Results 161 to 170 of about 1,815 (184)

Tofogliflozin: First Global Approval

Drugs, 2014
Tofogliflozin (Apleway(®), Deberza(®) [Japan]), an orally active small molecule sodium-glucose co-transporter type 2 (SGLT2) inhibitor, has been developed by Chugai Pharmaceutical for the treatment of type 2 diabetes mellitus (T2DM), and a marketing authorization application was filed in Japan in 2013 by licensees Sanofi K.K. and Kowa.
Raewyn M, Poole, Jennifer E, Prossler
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Development of a Scalable Synthesis of Tofogliflozin

The Journal of Organic Chemistry, 2016
An efficient and scalable synthesis of an antidiabetic drug, tofogliflozin (1), which was identified as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor, is described. A key factor in the synthesis of 1 was the selection of the purpose-designed protecting group, which plays a strategic role in protection, chemoselective activation ...
Yoshihito, Ohtake, Takashi, Emura, Masahiro, Nishimoto, Koji, Takano, Keisuke, Yamamoto, Satoshi, Tsuchiya, Sang-Yong, Yeu, Yasushi, Kito, Nobuaki, Kimura, Sunao, Takeda, Masao, Tsukazaki, Masatoshi, Murakata, Tsutomu, Sato   +12 more
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A Scalable Synthesis of Tofogliflozin Hydrate

Organic Process Research & Development, 2016
A newly process for the synthesis of tofogliflozin hydrate, a sodium-glucose cotransporter type 2 (SGLT2) inhibitor, was described. Three improvements were achieved, including the development of a regioselective Friedel–Crafts reaction, a high-yield reduction, and a mild metal–halogen exchange. These improvements ultimately resulted in the isolation of
Xiu-Dong Yang, Zhao-Xi Pan, Da-Jun Li, Guan Wang, Min Liu, Rong-Gui Wu, Yan-Hua Wu, Yong-Chen Gao   +7 more
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Metabolism and mass balance of SGLT2 inhibitor tofogliflozin following oral administration to humans

Xenobiotica, 2013
1. Tofogliflozin is a novel and selective SGLT2 inhibitor increasing glucosuria by inhibition of glucose re-absorption in the kidney for the treatment of type 2 diabetes mellitus. 2. In this study, the metabolism and the mass balance of tofogliflozin was evaluated following administration of a single oral dose of 20 mg [(14)C]-tofogliflozin to six ...
Manfred, Zell, Christophe, Husser, Olaf, Kuhlmann, Dietmar, Schwab, Takahide, Uchimura, Tomonori, Kemei, Kosuke, Kawashima, Mizuki, Yamane, Axel, Pähler   +8 more
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Tofogliflozin: A highly selective SGLT2 inhibitor for the treatment of type 2 diabetes

Drugs of Today, 2014
Diabetes mellitus impacts a substantial number of people worldwide and despite numerous antidiabetic medications available, approximately half of the drugs do not attain their recommended target, glycated hemoglobin (HbA1c). Recently, the kidney and its role in glucose reabsorption through the sodium/glucose cotransporter 2 (SGLT2) has been the target ...
R F, Rosenwasser, J N, Rosenwasser, D, Sutton, R, Choksi, B, Epstein   +4 more
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A Novel Double-Tracer Technique to Characterize Absorption, Distribution, Metabolism and Excretion (ADME) of [14C]Tofogliflozin After Oral Administration and Concomitant Intravenous Microdose Administration of [13C]Tofogliflozin in Humans

Clinical Pharmacokinetics, 2013
Human mass balance studies and the assessment of absolute oral bioavailability (F) are usually assessed in separate studies. Intravenous microdose administration of an isotope tracer concomitant to an unlabeled oral dose is an emerging technique to assess F.
Dietmar, Schwab, Agnes, Portron, Zoe, Backholer, Berthold, Lausecker, Kosuke, Kawashima   +4 more
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Pharmacokinetics and Pharmacodynamics of Tofogliflozin (a Selective SGLT2 Inhibitor) in Healthy Male Subjects

Drug Research, 2017
Abstract Tofogliflozin is a selective oral inhibitor of sodium-glucose co-transporter 2 for treatment of type 2 diabetes mellitus. The pharmacokinetics, pharmacodynamics, and safety of tofogliflozin were investigated in healthy male subjects. Three studies were conducted: single-ascending dose study (10–640 mg) in 56 Japanese and 24 Caucasian subjects;
Nahoko, Kasahara-Ito, Hiroyuki, Fukase, Yoichiro, Ogama, Tomohisa, Saito, Yasuhiro, Ohba, Sumire, Shimada, Yasuki, Takano, Tomoko, Ichihara, Kimio, Terao, Noboru, Nakamichi, Yuji, Kumagai, Sachiya, Ikeda   +11 more
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Effect of Tofogliflozin on Systolic and Diastolic Cardiac Function in Type 2 Diabetic Patients

Cardiovascular Drugs and Therapy, 2019
Recent studies have shown that sodium glucose cotransporter 2 (SGLT2) inhibitors have a favorable effect on cardiovascular events in diabetic patients. However, the underlying mechanism associated with a favorable outcome has not been clearly identified.
Munemitsu Otagaki, Koichiro Matsumura, Hiromi Kin, Kenichi Fujii, Hiroki Shibutani, Hiroshi Matsumoto, Hiroki Takahashi, Haengnam Park, Yoshihiro Yamamoto, Tetsuro Sugiura, Ichiro Shiojima   +10 more
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Pharmacokinetic and pharmacodynamic drug evaluation of tofogliflozin for the treatment of type 2 diabetes

Expert Opinion on Drug Metabolism & Toxicology, 2016
Sodium-glucose co-transporter 2 (SGLT-2) inhibitors are a new class of drugs that are increasingly used for the management of type 2 diabetes mellitus (T2DM). Among these, tofogliflozin has recently received marketing approval in Japan. Areas covered: In this review, the authors summarize the pharmacokinetic and pharmacodynamic profile of tofogliflozin
Kalliopi, Pafili, Efstratios, Maltezos, Nikolaos, Papanas   +2 more
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Tofogliflozin

Reactions Weekly, 2021
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