"目录号: HY-14751
GPCR/G ProteinNeuronal Signaling-
Rolapitant (SCH619734)是高效选择性具有口服活性的neurokininNK1 受体抑制剂，Ki值为0.66 nM。
Neurokinin Receptor
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生物活性
Description
Rolapitant (SCH619734) is a potent, selective and orally activeneurokininNK1 receptor antagonist with aKiof 0.66 nM.
IC50& Target
Ki: 0.66 nM (neurokinin)[1]
In Vitro
Rolapitant has a high affinity for the human NK1 receptor with a Kiof 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit[1].
In Vivo
Rolapitant reverses NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective dose (MED) of 0.1 mg/kg. Rolapitant is active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively, consistent with clinical data for other NK1 antagonists. Clinical efficacy of anti-emetics is highly correlated with efficacy in the ferret emesis model, suggesting rolapitant is a viable clinical candidate for this indication[1].
Clinical Trial
NCT02285647
Tesaro, Inc.
Chemotherapy-induced Nausea and Vomiting
September 2014
Phase 1
NCT02991456
Duke University-Tesaro, Inc.
Chemo-radiation Induced Nausea and Vomiting
August 15, 2017
Phase 2
NCT01499849
Tesaro, Inc.
Chemotherapy-induced Nausea and Vomiting
February 2012
Phase 3
NCT01500226
Tesaro, Inc.
Chemotherapy-induced Nausea and Vomiting
February 2012
Phase 3
NCT01500213
Tesaro, Inc.
Chemotherapy-induced Nausea and Vomiting
February 2012
Phase 3
NCT02382666
Tesaro, Inc.
Chemotherapy-induced Nausea and Vomiting
January 2015
Phase 1
NCT02732015
M.D. Anderson Cancer Center-Tesaro, Inc.
Sarcoma
October 2016
Phase 2
NCT02434861
Tesaro, Inc.
Chemotherapy-induced Nausea and Vomiting
May 2015
Phase 1
NCT00539721
Merck Sharp & Dohme Corp.
Postoperative Nausea and Vomiting
October 2007
Phase 2
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References
[1].Duffy RA, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100.