Rie Tsubota

Mitsubishi Tanabe Pharma Corporation

Author Statistics

Papers

Citation

H-Index

i-10 index

Research Trends

Author Order

Document Type

Co-Authors

Jyunko Okabe

Mitsubishi Chemical (Japan)

Yousuke Ikeda

National Hospital Organization Hokkaido Medical Center

Koki Kojima

Mitsubishi Tanabe Pharma Corporation

Akiko Idei

RIKEN Center for Sustainable Resource Science

Taku Iguchi

Mitsubishi Tanabe Pharma Corporation

Takehisa Kawata

Kyowa Kirin (Japan)

Ayako Kannami

Mitsubishi Chemical (Japan)

Yutaka Hisada

Mitsubishi Chemical (Japan)

Rikiya Ohashi

Hokkaido Pharmaceutical University

Hajime Fukuda

The University of Tokyo

Cooperative Institutions

Mitsubishi Tanabe Pharma Corporation

Mitsubishi Chemical (Japan)

Mitsubishi Group (Japan)

Tohoku University

Kyoto University

Wakayama Prefectural Tanabe High School

Tanabe Research Laboratories

Kyowa Kirin (Japan)

The University of Tokyo

Teikoku Seiyaku (Japan)

Author Statistics

Papers

Citation

H-Index

i-10 index

Research Field

Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism

Bioorganic & Medicinal Chemistry Letters (2018)

Hiroshi Miyazaki Yousuke Ikeda Osamu Sakurai Tsutomu Miyake Rie Tsubota

The calcium-sensing receptor (CaSR) plays an important role in sensing extracellular calcium ions and regulating parathyroid hormone secretion by parathyroid gland cells, and the receptor is a suitable target for the treatment of hyperparathyroidism. Cinacalcet hydrochloride is a representative CaSR agonist which widely used for the hyperparathyroidism. However, it has several issues to clinical use, such as nausea/vomiting and strong inhibition of CYP2D6. We tried to improve these issues of cinacalcet for a new pharmaceutical agent as a preferable CaSR agonist. Optimization from cinacalcet resulted in the identification of pyrrolidine compounds and successfully led to the discovery of evocalcet as an oral allosteric CaSR agonist. Evocalcet, which exhibited highly favorable profiles such as CaSR agonistic activity and good DMPK profiles, will provide a novel therapeutic option for secondary hyperparathyroidism.

Cinacalcet

Calcimimetic

Inverse agonist

10.1016/j.bmcl.2018.04.055

Cite

Citations (36)

CCDC 1817497: Experimental Crystal Structure Determination

The Cambridge Structural Database (2018)

Hiroshi Miyazaki Yousuke Ikeda Osamu Sakurai Tsutomu Miyake Rie Tsubota

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

10.5517/ccdc.csd.cc1z07y5

Cite

Citations (0)