Entecavir injection(entikawei) is a highly efficient and low resistance nucleoside analogue antiviral drug, and the product, as a novel formulation form, provides an important choice for patients who cannot take it orally or need rapid control of virus replication. The inhibitory effect of entikawei on HBV is 300 times stronger than lamivudine and 10 times stronger than adefovir, and it still maintains high activity against lamivudine resistant strains.
After intravenous injection, the injection directly enters the blood circulation, bypasses the first pass effect, and the blood concentration quickly reaches the therapeutic threshold, which is suitable for patients with acute severe hepatitis B or liver failure; The bioavailability of injection is close to 100%, significantly higher than that of oral preparations.
Additional information of chemical compound:
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Entecavir COA
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| Certificate of Analysis | ||
| Compound name | Entecavir | |
| Grade | Pharmaceutical grade | |
| CAS No. | 142217-69-4 | |
| Quantity | Customized | |
| Packaging standard | Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090056 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.38% |
| Loss on drying | ≤1.0% | 0.29% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.80% |
| Single impurity | <0.8% | 0.43% |
| Total microbial count | ≤750cfu/g | 80 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 400ppm |
| Storage | Store in a sealed, dark, and dry place below -20℃ | |
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| Chemical Formula | C12H15N5O3 |
| Exact Mass | 277.12 |
| Molecular Weight | 277.28 |
| m/z | 277.12 (100.0%), 278.12 (13.0%), 278.11 (1.8%) |
| Elemental Analysis | C, 51.98; H, 5.45; N, 25.26; O, 17.31 |
Core Mechanism of Action
The core function of entecavir injection is to specifically inhibit the replication of Hepatitis B Virus (HBV). It features high targeting and specificity, which precisely interferes with the reverse transcription process of hepatitis B virion and fundamentally blocks viral proliferation and spread. Its pharmacological action is highly selective with barely any impact on DNA synthesis in normal human cells, thus ensuring superior safety and laying a solid foundation for its long-term application in chronic hepatitis B treatment.
After entering the human body, entikawei is rapidly absorbed by cells and gradually phosphorylated by intracellular kinases to form its active metabolite, entikawei triphosphate (ETV-TP). This active metabolite has an intracellular half-life of up to 15 hours, sustaining effective drug concentration to exert persistent antiviral effects, reducing administration frequency, improving patient treatment compliance and supporting standardized long-term therapy.
Structurally similar to deoxyguanosine triphosphate (dGTP), the natural substrate of hepatitis B virion reverse transcriptase (HBV DNA polymerase), ETV-TP preferentially binds to reverse transcriptase and competitively suppresses its three core activities: inhibiting primer synthesis to halt the initiation of viral replication, blocking negative-strand DNA synthesis via pregenomic mRNA reverse transcription, and restraining DNA-dependent positive-strand DNA synthesis to fully hinder viral genome replication. In addition, incorporation of ETV-TP into nascent hepatitis B virion DNA strands directly terminates DNA chain elongation, preventing the formation of complete viral genomes, drastically lowering in-vivo viral load, alleviating continuous viral damage to hepatocytes and facilitating hepatocyte repair.
Notably, entikawei exhibits extreme specificity against hepatitis B virion with extremely low affinity for human cellular DNA polymerases, causing negligible disturbance to normal cellular DNA synthesis. Compared with other antiviral agents, it imposes less damage on hematopoietic function, renal function and other vital human organs, possessing prominent safety advantages. Such highly targeted antiviral property enables it to deliver potent antiviral efficacy while maximally protecting normal physiological functions, making it a first-line antiviral drug for chronic hepatitis B.
