RG7388

RG7388 is a non-imidazoline, selective MDM2 inhibitor that blocks the binding of MDM2 to p53 (IC₅₀ = 30 nM).¹ By inhibiting MDM2, RG7388 activates the p53 pathway in SJSA1 osteosarcoma cells and inhibits the growth of xenografts in nude mice.^1,2 RG7388 is orally available and prolonged daily administration results in loss of MDM2 and p21 protein, growth inhibition, and apoptosis in SJSA1 xenograft tumors.² Like other MDM2 inhibitors, RG7388 competitively inhibits multi-drug resistance protein 1 (MRP1) and reverse MRP1-mediated multidrug resistance in cancer cells in a p53-independent manner.³

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1. Ding, Q., Zhang, Z., Liu, J.J., et al. Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J. Med. Chem. 56(14), 5979-5983 (2013).

2. Higgins, B., Glenn, K., Walz, A., et al. Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach. Clin. Cancer Res. 20(14), 3742-3752 (2014).

3. Chen, L., Zhao, Y., Halliday, G.C., et al. Structurally diverse MDM2-p53 antagonists act as modulators of MDR-1 function in neuroblastoma. Br. J. Cancer 111(4), 716-725 (2014).