Enfuvirtide Injection

Enfuvirtide Injection, which is a synthetic peptide composed of 36 amino acids and belongs to the HIV fusion inhibitor class of drugs. It interferes with the fusion process between HIV virus and host cell membrane, preventing the virus from entering the cell for replication, thereby achieving the goal of inhibiting virus replication and controlling disease progression. Its appearance is usually white to off white freeze-dried powder, which needs to be dissolved in sterile injection water and injected subcutaneously. The development of Enfuvirtide began in the mid-1990s, jointly developed by Trimeris of the United States and Roche of Switzerland. Scientists have discovered the crucial role of the viral envelope protein gp41 in the fusion process of HIV virus and host cells through in-depth research. Gp41 contains two important heptapeptide repeat sequences (HR1 and HR2), which interact with the virus and cell membrane during fusion, forming a six helix bundle structure, thereby bringing the virus and cell membrane closer together and promoting fusion.

 

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Enfuvirtide​​​​​​​ COA

Certificate of Analysis
Compound name	Enfuvirtide
Grade	Pharmaceutical grade
CAS No.	159519-65-0
Quantity	15g
Packaging standard	PE bag+Al foil bag
Manufacturer	Shaanxi BLOOM TECH Co., Ltd
Lot No.	202501090053
MFG	Jan 9th 2025
EXP	Jan 8th 2028
Structure
Item	Enterprise standard	Analysis result
Appearance	White or almost white powder	Conformed
Water content	≤5.0%	0.43%
Loss on drying	≤1.0%	0.52%
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%	99.90%
Single impurity	<0.8%	0.24%
Total microbial count	≤750cfu/g	90
E. Coli	≤2MPN/g	N.D.
Salmonella	N.D.	N.D.
Ethanol (by GC)	≤5000ppm	500ppm
Storage	Store in a sealed, dark, and dry place below -20°C

Enfuvirtide Injection is a novel antiviral drug belonging to the category of fusion inhibitors. Its mechanism of action is unique and highly targeted, mainly exerting antiviral effects by interfering with the process of HIV-1 virus entering host cells.

The entry of HIV-1 virus into host cells is a highly coordinated multi-step process involving the fusion of the viral envelope and the host cell membrane. The core of this process is the synergistic effect of glycoproteins gp41 and gp120 on the viral envelope:

Binding of gp120 to CD4 receptor: HIV-1 virus first binds to the CD4 receptor on the surface of host cells through the gp120 protein on its envelope. This step is crucial for virus recognition and adsorption onto host cells.
Helper receptor binding: gp120 subsequently interacts with helper receptors (such as CCR5 or CXCR4), causing a conformational change in gp120 and exposing the fusion peptide of gp41.
Gp41 mediated membrane fusion: gp41 is a transmembrane protein that contains two important heptad repeat sequences, HR1 and HR2. During virus fusion, HR1 and HR2 interact to form a six helix bundle structure. This structure brings the viral envelope closer to and fuses with the host cell membrane, forming fusion pores that allow viral genetic material to enter the host cell.

Enfuvirtide is an artificially synthesized peptide drug consisting of 36 amino acid residues. Its design inspiration comes from the HR2 domain of the gp41 protein on the HIV-1 viral envelope. The amino acid sequence of Enfuvirtide is highly similar to the HR2 domain of gp41, allowing it to specifically bind to the HR1 domain of gp41.

Enfuvirtide interferes with the entry of HIV-1 virus into host cells through the following steps:

Combining the HR1 domain: When Enfuvirtide is injected into the body, it quickly distributes to the blood and tissues, and specifically binds to the HR1 domain of the gp41 protein on the HIV-1 viral envelope.

Preventing the formation of HR1-HR2 complexes: During viral fusion, the HR1 and HR2 domains of gp41 need to interact to form a six helix bundle structure, which is a critical step in membrane fusion. Enfuvirtide occupies the position where HR2 should bind by binding to the HR1 domain, thereby preventing the formation of HR1-HR2 complexes.

Locking gp41 in inactive state: Due to the presence of Enfuvirtide, gp41 is unable to complete its structural rearrangement and form a six helix bundle structure with fusion activity. Therefore, gp41 is locked in an inactive state and cannot mediate the fusion of the viral envelope with the host cell membrane.

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Blocking virus entry into host cells: Due to the inhibition of membrane fusion, HIV-1 virus is unable to release its genetic material into host cells, thus unable to complete the infection process. This effectively blocks the replication cycle of the virus, reducing its spread and replication within the body.

