Othera Pharmaceuticals originally developed OT-730 (now known as QLT 091568) as an oculoselective beta-blocker for reducing the elevated intraocular pressure associated with glaucoma. OT-730 was involved in phase II clinical trial in patients with ocular hypertension or open-angle glaucoma. However, these studies were discontinued. At December 30, 2009, QLT Inc. acquired OT-730.

SIM-010603 (Tafetinib) is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM-010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Moreover, SIM-010603 inhibited endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis. SIM-010603 inhibited tumor growth in these xenograft tumor growth models. SIM010603 reduced tumor MVD in T241-VEGF-A tumor xenograft models and decreased positive signals of CD31, NG2 in MDA-MB-435, and LLC-SW-44 xenograft tumor models. SIM-010603 was in development by Simcere Pharmaceutical Group for the cancer treatment. It was in phase I clinical trials by Simcere, Jilin Boda Pharma and Nanjing Yoko Biological Pharma for the treatment of solid tumours, but this research was discontinued.

DA-6886 is an antagonist of the 5-HT4 receptor, discovered by the Korean Dong-A ST Research Institute. The drug binds with high activity and selectivity to human 5-HT4 receptor splice variants, with mean pKi of 7.1, 7.5 and 7.9 for the human 5-HT4a, 5-HT4b, and 5-HT4d, respectively. DA-886 induced relaxation of the rat esophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. In the normal ICR mice, oral administration of the drug at 0.4 and 2 mg/kg resulted in a marked stimulation of colonic transit. DA-6886 was investigated in phase I clinical trial for the treatment of Irritable Bowel Syndrome.