SCH-619734 is an orally bioavailable, centrally-acting, selective neurokinin 1 receptor (NK1-receptor) antagonist with a Ki of 0.66 nM. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). Rolapitant is active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO: ≥ 25 mg/mL|
Efficacy and safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting over multiple cycles of moderately or highly emetogenic chemotherapy.
Rapoport B, et al. Eur J Cancer. 2016 Apr;57:23-30. PMID: 26851398.
Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC).
Rapoport B, et al. Support Care Cancer. 2015 Nov;23(11):3281-8. PMID: 25940030.
Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets.
Duffy RA, et al. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. PMID: 22497992.
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Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
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