Indantadol is an oral and nonselective
monoamine oxidase inhibitor and
NMDA antagonist that is being developed by Vernalis plc, under license from Chiesi Farmaceutici SpA, for the potential treatment of
neuropathic pain. In preclinical studies,
indantadol exhibited
neuroprotective effects after kainite-induced
seizures, and displayed
anticonvulsant and antihyperalgesic activity.
Indantadol also caused a dose-dependent decrease in exploratory motility. In a human heat-
capsaicin-induced
pain model,
indantadol at a dose of 500 mg effectively reduced the area of secondary
hyperalgesia to 67%.
Indantadol undergoes extensive liver metabolism, withthe formation of two major metabolites - CHF-3567 and
2-aminoindane. The
drug is excreted in urine partially as the parent compound, but mostly as CHF-3567. The tolerability profile of
indantadol at single doses up to 600 mg and twice-daily doses up to 400 mg in clinical trials was significantly more favorable than for other
NMDA antagonists. Most side effects have been observed to be mild, and include
dizziness and
asthenia.
Indantadol is currently in phase II clinical trials in patients with diabetic peripheral
neuropathic pain. Given the results available to date,
indantadol may have a role in the treatment of
neuropathic pain if the favorable pharmacokinetic profile and efficacy of the
drug are maintained in more extensive clinical trials.