PF-06840003 is a highly selective orally bioavailable Indoleamine 2,3-dioxygenase-1 (IDO-1) inhibitor with a potent antineoplastic activity. PF-06840003 reversed IDO-1-induced T-cell anergy in vitro. In vivo, PF-06840003 reduced intratumoral kynurenine levels in mice by >80% and inhibited tumor growth in multiple preclinical syngeneic models in mice, in combination with immune checkpoint inhibitors. A Phase 1 study of PF-06840003 in patients with Malignant Gliomas is ongoing.

TrioxBio's API, S-ethylisothiouronium diethylphosphate, MTR-104 (MTR- 105), is a nitric oxide synthase (NOS) inhibitor which blocks the production of nitric oxide, preventing the dilation of blood vessels and the other detrimental effects caused by excessive NOS activity. MTR-105, a fast-acting synthetic NOS inhibitor with rapid onset of action when administered parenterally, has been effective in alleviating hypotension experimentally and in several observational studies while reducing NO production. MTR-105 is registered and approved for clinical use in the Republic of Moldova where data have been collected from 434 patients exposed to the drug in pre- and postapproval clinical investigations.

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.