Gründer Gerhard
RWTH Aachen University, Department of Psychiatry and Psychotherapy, and JARA - Translational Brain Medicine, Pauwelsstrasse 30, Aachen, Germany.
Curr Opin Investig Drugs. 2010 Jul;11(7):823-32.
Cariprazine (RGH-188), which is being codeveloped by Gedeon Richter Ltd, Forest Laboratories Inc and Mitsubishi Tanabe Pharma Corp, is a novel putative antipsychotic drug that exerts partial agonism at dopamine D2/D3 receptors, with preferential binding to D3 receptors, and partial agonism at serotonin 5-HT1A receptors. Its activity at D2/D3 receptors may be lower than that of the prototype partial agonist aripiprazole. The antipsychotic activity of cariprazine was demonstrated in animal models, and data also suggest that the propensity for extrapyramidal side effects is low and that the drug may have procognitive properties. Cariprazine is rapidly absorbed, with high oral bioavailability and a long plasma elimination t1/2. Cariprazine is in phase III clinical trials in patients with schizophrenia and in patients with bipolar disorder. Data from phase II trials in patients with schizophrenia and bipolar mania indicate that the drug has antipsychotic and antimanic properties that are superior to placebo. With its unique receptor affinity profile, cariprazine may represent a potential enrichment of the therapeutic armamentarium for schizophrenia and affective disorders. Its activity against the cognitive deficits associated with schizophrenia has to be carefully investigated.
卡立哌嗪（RGH - 188）由吉德昂·里奇特有限公司、森林实验室公司和三菱田边制药公司联合开发，是一种新型的假定抗精神病药物，对多巴胺D2/D3受体具有部分激动作用，对D3受体具有优先结合能力，对5-羟色胺5-HT1A受体具有部分激动作用。其对D2/D3受体的活性可能低于原型部分激动剂阿立哌唑。卡立哌嗪的抗精神病活性在动物模型中得到证实，数据还表明其锥体外系副作用的倾向较低，且该药物可能具有促认知特性。卡立哌嗪吸收迅速，口服生物利用度高，血浆消除半衰期长。卡立哌嗪正在进行针对精神分裂症患者和双相情感障碍患者的III期临床试验。精神分裂症和双相躁狂症患者的II期试验数据表明，该药物具有优于安慰剂的抗精神病和抗躁狂特性。凭借其独特的受体亲和力特征，卡立哌嗪可能代表了精神分裂症和情感障碍治疗药物库的潜在扩充。必须仔细研究其针对与精神分裂症相关的认知缺陷的活性。