The mechanism of action of enfuvirtide Injection has the following unique advantages:

Targeting the early stages of the viral life cycle

Unlike other antiretroviral drugs such as reverse transcriptase inhibitors, integrase inhibitors, and protease inhibitors, Enfuvirtide acts on the early stages of the viral life cycle, before the virus enters the host cell. This enables it to block the infection process before the virus begins to replicate, thereby more effectively controlling virus replication.

Reducing the occurrence of viral drug resistance

Due to the fact that Enfuvirtide acts in the early stages of the virus lifecycle and its target (gp41) is relatively conserved during virus replication, it is difficult for the virus to develop drug resistance through mutations. This makes Enfuvirtide an important choice for treating HIV-1 infected patients who are resistant to other antiretroviral drugs.

Synergistic effects with other drugs

Enfuvirtide can be used in combination with other antiretroviral drugs such as reverse transcriptase inhibitors, integrase inhibitors, and protease inhibitors to form a multi drug combination therapy regimen. This combination therapy can target different stages of the virus lifecycle, effectively controlling virus replication, reducing the occurrence of virus resistance, and improving patients' quality of life.

Reduce viral load

Multiple clinical trials have shown that the combination of Enfuvirtide and other antiretroviral drugs can significantly reduce the viral load in the blood of multidrug-resistant HIV infected patients. For example, in a clinical trial targeting HIV-1 infected patients resistant to multiple antiretroviral drugs, treatment with Enfuvirtide in combination with other antiviral drugs resulted in an average decrease of 1.5-2.0 log10 copies/mL. This helps to control virus replication, slow down disease progression, and improve patients' quality of life.

Improve immune function

By reducing viral load, Enfuvirtide can also help restore patients' immune function. In the aforementioned clinical trials, the combination therapy with Enfuvirtide resulted in an average increase of 50-100 cells/μ L in CD4+T lymphocyte counts in patients. This helps to reduce the occurrence of opportunistic infections and improve the survival rate of patients.

Tolerance and safety

Although Enfuvirtide has shown good tolerability and safety in clinical applications, some patients may experience adverse reactions such as injection site reactions (such as pain, redness, and induration). These adverse reactions can usually be alleviated by adjusting the injection site or using local anesthetics. In addition, the use of Enfuvirtide may increase the risk of bacterial pneumonia, so patients' respiratory symptoms should be closely monitored during use and timely anti infective treatment should be given.

Long term treatment effect

Long term follow-up studies have shown that the combination of Enfuvirtide and other antiviral drugs can maintain long-term virological suppression and immunological improvement in patients with multidrug-resistant HIV infection. In a 48 week follow-up study, approximately 70% of patients treated with Enfuvirtide combination therapy were able to maintain viral load below the detection limit (<50 copies/mL), and CD4+T lymphocyte counts continued to increase. This indicates that the combination therapy of Enfuvirtide has long-lasting antiviral effects and immune reconstitution effects.

Current situation of multidrug-resistant HIV infection

 

According to WHO statistics, approximately 5% -10% of ART patients worldwide have multidrug resistance (MDR), defined as resistance to at least two types of antiretroviral drugs (NRTI, NNRTI, PI). In China, the proportion of MDR in treated patients has reached 12.3% and is showing an increasing trend year by year. These patients often have a viral load greater than 100000 copies/mL, CD4+T cell count less than 100 cells/μ L, and a significantly increased risk of opportunistic infections.

Limitations of Traditional ART

 

(1) Cross resistance: Traditional drugs have similar targets of action, and a single resistant strain may lead to multidrug failure through genetic mutations.
(2) Immune reconstitution failure: Even with viral load suppression, some patients' CD4+T cell counts cannot be restored (approximately 15% -30% of immune non responders).
(3) Accumulation of drug toxicity: Long term use of nucleoside reverse transcriptase inhibitors (NRTI) may lead to mitochondrial toxicity (such as acidosis and fat atrophy), while protease inhibitors (PI) can cause metabolic syndrome (such as hyperlipidemia and insulin resistance).

Differentiation advantages of Enfuvirtide

 

New mechanism of action: As a fusion inhibitor, Enfuvirtide has no cross resistance with existing ART drugs and can reconstruct effective treatment plans.
Rapid virological response: Clinical data shows that after combined optimized background therapy (OBT), patients' viral load decreased by an average of 1.5-2.0 log10 copies/mL, and 62% of patients had viral load<50 copies/mL at 48 weeks.
Immune protective effect: By blocking new cell infections, Enfuvirtide Injection can reduce the replenishment of the virus pool and buy time for the immune system to recover. Research has shown that after 12 weeks of treatment, the average CD4+T cell count increases by 50-100 cells/μ L, and the magnitude of the increase is negatively correlated with baseline viral load.

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