China—September 8，2023，The official website of the China National Medical Products Administration (CDE) announced that Akeso, Inc.'s Class 1 new drug AK131 injection has been approved for clinical use. This drug will be used in the treatment of advanced solid tumors. Publicly available information shows that AK131 is a dual-specificity antibody targeting PD-1 and CD73, developed independently by Akeso, Inc.

CD73 is a key regulatory factor in the development and progression of tumors, it can regulate tumor invasion and metastasis capabilities. CD73-catalyzed hydrolysis of adenosine has immunosuppressive activity and plays an important role in tumor immune escape, which can lead to therapeutic resistance to anti-PD-1 antibody therapy.CD73 and PD-1 are highly expressed in the tumor microenvironment, which lays a mechanistic foundation for anti-PD-1/CD73 antibody therapy.

According to the public information of Akeso, Inc., AK131 can inhibit the ectonucleotidase activity of CD73 and reduce the accumulation of adenosine, thus lifting the suppression of anti-tumor immune activity; at the same time, it can block the binding of PD-1 and its ligands PD-L1 and PD-L2, lifting the immune suppression.

At the 2022 American Association for Cancer Research (AACR) Annual Meeting, Akeso, Inc. presented preclinical study results for AK131.

1.AK131 can effectively block PD-1/PD-L1 interaction and has good anti-PD-1/PD-L1 activity.

2.AK131 effectively inhibits CD73 activity and stimulates cellular endocytosis of CD73.

3.AK131 inhibits both the CD73 and PD-1 pathways and therefore has a stronger immune-activating potency, inducing stronger IFN-γ and IL-2 secretion.

4.Expression of CD69, CD83, HLA-DR and IgM, markers of B cell activation, can be induced to increase by AK131.

5.AK131 can significantly inhibit the growth of tumor volume and has more powerful anti-tumor activity.