LIM-0705 + tacrolimus

LIM-0705 + tacrolimus is a combination drug consisting of LIM-0705, a small-molecule compound developed to be administered alongside tacrolimus, and tacrolimus itself, a calcineurin inhibitor. Tacrolimus is widely used as an immunosuppressant to prevent organ transplant rejection by inhibiting T-cell activation through binding FKBP12 and subsequently inhibiting calcineurin phosphatase activity. Tacrolimus reduces IL-2 transcription and T lymphocyte signal transduction. However, it can cause toxicities in organs such as the pancreas, brain, and kidneys. LIM-0705 is designed to activate specific ATP-binding cassette (ABC) transporters in vulnerable tissues to pump out tacrolimus from cells in these organs while preserving its immunosuppressive effect against tissue rejection. This mechanism aims to reduce the toxic side effects associated with tacrolimus without compromising efficacy. The combination has been studied in Phase 1 clinical trials for safety and tolerability in healthy male subjects; results showed that dosing LIM-0705 alone or combined with tacrolimus was safe and well tolerated with favorable pharmacokinetic effects on tissue distribution of tacrolimus[1][6][9].

Other names

FK-506 + LIM-0705