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Type: Journal article
Title: Ibudilast in healthy volunteers: Safety, tolerability and pharmacokinetics with single and multiple doses
Author: Rolan, P.
Gibbons, J.
He, L.
Chang, E.
Jones, D.
Gross, M.
Davidson, J.
Sanftner, L.
Johnson, K.
Citation: British Journal of Clinical Pharmacology, 2008; 66(6):792-801
Publisher: Blackwell Publishing Ltd
Issue Date: 2008
ISSN: 0306-5251
Statement of
Paul Rolan, Jacqueline A. Gibbons, Lin He, Eppie Chang, Drew Jones, Matthew I. Gross, Jennifer Bahr Davidson, Laura M. Sanftner & Kirk W. Johnson
Abstract: <h4>Aims</h4>To investigate the safety, tolerability and pharmacokinetics (PK) of ibudilast after a single-dose and a multiple-dose regimen.<h4>Methods</h4>Healthy adult male (n = 9) and female (n = 9) volunteers were evaluated over a 17-day stay in a Phase 1 unit. Subjects were randomized 1 : 3 to either oral placebo or ibudilast at 30-mg single administration followed by 14 days of 30 mg b.i.d. Complete safety analyses were performed and, for PK, plasma and urine samples were analysed for ibudilast and its major metabolite.<h4>Results</h4>Ibudilast was generally well tolerated. No serious adverse events occurred. Treatment-related adverse events included hyperhidrosis, headache and nausea. Two subjects discontinued after a few days at 30 mg b.i.d. because of vomiting. Although samples sizes were too small to rule out a sex difference, PK were similar in men and women. The mean half-life for ibudilast was 19 h and median T(max) was 4-6 h. Mean (SD) steady-state plasma C(max) and AUC(0-24) were 60 (25) ng ml(-1) and 1004 (303) ng h ml(-1), respectively. Plasma levels of 6,7- dihydrodiol-ibudilast were approximately 30% of the parent.<h4>Conclusions</h4>Ibudilast is generally well tolerated in healthy adults when given as a single oral dose of 30 mg followed by 30 mg b.i.d. (60 mg day(-1)) for 14 days. Plasma PK reached steady state within 2 days of starting the b.i.d. regimen. Exposure to ibudilast was achieved of a magnitude comparable to that associated with efficacy in rat chronic pain models.
Keywords: human volunteers; ibudilast; pharmacokinetics; Phase 1; safety; tolerability
RMID: 0020083746
DOI: 10.1111/j.1365-2125.2008.03270.x
Appears in Collections:Pharmacology publications

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