Pravadoline is the anti-nociceptive agent, which has analgesic efficacy against postoperative pain in humans. Pravadoline inhibits the enzyme cyclooxygenase, but in contrast to cyclooxygenase-inhibiting NSAIDs does not produce gastrointestinal irritation. Pravadoline inhibited the synthesis of prostaglandins in mouse brain both in vitro and ex vivo. Pravadoline demonstrated only weak anti-inflammatory activity relative to its anti-nociceptive potency. Single doses of pravadoline were safe and effective in humans, without serious adverse events. Single oral administration of pravadoline maleate induced acute tubular necrosis in male and female beagle dogs.