An open-label, randomized, two-period crossover study to compare the pharmacokinetic and safety profile of single dose of TAK-070 (50 mg) under fed and fasting condition in healthy volunteer - An open-label, randomized, study to compare the pharmacokinetic and safety profile of single dose of TAK-070 under fed and fasting condition

Start Date15 Aug 2015

Sponsor / Collaborator-

JPRN-UMIN000010218 / CompletedPhase 1IIT

A Randomized, Double-Blind, Placebo-Controlled, Sequential, Ascending Single and Multiple Dose, Safety, Tolerability, and Pharmacokinetic Study of TAK-070 in Healthy Elderly Subjects - A Randomized, Double-Blind, Placebo-Controlled, Sequential, Ascending Single and Multiple Dose, Safety, Tolerability, and Pharmacokinetic Study of TAK-070 in Healthy Elderly Subjects

Start Date11 Mar 2013

Sponsor / Collaborator-

100 Clinical Results associated with TAK-070

100 Translational Medicine associated with TAK-070

100 Patents (Medical) associated with TAK-070

Literatures (Medical) associated with TAK-070

01 Nov 2010·Brain ResearchQ4 · MEDICINE

Ameliorative effects of a non-competitive BACE1 inhibitor TAK-070 on Aβ peptide levels and impaired learning behavior in aged rats

Q4 · MEDICINE

Article

Author: Hiroaki Fukumoto ; Jun Terauchi ; Hideki Takahashi ; Ryouta Maeda ; Masaomi Miyamoto ; Kaneyoshi Kato

We examined the effects of TAK-070, a novel non-competitive β-secretase (BACE1) inhibitor, on the levels of Aβ peptides and behavioral deficits in rats. TAK-070 reduced soluble Aβ40 and Aβ42 levels of the cerebral cortex in a time- and dose-dependent manner in young rats. We found that the insoluble Aβ42 content increased significantly with aging from 22 months old without changing Aβ40 content. TAK-070 normalized the Aβ42 levels to those in young rats when they were fed chow containing TAK-070 starting at 19 months old for 6.5 months. Repeated administration of TAK-070 to aged rats for 2 weeks ameliorated the impaired spatial learning in the Morris water maze task and reduced the levels of soluble and insoluble Aβ peptides at doses of 0.3-1mg/kg, (p.o.). Interestingly, TAK-070 significantly recovered the reduced brain synaptophysin levels in aged rats to those in young rats. Our findings support the idea that partial inhibition of BACE1 by TAK-070 exerts symptomatic as well as disease-modifying effects for the treatment of Alzheimer's disease.

18 Aug 2010·The Journal of NeuroscienceQ1 · MEDICINE

A Noncompetitive BACE1 Inhibitor TAK-070 Ameliorates Aβ Pathology and Behavioral Deficits in a Mouse Model of Alzheimer's Disease

Q1 · MEDICINE

Article

Author: Hirode, Mitsuhiro ; Iwatsubo, Takeshi ; Miyamoto, Masaomi ; Tarui, Naoki ; Maeda, Ryouta ; Sagayama, Masumi ; Sakura, Yasufumi ; Kato, Kaneyoshi ; Kawamoto, Makiko ; Fukumoto, Hiroaki ; Hirai, Kazuko ; Matsui, Junji ; Terauchi, Jun ; Takahashi, Hideki ; Kakihana, Mitsuru ; Tomita, Taisuke

We discovered a nonpeptidic compound, TAK-070, that inhibited BACE1, a rate-limiting protease for the generation of Aβ peptides that are considered causative for Alzheimer's disease (AD), in a noncompetitive manner. TAK-070 bound to full-length BACE1, but not to truncated BACE1 lacking the transmembrane domain. Short-term oral administration of TAK-070 decreased the brain levels of soluble Aβ, increased that of neurotrophic sAPPα by ∼20%, and normalized the behavioral impairments in cognitive tests in Tg2576 mice, an APP transgenic mouse model of AD. Six-month chronic treatment decreased cerebral Aβ deposition by ∼60%, preserving the pharmacological efficacy on soluble Aβ and sAPPα levels. These results support the feasibility of BACE1 inhibition with a noncompetitive inhibitor as disease-modifying as well as symptomatic therapy for AD.

100 Deals associated with TAK-070

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 1	-	Takeda Pharmaceutical Co., Ltd.	-
Alzheimer Disease	Phase 1	JP	University of Tokyo	-

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