2009.07.06 RQ-00000004、RQ-00000010が"Thomson Pharma"のIDdb Meeting Reportで紹介されました
IDdb Meeting Reportで紹介されました
Digestive Disease Week 2009で発表を行ったラクオリア創薬の2つのプログラム（RQ-00000004、RQ-00000010）が、トムソンロイター社が提供する"Thomson Pharma"にて紹介されました。（以下、IDdb Meeting Report 2009, May 30 - June 4より転載）
- In vivo results for RQ-00000004
- Masaomi Taijimi (RaQualia) presented data from a preclinical study characterizing the pharmacology of the acid pump antagonist (APA) RQ-00000004 and comparing it revaprazan, which is currently on the market. RQ-00000004 and revaprazan had respective IC50 values of 0.47 and 0.69 microM for porcine H+/K+ ATPase. The compound demonstrated no species differences for porcine, canine and human gastric H+/K+-ATPase. In in vitro inhibition assays RQ-00000004 was more potent than revaprazan. The compound dose-dependently inhibited gastric acid secretion in Heidenhain pouch dogs with a long duration of action. The dogs were treated with oral doses of the compound following histamine-induced gastric secretion. Complete inhibition of secretion was observed at 1 mg/kg. Oral administration of revaprazan (1 and 3 mg/kg) also inhibited secretion, although complete secretion was not observed even at 3 mg/kg. RQ-00000004 was effective over 20 h with maximal efficacy observed within the first few hours of single dosing, indicating its immediate acting effect.
- Preclinical findings revealed for RQ-00000010
- Preclinical findings revealed for RQ-00000010 Toshinori Yamamoto of RaQualia Pharma, spun-out from Pfizer, displayed new findings for RQ-00000010, a 5-HT 4 partial agonist being investigated for the potential treatment of GERD. Dr Yamamoto believes the compound's low side-effect profile makes it a promising candidate to enter clinical development. In a dog clonidine-induced gastroparesis model, gastric emptying was significantly accelerated following the administration of the lowest dose of RQ-00000010 (0.1 microg/kg po). In safety pharmacology studies in vivo at doses of up to 30 microg/kg, there was no prolongation of QTc interval. The compound had Ki values of 0.87 and 1.8 nM for the human and dog recombinant 5-HT 4d receptors, respectively. In cell-based cAMP accumulation assays, RQ-00000010 had an EC50 value of 0.74 nM for the human 5-HT 4d receptor. The compound is expected to enter clinical development in 2010.
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