Primary purpose: To evaluate the efficacy of RX108 injection in patients with advanced hepatocellular carcinoma (HCC); Secondary purpose: To investigate the safety of RX108 injection in patients with advanced HCC; To evaluate the pharmacokinetic (PK) characteristics of RX108 injection after multiple administration in patients with advanced HCC.

Start Date26 Oct 2022

Sponsor / Collaborator

Suzhou NeuPharma Co., Ltd.

ChiCTR2100052066 / RecruitingPhase 2IIT

Safety and efficacy of RX108 delivered via drug eluting beads transarterial chemoembolization (DEB-TACE) in patients with primary hepatocellular carcinoma

Start Date01 Oct 2021

Sponsor / Collaborator

Fudan University Cancer Hospital

CTR20200524 / Active, not recruitingPhase 2

RX108在复发性胶质母细胞瘤患者中的II期临床研究

[Translation] Phase II clinical study of RX108 in patients with recurrent glioblastoma

考察RX108在复发性胶质母细胞瘤（rGBM）患者体内的疗效和安全性。

[Translation]

To investigate the efficacy and safety of RX108 in patients with recurrent glioblastoma (rGBM).

Start Date11 Jul 2020

Sponsor / Collaborator

Suzhou NeuPharma Co., Ltd.

100 Clinical Results associated with RX-108

100 Translational Medicine associated with RX-108

100 Patents (Medical) associated with RX-108

Literatures (Medical) associated with RX-108

01 Jun 2023·Molecular Cancer Therapeutics

Targeting Glutamine Metabolism with a Novel Na+/K+-ATPase Inhibitor RX108 in Hepatocellular Carcinoma

Article

Author: Qian, Xiangping ; Chakraborty, Sharmistha ; Yang, Peiying ; Chen, Dongmei ; Mou, Hongyuan ; Lorenzi, Philip L. ; Wei, Bo ; Wei, Daoyan ; Tan, Lin

AbstractThe poor prognosis and limited therapeutic options for human hepatocellular carcinoma (HCC), the most common form of liver cancer, highlight the urgent need to identify novel therapeutic modalities. Here, we describe the antitumor activity and underlying molecular mechanisms of a novel Na+/K+-ATPase inhibitor RX108 in human HCC cells and its xenograft model. RX108 dose-dependently inhibited HCC cell proliferation in vitro and tumor growth in a xenograft mouse model, and that the inhibition was associated with induction of apoptosis. Mechanistically, RX108 significantly downregulated alanine serine cysteine transporter 2 (ASCT2) protein expression and reduced glutamine and glutamate concentration in HCC cells and tumors. In addition, RX108 exposure led to a significant decrease in cell energy metabolism in Huh7 and Hep3B cells, including decreased levels of glutathione, NADH, NADPH, and mitochondrial respiration oxygen consumption rate. Furthermore, HCC cells exhibited evidence of glutamine addiction; the antiproliferative effect of RX108 was dependent on glutamine transport. Clinically, elevated ASCT2 mRNA expression in HCCs was associated with unfavorable survival. Taken together, these findings reveal a novel approach to target glutamine metabolism through inhibiting Na+/K+-ATPase and provide a rationale for using RX108 to treat HCC in patients whose tumors express ASCT2 at high levels. RX108 is currently under clinical development.

100 Deals associated with RX-108

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Indication	Highest Phase	Country/Location	Organization	Date
Metastatic Solid Tumor	NDA/BLA	US	Suzhou NeuPharma Co., Ltd.	01 Aug 2018
Advanced Malignant Solid Neoplasm	NDA/BLA	CN	Suzhou NeuPharma Co., Ltd.	12 Apr 2018
Hepatocellular Carcinoma	Phase 2	CN	Suzhou NeuPharma Co., Ltd.	26 Oct 2022
Recurrent Glioblastoma	Phase 2	CN	Suzhou NeuPharma Co., Ltd.	11 Jul 2020
Squamous cell carcinoma of head and neck metastatic	Phase 2	CN	Suzhou NeuPharma Co., Ltd.	10 Jul 2020

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