Cizolirtine. Laboratorios Dr Esteve.
Cizolirtine is a centrally-acting analgesic that is under development by Esteve for the potential treatment of pain [171179]. In March 2001, phase II and III trials in the US and Europe were ongoing [404223]. Its mechanism of action is based on the inhibition of substance P and calcitonin gene-related peptide release at the spinal cord level [404223] but this has not yet been fully confirmed. Cizolirtine does not produce gastrointestinal lesions or depress respiration [388894], however, it does exhibit antipyretic activity in animal models [260611], [388894]. The compound was disclosed in EP-00289380, published by Esteve in 1988. A method of resolving the racemic compound has also been claimed in WO-09902500.
Monck
N
N
Vemalis Research Ltd, Oakdene Court, 613 Reading Road, Winnersh, Wokingham, RG41 5UA, UK. n.monck@vemalis.com
D018712:Analgesics, Non-Narcotic / Q000009:adverse effects* / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D000818:Animals; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D006801:Humans; D010146:Pain / Q000188:drug therapy*; D011720:Pyrazoles / Q000009:adverse effects* / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D013329:Structure-Activity Relationship
D018712:Analgesics, Non-Narcotic; D011720:Pyrazoles; C075798:cizolirtine