Norastemizole Sepracor.
Sepracor and Janssen are developing the histamine H1 antagonist, norastemizole (an active metabolite of Johnson & Johnson's Hismanal), for the potential, non-sedating treatment of allergy. Sepracor expects to file an NDA with the FDA by the fourth quarter of 2000 [337315,358429]. As of September 1999, Sepracor was conducting two large-scale phase III seasonal allergic rhinitis studies [340260]. Sepracor expects norastemizole to be the most potent non-sedating histamine, with equal or more rapid onset of action than other therapies [229516]. Norastemizole is 13- to 16-fold more potent as an H1 antagonist than astemizole and 20- to 40-fold more potent in inhibiting histamine-induced bronchoconstriction. Following a single dose of norastemizole (25 mg p.o.), there is significant attenuation of histamine-induced wheal and flare responses within 30 min. The drug's major advantage is its lack of cardiotoxicity or interactions with other drugs that increase the risk of developing serious arrhythmias [301469]. In July 2000, Morgan Stanley Dean Witter predicted filing for FDA approval for allergic rhinitis during the first half of 2001, and a partnership announcement around the time of this NDA filing. The analysts also forecast European sales of $8.3 million in 2002, rising to $16.7 m by 2005 [384868].
University of Toledo, College of Pharmacy, 2801 W Bancroft Street, Toledo, OH 43606, USA. kbachma@utnet.utoledo.edu
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D000818:Animals; D018926:Anti-Allergic Agents / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D001562:Benzimidazoles / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D002986:Clinical Trials as Topic; D000075202:Contraindications; D015507:Drugs, Investigational / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D006801:Humans; D010880:Piperidines / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D006255:Rhinitis, Allergic, Seasonal / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D018926:Anti-Allergic Agents; D001562:Benzimidazoles; D015507:Drugs, Investigational; D010880:Piperidines; C106448:tecastemizole