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Evaluation of pharmacokinetic characteristics of a novel anti‐IBD drug, DA‐6034, in healthy volunteers
Author(s) -
Lim K. S.,
Chung J. Y.,
Kim J. R.,
Jung H. R.,
Cho J. Y.,
Yu K. S.,
Son M. W.,
Chung J. Y.,
Jang I. J.,
Shin S. G.
Publication year - 2005
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/j.clpt.2004.12.106
Subject(s) - medicine , pharmacokinetics , dosing , tolerability , cmax , adverse effect , placebo , pharmacology , drug , clinical trial , pathology , alternative medicine
Background IBDs are chronic, recurrent diseases which need long‐term treatment. We conducted a phase I clinical trial of DA‐6034, an extractor of wormwood, to evaluate the tolerability, safety, and PK of this compound. Methods A double‐blind, dose randomized, placebo‐controlled, dose‐rising study was conducted in 67 healthy volunteers. The volunteers were randomly allocated to single‐dose groups of 10mg, 20mg, 50mg, 100mg, and 200mg (8 per dose including 2 placebos) or multiple‐dose groups of 20mg, 50mg, and 100mg (twice‐daily dosing for 7 days; 9 per dose including 3 placebos). After dosing serial blood and urine samples were taken. Drug concentrations were determined by HPLC assay. Assessments of safety and tolerability were made. Results The Cmax of DA‐6034 was very low (2.52±1.47ng/mL in 200mg group). Four subjects taking active drugs of 10mg, 20mg, and 50mg group showed that plasma concentrations were below the LLQ at all time points. Urinary cumulative amount of excretion to 48 hour after dosing was 0.3%. No serious adverse effects were observed. Conclusions DA‐6034 was little absorbed in healthy volunteers, as expected from the preclinical data. The target organ is the GI tract, so the PK of DA‐6034 which was little absorbed to systemic circulation and was localized in the GI tract is expected to be advantageous for patients. However, it is possible that in patients the absorption pattern is altered by inflammation, so further evaluation of the PK along with efficacy of DA‐6034 in IBD patients is expected. Clinical Pharmacology & Therapeutics (2005) 77 , P57–P57; doi: 10.1016/j.clpt.2004.12.106