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An Open-Label, Randomized, Pivotal Bioequivalence Study of Oral Rolapitant.
Clin Pharmacol Drug Dev 2019; 8(2):152-159CP

Abstract

Rolapitant, a selective and long-acting neurokinin-1 receptor antagonist, is approved in an oral formulation for prevention of delayed chemotherapy-induced nausea and vomiting in adults. This pivotal open-label, randomized, single-dose, multicenter, parallel-group study assessed the bioequivalence of a single oral dose of 180 mg of rolapitant administered in tablet (2 × 90-mg tablets) or capsule (4 × 45-mg capsules) form in healthy male and female subjects. Blood samples for pharmacokinetic analysis were collected predose and at times up to 912 hours postdose. The rolapitant tablet was considered bioequivalent to the rolapitant capsule if the 90% confidence intervals for the ratios of the geometric means for rolapitant, observed maximum plasma concentration (Cmax), and area under the curve from time 0 extrapolated to infinity (AUC0-∞) were within the 0.80-1.25 range. The pharmacokinetic profiles of the capsule group (n = 43) and tablet group (n = 44) were similar. The geometric mean ratios of Cmax and AUC0-∞ were 0.99 (0.89-1.11) and 1.05 (0.92-1.19), respectively, establishing bioequivalence of the rolapitant tablet and capsule formulations. Both formulations were well tolerated, with a similar incidence of treatment-emergent adverse events in the 2 groups.

Authors+Show Affiliations

TESARO, Inc., Waltham, MA, USA.TESARO, Inc., Waltham, MA, USA.TESARO, Inc., Waltham, MA, USA.TESARO, Inc., Waltham, MA, USA.TESARO, Inc., Waltham, MA, USA.TESARO, Inc., Waltham, MA, USA.TESARO, Inc., Waltham, MA, USA.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30624856

Citation

Zhang, Zhi-Yi, et al. "An Open-Label, Randomized, Pivotal Bioequivalence Study of Oral Rolapitant." Clinical Pharmacology in Drug Development, vol. 8, no. 2, 2019, pp. 152-159.
Zhang ZY, Wang J, Arora S, et al. An Open-Label, Randomized, Pivotal Bioequivalence Study of Oral Rolapitant. Clin Pharmacol Drug Dev. 2019;8(2):152-159.
Zhang, Z. Y., Wang, J., Arora, S., Lu, S., Powers, D., Kansra, V., & Wang, X. (2019). An Open-Label, Randomized, Pivotal Bioequivalence Study of Oral Rolapitant. Clinical Pharmacology in Drug Development, 8(2), pp. 152-159. doi:10.1002/cpdd.651.
Zhang ZY, et al. An Open-Label, Randomized, Pivotal Bioequivalence Study of Oral Rolapitant. Clin Pharmacol Drug Dev. 2019;8(2):152-159. PubMed PMID: 30624856.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - An Open-Label, Randomized, Pivotal Bioequivalence Study of Oral Rolapitant. AU - Zhang,Zhi-Yi, AU - Wang,Jing, AU - Arora,Sujata, AU - Lu,Sharon, AU - Powers,Dan, AU - Kansra,Vikram, AU - Wang,Xiaodong, Y1 - 2019/01/09/ PY - 2017/09/25/received PY - 2018/12/03/accepted PY - 2019/1/10/pubmed PY - 2019/1/10/medline PY - 2019/1/10/entrez KW - CINV KW - NK-1 receptor antagonist KW - Rolapitant KW - bioequivalence KW - nausea SP - 152 EP - 159 JF - Clinical pharmacology in drug development JO - Clin Pharmacol Drug Dev VL - 8 IS - 2 N2 - Rolapitant, a selective and long-acting neurokinin-1 receptor antagonist, is approved in an oral formulation for prevention of delayed chemotherapy-induced nausea and vomiting in adults. This pivotal open-label, randomized, single-dose, multicenter, parallel-group study assessed the bioequivalence of a single oral dose of 180 mg of rolapitant administered in tablet (2 × 90-mg tablets) or capsule (4 × 45-mg capsules) form in healthy male and female subjects. Blood samples for pharmacokinetic analysis were collected predose and at times up to 912 hours postdose. The rolapitant tablet was considered bioequivalent to the rolapitant capsule if the 90% confidence intervals for the ratios of the geometric means for rolapitant, observed maximum plasma concentration (Cmax), and area under the curve from time 0 extrapolated to infinity (AUC0-∞) were within the 0.80-1.25 range. The pharmacokinetic profiles of the capsule group (n = 43) and tablet group (n = 44) were similar. The geometric mean ratios of Cmax and AUC0-∞ were 0.99 (0.89-1.11) and 1.05 (0.92-1.19), respectively, establishing bioequivalence of the rolapitant tablet and capsule formulations. Both formulations were well tolerated, with a similar incidence of treatment-emergent adverse events in the 2 groups. SN - 2160-7648 UR - https://www.unboundmedicine.com/medline/citation/30624856/An_Open-Label,_Randomized,_Pivotal_Bioequivalence_Study_of_Oral_Rolapitant L2 - https://doi.org/10.1002/cpdd.651 DB - PRIME DP - Unbound Medicine ER -