Mychexin (WGI-0301) / Opus Genetics, Zhejiang Haichang Bio-Tech - LARVOL DELTA

Phase 2 Study of WGI-0301 for Advanced HCC (clinicaltrials.gov) - P2 | N=60 | Not yet recruiting | Sponsor: Zhejiang Haichang Biotech Co., Ltd. | Initiation date: Apr 2024 ➔ Aug 2024

Metastases • Trial initiation date • Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor

Anti-tumor effect of the combination of a lipid nanoparticle suspension of an AKT-1 antisense oligonucleotide (WGI-0301) with tyrosine kinase inhibitors in an orthotopic murine tumor model (AACR 2024) - "Background: Archexin is a fully phosphorothioated 20-mer antisense oligonucleotide, complementary to AKT-1 mRNA, which leads to the inhibition of translation and the downstream pathway activities of AKT-1 mRNA... The anti-tumor effect of combining WGI-0301 with Lenvatinib/Sorafenib/Cabozantinib was assessed using a Hep3B-Luciferase orthotopic mouse tumor model... The combination of WGI-0301 with TKIs demonstrated superior anti-tumor efficacy over TKI monotherapy in the absence of substantial increase in toxicity. This finding warrants further robust clinical investigation in patients with advanced HCC."

Preclinical • Oncology • Solid Tumor • AKT1

Phase 2 Study of WGI-0301 in Combination With Sorafenib for Advanced HCC (clinicaltrials.gov) - P2 | N=60 | Not yet recruiting | Sponsor: Zhejiang Haichang Biotech Co., Ltd.

Combination therapy • Metastases • New P2 trial • Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor

A Phase I First in Human Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of WGI-0301 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=24 | Recruiting | Sponsor: Zhejiang Haichang Biotech Co., Ltd. | Trial completion date: Dec 2023 ➔ Dec 2024 | Trial primary completion date: Sep 2023 ➔ Oct 2024

Metastases • Trial completion date • Trial primary completion date • Oncology • Solid Tumor

Orphan Designation: Treatment of Hepatocellular Carcinoma (FDA) - Date Designated: 09/20/2023

Orphan drug • Gastrointestinal Cancer • Hepatocellular Cancer • Liver Cancer • Oncology • Solid Tumor

A Phase I First in Human Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of WGI-0301 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=24 | Recruiting | Sponsor: Zhejiang Haichang Biotech Co., Ltd. | Not yet recruiting ➔ Recruiting | Trial completion date: Sep 2023 ➔ Dec 2023

Enrollment open • Trial completion date • Oncology • Solid Tumor

The anti-tumor and anti-angiogenic effects of a lipid nanoparticle suspension of an AKT-1 anti-sense oligonucleotide (AACR 2023) - "Archexin is a fully phosphorothioated 20-mer antisense oligonucleotide, which can specifically bind to AKT-1 mRNA resulting in RNase H-based AKT-1 downregulation. Data obtained demonstrated anti-tumor and anti-angiogenesis efficacy of WGI-0301. In addition, combining WGI-0301 with Sorafenib or Lenvatinib resulted in increased anti-angiogenetic activity relative to monotherapy. WGI-0301 warrants further investigation as a selective AKT-1 inhibitor."

Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor • AKT1

Results of a phase II study to evaluate the safety and efficacy of RX-0201 in combination with everolimus in subjects with metastatic renal cell carcinoma (mRCC). (ASCO-GU 2019) - P1b/2; "In this mRCC population with extensive prior therapy, RX-0201 in combination with everolimus was safe, well-tolerated, and showed promising efficacy. The results also support the therapeutic significance of the AKT-1/mTOR pathway in mRCC."

Clinical • Combination therapy • P2 data • Genito-urinary Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor

A Phase I First in Human Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of WGI-0301 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=24 | Not yet recruiting | Sponsor: Zhejiang Haichang Biotech Co., Ltd. | Initiation date: Apr 2022 ➔ Aug 2022

Trial initiation date • Oncology • Solid Tumor

Results of a phase II study to evaluate the safety and efficacy of RX-0201 in combination with everolimus in subjects with metastatic renal cell carcinoma (mRCC). (ASCO-GU 2019) - P1b/2; "In this mRCC population with extensive prior therapy, RX-0201 in combination with everolimus was safe, well-tolerated, and showed promising efficacy. The results also support the therapeutic significance of the AKT-1/mTOR pathway in mRCC."

Clinical • Combination therapy • Genito-urinary Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor

Dose-Finding, Safety and Efficacy Study of RX-0201 Plus Everolimus in Metastatic Renal Cell Cancer (clinicaltrials.gov) - P1b/2; N=28; Terminated; Sponsor: Rexahn Pharmaceuticals, Inc.; Trial completion date: Dec 2018 ➔ May 2018; Recruiting ➔ Terminated

Trial completion date • Trial termination • Biosimilar • Genito-urinary Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor

T7 Peptide-conjugated Lipid Nanoparticles for Dual-modulation of Bcl-2 and Akt-1 in Lung and Cervical Carcinomas. (PubMed, Mol Pharm) - "In addition, both T7-conjugated Co-ASO-LNPs and non-T7-conjugated Co-ASO-LNPs at a molar ratio of (G3139-GAP to RX-0201-GAP at 1:2) showed efficient downregulation of both Bcl-2 and Akt-1 in both A549 and KB cells. Furthermore, T7-conjugated co-loaded ASOs-LNPs (Co-ASOs-LNPs) produced superior anti-tumor activity, prolonged the overall survival time, and demonstrated tumor targeting activity in an A549 xenograft model."

IO Biomarker • Journal