Table 6.

Key trials in the development of the neurokinin (NK)₁-receptor antagonist rolapitant

References	Design	Investigational arm	Comparator	Chemotherapy	Primary parameter	Result
Rapoport et al. [115]	R, DB, P n = 454	Day 1: a) ROL 9 mg PO b) ROL 22.5 mg PO c) ROL 90 mg PO d) ROL 180 mg PO All: OND 32 mg IV + DEX 20 mg PO on day 1 + DEX 8 mg × 2 PO on days 2–4	OND 32 mg IV + DEX 20 mg PO on day 1 + DEX 8 mg × 2 PO on days 2–4	CIS	Complete response (no EE, no rescue medication) 0–120 h	ROL + OND + DEX > OND + DEX, all doses except ROL 9 mg ROL 180 mg chosen for phase III studies
Rapoport et al. [116]	R, DB, P n = 1070	ROL 180 mg PO + GRA 10 µg/kg IV + DEX 20 mg PO on day 1 + DEX 8 mg × 2 PO on days 2–4	GRA 10 µg/kg IV + DEX 20 mg PO on day 1 + DEX 8 mg × 2 on days 2–4	CIS	Complete response (no EE, no rescue medication) 24–120 h	ROL + GRA + DEX > GRA + DEX
Schwartzberg et al. [117]	R, DB, P n = 1332	ROL 180 mg PO + GRA 2 mg PO + DEX 20 mg PO on day 1 + GRA 2 mg × 1 on days 2–3	GRA 2 mg PO + DEX 20 mg PO on day 1 + GRA 2 mg × 1 on days 2–3	AC or various MEC	Complete response (no EE, no rescue medication) 24–120 h	ROL + GRA + DEX > GRA + DEX

A anthracycline, APR aprepitant, C cyclophosphamide, CIS cisplatin, DB double-blind, DEX dexamethasone, EE emetic episodes, GRA granisetron, IV intravenously, MEC moderately emetogenic chemotherapy, OND ondansetron, P parallel, PLA placebo, PO orally, R randomized, ROL rolapitant