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TAK‐648 is a PDE4 inhibitor with demonstrated preclinical antidiabetic properties. Our objective was to develop a translational pharmacokinetic/pharmacodynamic (PK/PD) model for human type 2 diabetes (T2D) dose prediction using HbA1c results from a db/db mouse study. Estimated parameters in combination with tPDE4i values calculated for the clinical roflumilast dose of 500 μg were used to translate preclinical effects of TAK‐648 to required exposure in humans. A first‐in‐human study with single TAK‐648 doses of 0.05–0.85 mg in healthy volunteers yielded mean maximum TAK‐648 concentrations (Cmax) and area under the curve (AUC) values from 0.62–11.9 μg/L and 4.58–93.8 μg*h/L, respectively. Based on the performed pharmacokinetic/pharmacodynamic analysis and clinical PK results, clinical efficacy would be expected at a daily dose of 0.1 mg, which is well within the investigated clinical dose range. This result significantly enhanced the confidence in TAK‐648 for type 2 diabetes treatment and underlines the necessity of translational approaches in early preclinical phases.

100 Deals associated with TAK-648

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R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Nonalcoholic Steatohepatitis	Phase 1	-	Takeda Pharmaceutical Co., Ltd.	-
Nonalcoholic Steatohepatitis	Phase 1	-	ARTham Therapeutics, Inc.Startup	-
Diabetes Mellitus, Type 2	Discovery	US	Takeda Pharmaceutical Co., Ltd.	01 Apr 2015
Diabetic Nephropathies	Discovery	US	Takeda Pharmaceutical Co., Ltd.	-

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Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02430870 (CTgov)	Phase 1	Diabetes Mellitus, Type 2	48	TAK-648 (Part 1 Cohort 1: TAK-648 0.35 mg)	mivzwlwtah(eofwxdpnru) = igghuralqk sjzjqtacwj (txnvtzjkog, qprzzspprk - wqiopcxxiv) View more	-	31 Aug 2016
				TAK-648 (Part 1 Cohort 2: TAK-648 0.80 mg)	mivzwlwtah(eofwxdpnru) = rfjgodfyqw sjzjqtacwj (txnvtzjkog, egyoicuodw - dxgdmhvbvh) View more
NCT02684396 (CTgov)	Phase 1	-	39	TAK-648 (Cohort 1: TAK-648 0.05 mg)	piowbsaogw(xrwitomuvh) = npvempeqef ybwdbpvcnw (lglyldzwyk, nukbabwwss - oigaorsctr) View more	-	13 Jul 2016
				TAK-648 (Cohort 2: TAK-648 0.15 mg)	piowbsaogw(xrwitomuvh) = nnyzvpebmi ybwdbpvcnw (lglyldzwyk, xwweqnfmds - xxetmrpqap) View more