Tacrolimus

Inside the plate · In BMP and TGF-β, Calcium and NFAT

Chemical structure of Tacrolimus
Structure: Tacrolimus, PubChem CID 445643

Approved, for something elseMeasured in people, not heightBy mouthSmall moleculeAlso FK506

A transplant medicine. It grabs a small protein, and the pair switches off the enzyme that lets a cartilage transcription factor into the nucleus. That same small protein is also a catch on the bone-building receptor.

A macrolide immunosuppressant. It binds FKBP12, and the complex inhibits calcineurin, the phosphatase that strips the phosphates keeping NFAT out of the nucleus. The same FKBP12 restrains the BMP type I receptor, which is why the drug turns up in fibrodysplasia ossificans progressiva research. Approved for prophylaxis of organ rejection in adult and paediatric recipients of allogeneic kidney, liver, heart or lung transplants, in combination with other immunosuppressants.

Prograf label

Risks. Its label carries the strongest class of warning there is, for cancers and serious infections that can lead to hospital or death. It also damages the kidneys and the nerves, raises blood pressure and blood sugar, thickens the heart muscle and rules out live vaccines.

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