This week in therapeutics




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IL-6; IL-6 signal transducer (IL-6ST; gp130; CD130); JAK kinase (JAK); signal transducer and activator of transcription 3 (STAT3)

In vitro studies suggest two marketed drugs could inform the design of inhibitors that block the IL-6-CD130 interaction and help treat cancer. Fragment-based drug design and virtual screening identified raloxifene and bazedoxifene as potential inhibitors of the IL-6-CD130 interaction that activates JAK and STAT3 signaling. In a CD130+ human pancreatic cancer cell line, both drugs reduced viability at micromolar IC50 values. In an estrogen receptor-negative human breast cancer cell line, the drugs reduced viability at micromolar IC50 values. Ongoing work includes optimizing the two drugs for potency against the IL-6-CD130 interaction.
Eli Lilly and Co. and Takeda Pharmaceutical Co. Ltd. market Evista raloxifene, a selective estrogen receptor modulator (SERM), to treat osteoporosis and breast cancer.
Ligand Pharmaceuticals Inc. and Pfizer Inc. market the SERM Conbriza bazedoxifene to treat osteoporosis.

SciBX 7(6); doi:10.1038/scibx.2014.167
Published online Feb. 13, 2014

Unpatented; unlicensed; available for partnering

Li, H. et al. J. Med. Chem.;
published online Jan. 23, 2014;
Contact: Chenglong Li, The Ohio State University, Columbus, Ohio