Innovative Drugs-Relin Medicine

Breakthrough First-in-Class New drug MS-553

Joint developers: Mingsight/Mingsight Relin

MS-533 is a novel highly selective protein kinase C (PKC) inhibitor that selectively inhibits PKC β, α, and θ, while having little effect on other isoforms such as PKC δ and others kinases.

PKC-β is one of the key links in the BCR pathway, and plays an important regulatory role in the activation, working, and proliferation of B cells.

5+indications

Conduct trials in25+domestic and foreign clinical institutions

5 internationally renowned academic centers

20+renowned domestic medical institutions

High selectivity and efficiency in targeting

First-in-Class New Drug

Diversified indications

Collaborating with global and domestic authoritative academic institutions to conduct phase I/II clinical trials

High selectivity and efficiency in targeting

Breaking through poor selectivity in previous generation of protein kinase C (PKC) inhibitors, MS-533 has high selectivity and is significantly superior to previous generation ones in terms of safety, pharmacokinetic characteristics, and therapeutic efficacy, which is the only inhibitor of B cells receptor signaling pathway (BCR) that can target multiple drug-resistant variants on BTK and PLCG2.

The target of MS-553 is PKCβ, located in downstream of BTK and PLCG2, which is a key kinase that controls this pathway.

Effective in patients who are resistant to BTK and against resistant mutations in both BTK and PLCG2 resulting from non-reversible (e.g. ibrutinib) and reversible BTK inhibitors (e.g. pirtobrutinib).

First-in-Class New Drug

First-in-Class series of novel protein kinase C (PKC) inhibitors

Introduced from an American pharmaceutical giant, with global exclusivity right

Innovative chemical structure

Selected as the 12th Five-Year Plan of the National Major Scientific and Technological Special Project for "Significant New Drugs Innovation and Development〞. (Project number: 2013ZX09102003)

Diversified indications

As Pipeline in a Product that can be developed along multiple routes for the treatment of B cell blood cancer, DME(Diabetic macular edema) and other eye diseases, autoimmune diseases, and others.

The following indications have been approved for clinical trials:

Diabetic retinopathy

Preliminary results from clinical trials of oral treatment for diabetic macular edema demonstrate a clear therapeutic effect and the potential to become the first non-invasive and highly effective treatment for macular edema.

Rheumatoid arthritis

Systemic lupus erythematosus

Chronic lymphocytic leukemia

B-cell lymphoma

Collaborating with global and domestic authoritative academic institutions to conduct phase I/II clinical trials

Clinical trials in frontline and refractory/recurrent chronic lymphocytic leukemia have validated the drug's effectiveness, it’s expected to become a potential new generation B-cell receptor inhibitor after BTK inhibitors

The phase I clinical trial of 116 healthy individuals was completed at three clinical trails centers in the United States, Australia, and Hong Kong: the drug demonstrated excellent safety and pharmacokinetic data

The CLL trial is conducted at five internationally renowned centers in the United States, led by Ohio State University (OSU):

Ohio State University (OSU), Huntsman Cancer Institute at the University of Utah, University of Michigan, Columbia University, and Cancer Center at the University of Texas (MD Anderson)