Otsuka Pharmaceutical Co., Ltd.

Pharmaceuticals
April 21, 2016

Otsuka receives two commendations by the Japanese Government for the development of an anti-tuberculosis agent and an aquaretic/ADPKD treatment

Otsuka Pharmaceutical Co., Ltd. is pleased to announce that the company has been awarded two commendations for Science and Technology by the Minister of Education, Culture, Sports, Science, and Technology. These prizes for Science and Technology, in the Development Category, were for the research and development of delamanid, an effective treatment for multi-drug resistant tuberculosis, and for the development of tolvaptan, an antagonist of the vasopressin V2 receptor. The commendations were presented on April 20, 2016, in a ceremony held in the Ministry of Education, Culture, Sports, Science, and Technology.

About development of delamanid
Prize recipients:

Makoto Matsumoto, Pharmaceutical Business Division, senior director
Hiroyuki Hashizume, Pharmaceutical Marketing Headquarters, Product Planning And Management Group, product management manager
Hirofumi Sasaki, Medicinal Chemistry Research Laboratories, associate head and project OPC
Hidetsugu Tsubouchi, Compliance & Ethics Department, manager
Masanori Kawasaki, TB Projects, associate director

About one-third of the world's population is thought to be infected with Mycobacterium tuberculosis, and 9.6 million people each year develop tuberculosis (TB). Of these cases, 480,000 patients develop multidrug-resistant tuberculosis (MDR-TB), of which 22% develop extensively drug-resistant tuberculosis (XDR-TB), and 35% will die as a result of the disease. There have been no new anti-TB drugs developed since the introduction of rifampicin over forty years ago. Therefore, there has been an increasing need for new therapeutic agents to treat TB, especially the drug-resistant strains. In the development of the drug, Otsuka Pharmaceutical modified a structure unrelated to existing agents, nitro-imadazooxazole, which had a strong antibacterial potency to Mycobacterium tuberculosis. In preliminary tests in MDR-TB patients, the sputum samples for resistant bacteria became negative sooner than existing treatments and patient mortality was significantly reduced. As a result of favorable trials, the drug was approved in Japan, Europe, and Korea in 2014.
The commendation was awarded to delamanid for its contribution to the medical care of TB, by addressing the pressing need for new effective treatments to the increasing occurrence of MDR-TB.

About development of tolvaptan
Prize recipients:

Yoshitaka Yamamura, Pharmaceutical Business Division, senior director
Hidenori Ogawa, Medicinal Chemistry Research Laboratories
Hiroyuki Fujiki, New Drug Research Division, Biology and Translational Research Unit, senior research scientist
Youichi Yabuuchi, Otsuka Pharmaceutical Factory, Inc., corporate adviser

Sodium-excretion type diuretics have a range of applications, including treatment of fluid retention in heart failure and liver cirrhosis, however, due to undesirable effects in serum electrolyte concentrations and renal function, a diuretic with a different mode of action was sought by physicians. Otsuka Pharmaceutical developed a novel agent that acts as selective antagonist of the V2 receptor and unlike other diuretics, only leads to the excretion of water and not electrolytes. In addition, there was the long-sought-for treatment for the hereditary disease Autosomal Dominant Polycystic Kidney Disease (ADPKD). In this disease, large cysts form in the kidney, impairing kidney function and resulting in development of end-stage renal failure in over half patients by age 70. It was also discovered that this vasopressin V2 receptor antagonist may have an application in ADPKD by hindering the proliferation and enlargement of these cysts. Otsuka subsequently played a pivotal role in the clinical development of tolvaptan for ADPKD, and it is presently the only treatment option known to delay the long-term progression of ADPKD.