in treating resistant cutaneous lesions. 2, 3
Available Topical Concentrations
- 0.03% ointment: Approved for children ages 2-15 years 2, 4
- 0.1% ointment: Approved for patients 16 years and older; this is the concentration used in lupus studies 2, 4
Application for Lupus
Apply tacrolimus 0.1% ointment twice daily to affected facial and cutaneous lesions. 3, 5, 6 The ointment is marketed under the brand name Protopic in the United States for dermatologic use, though its use in lupus is off-label. 2
Clinical Evidence in Lupus
The topical formulation shows variable efficacy depending on lupus subtype:
- Best response: Facial erythematous lesions in systemic lupus erythematosus (SLE) with edematous or telangiectatic changes, with marked improvement seen in 4-8 weeks 3, 5, 6, 7
- Moderate response: Subacute cutaneous lupus erythematosus (SCLE) lesions show mixed results 3, 8
- Limited response: Chronic discoid lupus erythematosus (DLE) with typical discoid plaques often shows poor response, likely due to chronicity and scarring 3, 6, 8
Important Caveats
Tacrolimus ointment should not be applied to moist skin or immediately after bathing to minimize burning and irritation, which are the most common side effects. 4 The medication is particularly useful for facial lesions where long-term corticosteroid use would risk skin atrophy. 2, 4
Systemic Formulations (Not for Lupus Skin Disease)
Oral capsules (0.5 mg, 1 mg, 5 mg) and intravenous solution are FDA-approved only for transplant rejection prophylaxis, not for lupus treatment. 2, 1 These systemic formulations have insufficient evidence for managing cutaneous lupus and carry significant immunosuppression risks. 2