Each year, over a million women worldwide are diagnosed with breast cancer, accounting for 25% of all female cancers. About 1 in 8 women are predicted to develop this disease during her lifetime. Over the last two decades, single and combination chemotherapy, based on results from clinical trials, has led to a considerable reduction in morbidity and increased survival of breast cancer patients. However, more recently, progress has seemingly been stalled. An effort to identify biomarkers that would predict the response to a particular therapy ensued and this approach has been well validated with respect to several tumor-related biomarkers. The next step in the advancement of breast cancer therapy was the search for new molecular targets followed by the design of appropriate modalities directed against these targets. One of the more promising of these new targets that has yet to be fully exploited is the Prolactin Receptor (PRLR).
The disclosed invention are novel small molecule inhibitors of PRLR formulated as pharmaceutical compositions and administered as both injectable solutions and oral dosing forms for the treatment of breast cancer, prostate cancer and for control of nociceptive pain.