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Summary   Background   TAK ‐438 (vonoprazan) is a potassium‐competitive acid blocker that reversibly inhibits gastric H + , K + ‐ ATP ase.    Aim  To evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of  TAK ‐438 in healthy Japanese and non‐Japanese men.    Methods  In two Phase I, randomised, double‐blind, placebo‐controlled studies, healthy men (Japan  N  = 60;  UK   N  = 48) received  TAK ‐438 10–40 mg once daily at a fixed dose level for 7 consecutive days. Assessments included safety, tolerability, pharmacokinetics and pharmacodynamics (intragastric  pH ).    Results  Plasma concentration–time profiles of  TAK ‐438 at all dose levels showed rapid absorption (median  T  max  ≤2 h). Mean elimination half‐life was up to 9 h. Exposure was slightly greater than dose proportional, with no apparent time‐dependent inhibition of metabolism. There was no important difference between the two studies in  AUC  0‐tau  on Day 7.  TAK ‐438 caused dose‐dependent acid suppression. On Day 7, mean 24‐h intragastric  pH >4 holding time ratio ( HTR ) with 40 mg  TAK ‐438 was 100% (Japan) and 93.2% ( UK ), and mean night‐time  pH >4  HTR  was 100% (Japan) and 90.4% ( UK ).  TAK ‐438 was well tolerated. The frequency of adverse events was similar at all dose levels and there were no serious adverse events. There were no important increases in serum alanine transaminase activity. Serum gastrin and pepsinogen I and  II  concentrations increased with  TAK ‐438 dose.    Conclusions   TAK ‐438 in multiple rising oral dose levels of 10–40 mg once daily for 7 days was safe and well tolerated in healthy men and caused rapid, profound and sustained suppression of gastric acid secretion throughout each 24‐h dosing interval. Clinicaltrials.gov identifiers:  NCT 02123953 and  NCT 02141711.

alimentary pharmacology and therapeutics

Randomised clinical trial: safety, tolerability, pharmacokinetics and pharmacodynamics of repeated doses of  TAK ‐438 (vonoprazan), a novel potassium‐competitive acid blocker, in healthy male subjects