[Introduction of novel anti-emetic agent, indisetron hydrochloride, developed recently in Japan].
Recently, an anti-emetic agent, indisetron hydrochloride was developed in Japan. In the pre-clinical studies, it showed almost similar affinity to 5-HT3 receptor as those developed before. Indisetron reduced 2-methyl-5-serotonin (HT)-induced bradycardia. The 5-HT3 antagonistic activity was over 20 times more than that of granisetron or ondansetron, indicating the excellent anti-emetic activity against anticancer drug induced vomiting. After phase I and II clinical studies, phase III studies consisting of a comparative double-blind randomized clinical trial (comparing with ondansetron) and open clinical trials, the effectiveness and safety profiles of this indisetron were clearly shown. From these studies, it was considered that indisetron seemed to be equally or more effective against chemotherapy-induced nausea and vomiting compared with existed 5-HT3 receptor antagonists.
Tsukagoshi
Shigeru
S
D000818:Animals; D000932:Antiemetics / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D001952:Bridged-Ring Compounds / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D002945:Cisplatin / Q000009:adverse effects; D004311:Double-Blind Method; D006168:Guinea Pigs; D006801:Humans; D009325:Nausea / Q000517:prevention & control*; D009369:Neoplasms / Q000188:drug therapy; D011720:Pyrazoles / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D016032:Randomized Controlled Trials as Topic; D051381:Rats; D058831:Serotonin 5-HT3 Receptor Antagonists; D014840:Vomiting, Anticipatory / Q000517:prevention & control*
D000932:Antiemetics; D001952:Bridged-Ring Compounds; D011720:Pyrazoles; D058831:Serotonin 5-HT3 Receptor Antagonists; C500220:indisetron hydrochloride; D002945:Cisplatin