Main Therapeutic Effects
The product is mainly applied to control and ameliorate the progression of chronic hepatitis B. Its core therapeutic goal is to potently and continuously suppress hepatitis B virion replication, mitigate hepatocytic inflammation and necrosis, preserve normal hepar function, delay the progression to severe complications such as hepar cirrhosis and hepatocytic carcinoma, relieve clinical symptoms, enhance patients' quality of life and guarantee long-term survival of patients, with its therapeutic effects manifested in four interrelated and synergistic aspects as follows:
1. Potently Reduce Hepatitis B Viral Load
hepatitis B virion viral load is a core indicator evaluating disease severity and therapeutic efficacy of chronic hepatitis B. Higher viral load indicates more active viral replication, severer hepatocytic injury and elevated risks of hepar cirrhosis and liver cancer. Entikawei boasts powerful antiviral activity and ranks among the most effective clinical anti-HBV agents. Clinical data verify that it can rapidly and markedly decline hepatitis B virion DNA levels in both treatment-naive patients and lamivudine-resistant patients.
For adult patients with compensated hepar disease receiving initial nucleoside analog therapy, most can achieve undetectable hepatitis B virion DNA levels (＜50 IU/mL) within 12 weeks of standardized treatment. For lamivudine-resistant patients, proper dose adjustment enables entecavir injection to effectively inhibit viral replication and steadily reduce viral load, creating favorable conditions for subsequent hepar function recovery.
2. Improve Liver Function and Repair Hepatocellular Injury
The core pathological changes of chronic hepatitis B are virus-induced hepatocytic inflammation and necrosis leading to abnormal hepar function, manifested as elevated alanine transaminase (ALT), aspartate transaminase (AST), abnormal bilirubin and albumin levels, and even hepar failure in severe cases.
By suppressing viral replication and reducing viral stimulation on hepatocytes, it alleviates hepatocellular inflammation fundamentally and builds a favorable environment for damaged hepatocyte repair. Massive clinical evidence proves that along with declining viral load, hepar injury markers including ALT and AST gradually return to normal, and indicators reflecting hepatitic synthesis and metabolism function are significantly improved. It effectively delays hepatitic fibrosis progression, maintains complete hepar function and prevents further hepar function deterioration.
For patients with decompensated chronic hepatitis B accompanied by severe hepar damage and multiple complications, entikawei can steadily inhibit viral replication, relieve hepatic inflammation, lower the incidence of hepatitic encephalopathy, hepatorenal syndrome, ascites and other critical complications, stabilize severe conditions, elevate short-term survival rate, win time for comprehensive treatment and support gradual hepar function recovery.
3. Delay Progression of hepatitic Fibrosis, Liver Cirrhosis and hepatocytic Carcinoma
Uncontrolled chronic hepatitis B leads to persistent hepatocytic damage, progressive hepatitic fibrosis and eventual liver cirrhosis, which may further develop into primary hepatocytic carcinoma, one of the leading fatal causes for hepatitis B patients. Long-term potent viral suppression by the product can effectively slow down hepatitic fibrosis progression, achieve obvious histological improvement and reverse mild hepatitic fibrosis in early-stage patients.
Long-term clinical follow-up studies confirm that standardized long-term entikawei treatment significantly reduces the incidence of hepar cirrhosis and hepatocytic carcinoma compared with untreated patients. It notably cuts disease progression risks and prolongs survival time for high-risk populations with high viral load, recurrent abnormal hepar function and family history of hepar cirrhosis. Moreover, for hepatitis B-related liver transplant recipients, the product efficiently inhibits hepatitis B virion recurrence post-operation, stabilizes graft hepar function, improves hepar transplant success rate and ensures long-term postoperative survival.
4. Alleviate Clinical Symptoms and Improve Quality of Life
Chronic hepatitis B patients commonly suffer from fatigue, poor appetite, nausea, abdominal distension and dull right upper quadrant pain, which are closely correlated with virus-induced hepar dysfunction and severely disturb daily life, work and mental state. By suppressing viral replication and restoring hepar function, entecavir injection effectively relieves the above discomforts. During treatment, patients gradually regain physical strength and appetite, with gastrointestinal and hepatitic discomfort relieved or eliminated, thereby greatly improving life quality, helping patients resume normal work and daily activities and easing physical and mental burdens caused by the disease.
