GPR40 agonists for the treatment of type 2 diabetes: life after 'TAKing' a hit.
Montréal, Canada. In Diabetes Obes Metab, Jul 2015
This idea has been validated in both preclinical and clinical studies, in which activation of GPR40 was shown to improve glycaemic control by stimulating glucose-dependent insulin secretion; however, the recent termination of phase III clinical trials using the GPR40 agonist TAK-875 (fasiglifam) has raised important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of this receptor's basic biology.
[New therapies in metastatic castration resistant prostate cancer].
Villejuif, France. In Bull Cancer, Jun 2015
Several other treatments are on trial targeting different pathways: androgene pathway (TAK-007, ARN-509, ODM-201, TOK-001), immune system (sipuleucel, ipilimumab, PROSTVAC-V/F, tasquinimod), but also tumor cell (PARP inhibitor, cabozantinib).
Endothelin receptors and their antagonists.
Cambridge, United Kingdom. In Semin Nephrol, Mar 2015
The role of the two receptors has been delineated using highly selective ET(A) (BQ123, TAK-044) and ET(B) (BQ788) peptide antagonists.
Molecular pathways: novel approaches for improved therapeutic targeting of Hedgehog signaling in cancer stem cells.
Jacksonville, United States. In Clin Cancer Res, Mar 2015
However, to date, Hh inhibitors, specifically those targeting Smoothened [such as vismodegib, BMS-833923, saridegib (IPI-926), sonidegib/erismodegib (LDE225), PF-04449913, LY2940680, LEQ 506, and TAK-441], have demonstrated good efficacy as monotherapy in patients with basal cell carcinoma and medulloblastoma, but have shown limited activity in other tumor types.