Has broad-spectrum anti-cancer potential!

On October 8, CStone Pharmaceuticals announced that the preclinical research data of the potential “best-in-class” drug CS5001 will be selected for the 33rd International Conference on Molecular Targets and Cancer Therapy in 2021, and will be displayed in the form of posters.
Research results
.

The results showed that CS5001 showed strong selective cytotoxicity in a variety of cell lines expressing ROR1 , and showed significant in vivo anti-tumor activity in xenograft mouse models

It has shown strong selective cytotoxicity in a variety of cell lines expressing ROR1 and has shown significant in vivo anti-tumor activity in xenograft mouse models

CS5001 is an antibody-conjugated drug (ADC) composed of a human monoclonal antibody targeting receptor tyrosine kinase-like orphan receptor 1 (ROR1)
.

Through targeted coupling technology, CS5001 combines a unique β-glucuronide linker and pyrrolobenzodiazepine (PBD) protoxin dimer

CS5001 is an antibody-conjugated drug (ADC) composed of a human monoclonal antibody targeting receptor tyrosine kinase-like orphan receptor 1 (ROR1)

Studies have shown that CS5001 binds to human ROR1 but not ROR2
.

CS5001 has similar affinity to mouse, rat and cynomolgus ROR1

Demonstrates strong cytotoxicity

CS5001 showed significant anti-tumor activity in both Jeko-1 and MDA-MB-231 xenograft tumor models , and was dose-dependent
.

In addition, in the Jeko-1 model, CS5001 exhibited a higher therapeutic effect at the same toxic dose compared with the ROR1 ADC based on the MMAE toxin molecule

Shows significant anti-tumor activity in a dose-dependent manner

Dr.
Xie Yizhao, Chief Scientific Officer of CStone Pharmaceuticals, said: "ROR1 is a very potential drug target, which is highly differentially expressed in a variety of solid tumors and hematological malignancies, but is not expressed in adult healthy tissues
.

This means that ROR1 is expected to become a new drug target with broad-spectrum anti-cancer potential like PD-1/L1

This means that ROR1 is expected to become a new drug target with broad-spectrum anti-cancer potential like PD-1/L1

At present, CS5001 has completed the pre-clinical studies required for clinical application.
It has a unique design that combines the linker with the pyrrolobenzodiazepine protoxin payload (Payload) that uses tumor-specific activation
.

Only after CS5001 reaches the tumor, its linker is cleaved to release the PBD protoxin, and then the PBD protoxin is activated in the tumor cells, thereby killing the tumor cells

This "dual control" mechanism of linker plus protoxin effectively solves the typical toxicity problems associated with traditional PBD loads, and has better safety

In October 2020, CStone Pharmaceuticals and LegoChem Biosciences reached a licensing agreement on the development and commercialization of CS5001
.

According to the terms of the agreement, CStone Pharmaceuticals obtained an exclusive license to lead the development and commercialization of CS5001 in other regions of the world outside of Korea

Reference materials:

Reference materials:

[1] CStone Pharmaceuticals announces CS5001 (ROR1 ADC) research data Retrieved Oct 08.

[1] CStone Pharmaceuticals announces CS5001 (ROR1 ADC) research data Retrieved Oct 08.
2021.
from https:// at the 33rd International Conference on Molecular Targets and Cancer Therapy in 2021