BI 44370 was developed as a calcitonin gene-related peptide receptor antagonist for the treatment of acute migraine attacks. In spite of the positive results from the phase II clinical trials, the BI-44370 study has been discontinued.

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.

H3B-6527 is a highly selective covalent FGFR4 inhibitor with at least 250-fold selectivity over FGFR1-3. H3B-6527 inhibits FGFR4 signaling, proliferation, and leads to apoptosis in Hepatocellular carcinoma (HCC) cell line. Treatment on Hep3B cells leads to robust activation of caspase-3/7, an apoptotic marker, in a concentration-dependent manner, indicating FGFR4 inhibition by H3B-6527 leads to cell death in HCC cell lines. In the Hep3B human HCC xenograft mouse model, H3B-6527 shows dose-proportional plasma exposures and greater than dose-proportional tumor exposures within the dose range evaluated (30, 100, and 300 mg/kg). Oral treatment of H3B-6527, twice daily, inhibits xenograft growth in a dose-dependent manner in nude mice, with the 300 or 100 mg/kg twice daily, significantly inhibiting tumor growth in both Hep3B subcutaneous and orthotopic xenograft model and causing tumor regressions in the subcutaneous xenograft model.

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.