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1.Unmet Clinical needs

Drug resistance of bacteria caused by abuse of antibiotics has become one of the most urgent public health problems today, especially the most difficult to treat multi drug resistant bacteria, including MRSA, MRSE, PRSP, VRE and multidrug resistant gram-negative bacteria.
Linezolid, vancomycin and telicoplanin are commercially available drugs for the treatment of MRSA. By 2015, before the expiry of the patent, the global annual sales of linezolid had stabilized at $1 billion, with a peak of $1.353 billion. In 2020, the sales of linezolid exceeded ￥05 billion in China.
The adverse reaction of linezolid was mainly bone marrow toxicity, which led to the decrease of platelets and hemorrhage. Moreover, There are some multidrug resistant bacteria with no response to linezolid.

2.Asset’s efficacy better than linezolid, and it is a replacement product of linezolid.

3.Asset was no cross resistance to linezolid.

1) In vitro, Asset showed stronger antibacterial activity against a variety of linezolid resistant strains, and was superior to Tedizolid.

2) In vivo, Its antibacterial effect on MRSA, ARE and LRSA induced systemic infections in mice was 2-4 times better than that of linezolid.

3) In vivo, Its antibacterial effect on lethal bacteria induced pulmonary infection, MRSA induced complex/non-complex subcutaneous infections in mice is significantly better than that of linezolid.

4.Asset’s pharmacokinetic characteristics are better than linezolid, and it can achieve a low dose of 200mg, administered once a day.

5.Asset is much safety than linezolid and tedizolid.

1) High and low dose asset has no obvious changes in blood and biochemical test in rat 35 days repeat-dose toxicity experiment. However, linezolid and tedizolid showed severe toxicity.

2) Low dose asset does not cause myelosuppression like linezolid and tedizolid. And high dose asset’s myelosuppression toxicity is far less than linezolid and tedizolid.

3) In male rat : NOAEL=90mpk, Treatment window=15-18 times;

In female rat: NOAEL =30mpk, Treatment window=5-6 times.

Research progress：

Asset has approved pre-IND.