Minodronic acid

Minodronic acid (YM-529) is an FPP synthase inhibitor with an IC₅₀ of 3 nM, and also an antagonist of P2X2/3 receptors with an IC₅₀ of 62.7 μM. Minodronic acid induces tumor cell apoptosis and inhibits cell growth. Minodronic acid also suppresses bone resorption. Minodronic acid can be used in research related to osteoporosis and cancer^[1][2]. In Vitro:Minodronic acid (5-100 μM; 72 h) inhibits the proliferation of human bladder cancer cell lines 253J, 5637, RT4, RT112, TCCSUP, KU-7 and UM-UC-3 in a dose-dependent manner^[1].
Minodronic acid (30 μM; 48 h) induces apoptosis in human bladder cancer cells^[1].
Minodronic acid (0.25-2.0 × IC₅₀; 72 h) exhibits synergistic or additive antiproliferative effects when combined with Cisplatin (HY-17394) or Paclitaxel (HY-B0015) in human bladder cancer cell lines KU-7, RT112 and UM-UC-3^[1].
Minodronic acid (0.1-1 μM; 3 days) potently inhibits osteoclast-mediated bone resorption in rabbits and induces dose-dependent morphological changes; at 1 μM, it almost completely inhibits bone resorption and causes osteoclast detachment, while at 0.1 μM, it only exerts partial inhibitory effects accompanied by the disappearance of the ruffled border^[2]. In Vivo:Minodronic acid (80 μg/kg; subcutaneous injection; once weekly; for 3 consecutive weeks) significantly inhibits the growth of bladder cancer bone metastases in BALB/c nu/nu mice without causing adverse effects^[1].
Minodronic acid (30-100 μM; transurethral administration; 5 days) inhibits the growth of orthotopic bladder cancer in SCID mice ^[1].
Minodronic acid (0.05-5 mg/kg; subcutaneous injection; single administration) accumulates in the calcified and ossified regions of rat bones, concentrates in osteoclast-containing bone tissue sites, and exhibits dose-dependent bone tissue localization characteristics^[2].