GRC 27864 is a potent, selective, and orally bioavailable inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), a novel therapeutic target in pain management, which is upregulated under inflammatory conditions. A Phase 1 single ascending dose and a multiple ascending dose study have been completed in the UK with no safety concerns. It is currently in Phase 2 development. The most common AEs for patients receiving single doses were headaches and dizziness. For patients who received multiple doses the most common AEs were nausea, diarrhoea and abdominal pain, none of which were dose limiting.
Gynecomastia is a common adverse effect of bicalutamide (Casodex) therapy that may prompt some men to discontinue prostate cancer treatment. Tamoxifen has been recommended as a preventive agent for gynecomastia in these patients. A double-blind study of 282 men randomized to receive 20 mg of tamoxifen once per day with bicalutamide or bicalutamide alone found that after six months, gynecomastia and breast pain were significantly reduced in men who received tamoxifen ( versus percent in the control group). 41 An Italian randomized controlled trial of 80 participants also found that 20 mg of tamoxifen once per week is as effective as 20 mg once per day. 42