Delving into the Latest Updates on Fosrolapitant with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

NK1R

Mechanism

NK1R antagonists(Neurokinin 1 receptor antagonists)

Therapeutic Areas

Other Diseases

Active Indication

Postoperative Nausea and VomitingVomiting

Inactive Indication-

Originator Organization

Jiangsu Hengrui Pharmaceutical Group Co. Ltd.

Active Organization

Fujian Suncadia Pharmaceuticals Co Ltd.

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC27H29F6N2O8P

InChIKeyPKXQGSOAMISYFP-LJXNEXSDSA-N

CAS Registry2573694-38-7

Author: Wang, Ruoyu ; Zhao, Yuanyuan ; Cao, Ke ; Leng, Shuang ; Zhang, Mingjun ; Lin, Dang ; Lin, Li ; Zhou, Huaqiang ; Zhang, Li ; Qin, Xia ; Li, Weiwei ; Li, Xiang ; Qin, Zhiquan ; Zhang, Songnan ; Wang, Zhenghua ; Li, Na ; Yi, Tienan ; Zang, Aimin ; Zhou, Ningning ; Huang, Yan ; Wang, Yujiao ; Li, Xiumin ; Fang, Wenfeng ; Yu, Yan ; Cao, Fengjun ; Wang, Huan ; Zhang, Yaxiong ; Lu, Yanda ; Yang, Runxiang ; Yao, Jun ; Yang, Yunpeng ; Zheng, Qinhong ; Zhou, Yan ; Mei, Jiazhuan ; Chen, Jinping ; Yang, Xue ; Zhou, Ting ; Chen, Gang

PURPOSEMixed formulation of fosrolapitant and palonosetron (PALO), HR20013, is a novel fixed-dose intravenous antiemetic combination that could simultaneously antagonize neurokinin-1 and 5-hydroxytryptamine-3 receptors. This study was designed to evaluate the efficacy and safety of HR20013 plus dexamethasone (DEX) versus fosaprepitant (FAPR) plus PALO + DEX for preventing chemotherapy-induced nausea and vomiting (CINV) in patients receiving highly emetogenic chemotherapy (HEC).METHODSThis is a noninferiority study. Chemotherapy-naïve patients were randomly assigned 1:1 to receive HR20013 (day 1) or FAPR + PALO (day 1) before each cycle of cisplatin-based HEC (two cycles in total), together with oral DEX (day 1-4). The primary end point was overall (0-120 hours) complete response (CR; no vomiting/no rescue therapy) rate in cycle 1. The key secondary end point was CR rate at the beyond delayed phase (120-168 hours) in cycle 1.RESULTS Three hundred seventy-three patients were enrolled to receive HR20013 + DEX and 377 to FAPR + PALO + DEX. The overall CR rate in cycle 1 was 77.7% for HR20013 + DEX and 78.2% for FAPR + PALO + DEX (difference = –0.9% [95% CI, –6.7 to 5.0]; one-sided P < .01), demonstrating that HR20013 + DEX was noninferior to FAPR + PALO + DEX. The superiority of HR20013 + DEX over FAPR + PALO + DEX in CR rate at the beyond delayed phase in cycle 1 was not met (90.3% v 86.5%; two-sided P = .11). In cycle 2, HR20013 + DEX showed greater proportions of patients reporting no impact on daily life at the delayed (24-120 hours) and beyond delayed phases compared with FAPR + PALO + DEX. The incidences of treatment-related adverse events were 35.7% during cycle 1 and 42.1% during entire study for HR20013 + DEX, versus 38.2% and 44.0% for FAPR + PALO + DEX. CONCLUSIONHR20013 + DEX was noninferior to FAPR + PALO + DEX for preventing HEC-CINV and well tolerated, with the potential to reduce the impact of CINV on daily life.

100 Deals associated with Fosrolapitant

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Postoperative Nausea and Vomiting	Phase 2	CN	Fujian Suncadia Pharmaceuticals Co Ltd.	01 Jun 2024
Vomiting	Phase 2	CN	Fujian Suncadia Pharmaceuticals Co Ltd.	01 Jun 2024