Ibudilast (AV-411). A new class therapeutic candidate for neuropathic pain and o

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Expert Opin Investig Drugs. 2007 Jul;16(7):935-50.

Ibudilast (AV-411). A new class therapeutic candidate for

neuropathic pain and opioid withdrawal syndromes.

Ledeboer A, Hutchinson MR, Watkins LR, KW.

Avigen, Inc., Department of Preclinical Development, Alameda, CA

94502, USA.

The treatment of neuropathic pain is a major unresolved medical

challenge. Present pharmacotherapies only have modest efficacy and

numerous side effects. The use of opioid analgesics is additionally

coupled with dependence and withdrawal syndromes. Ibudilast (AV-411)

is a non-selective phosphodiesterase inhibitor that is also known to

suppress glial cell activation. It has been used clinically for

other indications with a good safety profile. As glial cell

activation is considered to crucially contribute to neuropathic pain

as well as opioid dependence and withdrawal, the authors conceived

that ibudilast may be useful for treating these conditions.

Preclinical data indicate that ibudilast crosses the blood-brain

barrier, is well tolerated, is active on oral administration,

reduces glial activation and attenuates pain symptoms in diverse rat

models of neuropathic pain. In addition, it enhances acute morphine

analgesia and attenuates morphine tolerance and withdrawal. Thus

ibudilast may improve opioid efficacy and is a promising therapeutic

candidate for neuropathic pain, with a novel mechanism of action.