VTP-27999 is an alkyl amine renin inhibitor. This compound demonstrated excellent selectivity over related and unrelated off-targets, >15% oral bioavailability in three species, oral efficacy in a double transgenic rat model of hypertension, and good exposure in humans. Vitae Pharmaceuticals was developing VTP 27999 for the treatment of chronic kidney disease. VTP 27999 was in phase I clinical development in the US. However, the product is no more on the company pipeline and it appears that the development has been discontinued.

TAS-108 (also known as SR-16234) is a selective estrogen receptor modulator (SERM) and has been reported to have estrogen receptor (ER) α antagonistic activity and a strong affinity with a weak partial agonistic activity to ERβ receptor. It is known that ERs play a central role in the diverse actions of estrogen. TAS-108 was studied in phase II clinical trials to treat recurrent or recurrent inoperable breast cancer. In addition, TAS-108 participated in Japan in a phase II clinical trial in Endometriosis patients. The phase III studies are being planned with the drug.

MGB-BP 3 is an antibacterial agent being developed by MGB Biopharma. This drug is now in phase II clinical trial to assess the safety, tolerability, and efficacy of incremental doses in patients with Clostridium difficile-associated diarrhea. In addition, this drug is studied for the treatment of Gram-positive infections; and skin and soft tissue infections.

FLOTEGATIDE is a cyclic tripeptide with arginine-glycine-aspartic acid (R-G-D) motif. Its 18F radiolabelled form is a positron emission tomography (PET) tracer targeting integrin alpha-V/beta-3.

PZ-128 (also known as P1pal7 ) is a cell-penetrating pepducin inhibitor of PAR1 that targets the receptor-G-protein interface on the inside surface of platelets. In preclinical studies, PZ-128 suppresses PAR1 aggregation and arterial thrombosis in guinea pigs and baboons and strongly synergized with oral clopidogrel. PZ-128 shows potent anti-metastatic and anti-angiogenic activity in Breast, Ovarian, and Lung Cancer preclinical studies. In clinical trials, PZ-128 shows a promising antiplatelet activity that provides rapid, specific, dose-dependent, and reversible inhibition of platelet protease-activated receptor-1 through a novel intracellular mechanism.

GSK-2256294 is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH. GSK-2256294A also displays potent cellular inhibition (IC50 = 0.66 nM) of sEH in an assay developed using a cell line transfected with the human sEH enzyme. GSK-2256294 was well-tolerated and demonstrated sustained inhibition of sEH enzyme activity. These data support further investigation in patients with endothelial dysfunction or abnormal tissue repair, such as diabetes, wound healing or COPD. GSK-2256294 is in phase I clinical trials for the treatment of COPD.