The research and development of entikawei commenced in the 1990s, led by Bristol-Myers Squibb Company. Initially, it was developed as a candidate anti-herpes simplex virus drug rather than a hepatitis B therapeutic agent. The R&D team focused on structural optimization of nucleoside antiviral compounds to screen broad-spectrum and high-efficiency small-molecule antiviral drugs.
In activity screening of various carbocyclic nucleoside analogs, the compound was found to only exert moderate inhibitory effect on herpes virus, failing to meet clinical application standards and lacking development value for herpes treatment.
Subsequent broad-spectrum antiviral screening experiments made a groundbreaking discovery that this compound possessed extremely specific and potent inhibitory activity against hepatitis B virion, far exceeding mainstream anti-HBV drugs at that time.
In vitro cellular experiments also confirmed its low cytotoxicity and prominent safety profile. Based on this key finding, the R&D team promptly adjusted the research orientation and officially positioned it as a novel anti-HBV drug, carrying out systematic structural optimization, pharmacological verification and pharmacodynamic tests.
In 1997, the core chemical structure of entikawei was finalized, with basic pharmacology and toxicology studies completed, after which it entered clinical trials.
After years of verification in Phase I, II and III clinical trials, its advantages including strong antiviral potency, low drug resistance and high safety were fully validated.
In 2005, entikawei was officially approved for marketing by the U.S. FDA and launched into the Chinese market in the same year. As the world's first new-generation first-line anti-HBV drug with high efficacy and low drug resistance, it completely revolutionized the clinical treatment pattern of chronic hepatitis B.
Chemically, entikawei is a carbocyclic guanosine nucleoside analog consisting of a chiral five-membered carbocyclic ring and guanine base. The chiral centers within its structure are critical to biological activity, hence the core synthesis challenges lie in precise chiral configuration control, impurity removal and yield improvement.
The original research synthetic route featured cumbersome procedures and high production costs, while subsequent domestic research teams optimized the process to realize efficient industrial production.
The original synthesis adopts cyclopentadiene derivatives as starting materials to construct the core five-membered carbocyclic skeleton via multi-step addition, cyclization and hydrolysis reactions. Single active configuration intermediates are obtained through chiral resolution, followed by condensation reaction with guanine parent nucleus to prepare crude entikawei.
Traditional techniques are restricted by low chiral resolution efficiency, excessive by-products and difficulty in purity control, limiting large-scale production.
Domestic researchers innovatively developed a chiral directional synthesis technology that abandons traditional resolution methods. By regulating reaction temperature, catalyst ratio and solvent system, target chiral intermediates are directly synthesized directionally to reduce invalid isomer generation and lower impurity content from the source.
The optimized synthetic process mainly includes three core steps: constructing high-purity chiral carbocyclic skeletons via asymmetric catalytic cyclization to ensure active drug configuration; implementing protection and modification on hydroxyl groups of carbocyclic side chains to avoid side reactions during condensation; conducting nucleophilic condensation with guanine base, followed by deprotection, refining and recrystallization purification to obtain high-purity entikawei bulk drugs.
This optimized process greatly simplifies reaction steps, boosts raw material utilization rate and product purity, resolves impurity control difficulties in original research techniques, bypasses original patent barriers and achieves domestic large-scale mass production, providing sufficient raw material support for the clinical popularization of entikawei injection.
FAQ
What is it used for?
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Entikawei is used to treat liver infection caused by hepatitis B virus. It belongs to the family of medicines called antivirals. Antivirals are used to treat infections that are caused by viruses. This medicine will not cure the hepatitis B virus, but it will keep it from reproducing and causing more liver damage.
How long to take it for hepatitis B?
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Treatment duration will be long-term in most patients until there is a loss of surface antigen (note though loss of surface antigen occurs in less than 10% of patients). You will therefore likely remain on entecavir for life or until other treatments become available.
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