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Entecavir（SQ 34676; BMS 200475）is selective and effective HBV Inhibitor. In HepG2 cells EC50 value is 3.75 nM. The latest anti-hepatitis B and anti-AIDS first-line drugs.

Entecavir effect

This product is a guanine nucleoside analog, which has an inhibitory effect on hepatitis B virus (HBV) polymerase. It can be phosphorylated into active triphosphate, and the half-life of triphosphate in the cell is 15 hours. By competing with HBV polymerase’s natural substrate deoxyguanosine triphosphate, entecavir triphosphate can inhibit all three activities of viral polymerase (reverse transcriptase): (1) HBV polymerase initiation; (2) pregenomic mRNA The formation of the negative strand of reverse transcription; (3) The synthesis of the positive strand of HBV DNA. The inhibitory constant (Ki) of entecavir triphosphate on HBV DNA polymerase is 0.0012μM. Entecavir triphosphate has weak inhibitory effect on cell α, β, δ DNA polymerase and mitochondrial γ DNA polymerase, with Ki value of 18 to 160 μM.

Physical and chemical properties of Entecavir

Entecavir Customs

Additional information:

Qu Qiang (PhD in clinical pharmacology, Department of Pharmacy, Xiangya Hospital, Central South University) and Wang Ruoguang (Doctor of Medicine, postdoctoral in biology, Changsha Ruoguang Medical Research Center) also wrote that: in the entecavir regimen, entecavir can be taken for several years or even 10 years. More than years. And it can be used by pregnant women, showing good safety.

Judging from these known molecular pharmacological mechanisms, Entecavir may have a broad-spectrum antiviral effect, not only effective against HBV.

We also often use Entecavir to treat viral respiratory infections in the clinic, and the effect is remarkable.

At present, in a retrospective analysis of more than 500 COVID19 patients in Hubei (a place), only one person took entecavir. The prescription time was in early January, and then the drug was stopped.

While supporting medical staff in Hubei, some grassroots doctors, or high-risk groups, currently using Entecavir to prevent COVID19, there is no case of infection. Suspected people taking entecavir, no one has progressed to be diagnosed with COVID19.

Patent issues:

There are mainly two processes, 06 process and 89 process. The expiration of the patent for the 06 process is too early (expires in 2023)! Although the cost of the process is low, the quality is relatively good, and the workers can be strong, personal advice: For chemical plants, use the 06 process not to be too arrogant; for pharmaceutical companies, don’t take a fluke and don’t be too risky .

In 2014, Chia Tai Tianqing achieved annual sales of 10 billion yuan by relying on generic drugs such as entecavir, of which entecavir accounted for 20%.

Since entecavir was approved for import in 2005, more than 100 domestic pharmaceutical companies have applied for the registration of the product; among them, the approved production companies include Jiangsu Zhengda Tianqing Pharmaceutical (first imitation), Hainan Zhonghe Pharmaceutical, and Fujian Guangxi Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical, Suzhou Dawnrays Pharmaceutical, Shanghai Qingsong Pharmaceutical, Sichuan Haisco Pharmaceutical, Shandong Lukang, Zhejiang Huasheng Biopharmaceutical, Changzhi Sanbao Biochemical.

Pharmaceutical, Anhui Baker Biopharmaceutical, Hunan Concord Pharmaceutical Industry, Beijing Xiehe Pharmaceutical Factory, Beijing Baiao Pharmaceutical, Xinlitai Pharmaceutical, Dongyangguang, etc.; further from the date of contract, this product has entered the ranks of popular declared varieties since 2007.