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tacrolimus immediate-release + tacrolimus extended-release
- Development stage
- Unknown
- Lead developer
- Astellas Pharma
- Modality
- Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
This is a combination of two formulations of the same active ingredient, tacrolimus, an immunosuppressant macrolide. Prograf is the immediate-release formulation of tacrolimus, typically administered every 12 hours, while Advagraf is an extended-release formulation designed for once-daily dosing. Both are used to prevent organ rejection in patients who have received allogeneic transplants (kidney, liver, heart), and both require careful therapeutic drug monitoring due to a narrow therapeutic index and variable pharmacokinetics. The mechanism of action involves inhibition of calcineurin in T cells by binding to FKBP12 (FK506-binding protein), thereby suppressing T-cell activation and proliferation. Both products are developed and manufactured by Astellas Pharma[1][3][6][7].
- Brand names
- PrografAdvagraf
- Other names
- tacrolimus immediate-release + tacrolimus extended-releaseFK506FK-506FK 506
02
Targets
FKBP1ACN (Calcineurin)
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