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General Description:

Eflapegrastim, identified by CAS number 1384099-30-2, is a notable compound with significant therapeutic applications. Febrile neutropenia (FN), defined as the co-occurrence of fever (temperature > 38 ◦C) and severe neutropenia (ANC < 500 cells/mm³), is a potential side effect of myelosuppressive chemotherapy in which the patient develops an infection during a period of significant neutropenia. It typically develops during the first cycle of chemotherapy and is associated with an increased risk of morbidity and mortality. The primary factor associated with FN risk is the chemotherapy regimen being administered - regimens are classified as either high-, intermediate-, or low-risk for FN, and relevant guidelines recommend the use of pharmacologic prophylaxis against FN in patients receiving high-risk regimens and those receiving intermediate-risk regimens who have ≥1 additional risk factor. Granulocyte-colony stimulating factors (G-CSFs) - which include and - were first used clinically in the 1990s and are the primary means of prophylaxis against chemotherapy-induced neutropenia, including FN. They trigger signaling pathways that control the differentiation, proliferation, migration, and survival of neutrophils, thereby helping to restore depressed neutrophil counts. Eflapegrastim is a form of recombinant human G-CSF comprising a human G-CSF analog coupled to the Fc fragment of human IgG4 via a polyethylene glycol linker. In September 2022, eflapegrastim was approved by the US FDA as a prophylactic against infection, as manifested by febrile neutropenia, in patients receiving certain myelosuppressive anti-cancer drugs.

Indications:

This drug is primarily indicated for: Eflapegrastim is indicated to decrease the incidence of infection, as manifested by febrile neutropenia, in adult patients with non-myeloid malignancies receiving myelosuppressive anti-cancer drugs associated with a clinically significant incidence of febrile neutropenia. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Eflapegrastim undergoes metabolic processing primarily in: Eflapegrastim is likely metabolized via endogenous degradation following internalization by cells expressing G-CSF receptors. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Eflapegrastim are crucial for its therapeutic efficacy: The T_max of eflapegrastim is dose-dependent and increases with increasing dose. Following administration of the recommended dosage in patients with breast cancer, the median T_max of eflapegrastim-xnst is 25 hours. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Eflapegrastim is an important consideration for its dosing schedule: In patients with breast cancer, the geometric mean half-life of eflapegrastim-xnst is 36.4 hours. This determines the duration of action and helps in formulating effective dosing regimens.

Route of Elimination:

The elimination of Eflapegrastim from the body primarily occurs through: Following subcutaneous administration, eflapegrastim is not detectable in the urine. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Eflapegrastim is distributed throughout the body with a volume of distribution of: The volume of distribution of eflapegrastim-xnst is 1.44 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Eflapegrastim is a critical factor in determining its safe and effective dosage: The clearance of eflapegrastim-xnst decreased with increasing dose, suggesting target-mediated clearance by neutrophils. With repeat dosing clearance appears to increase, potentially due to the subsequent increase in circulating neutrophils. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Eflapegrastim exerts its therapeutic effects through: Eflapegrastim increases absolute neutrophil count (ANC) in a dose-dependent manner in both healthy subjects and cancer patients. In rat studies, it was associated with higher serum and bone marrow concentrations than pegfilgrastim, which translated to a significantly shorter duration of neutropenia when eflapegrastim was administered 24 hours post-chemotherapy compared to pegfilgrastim. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Eflapegrastim functions by: Eflapegrastim is a recombinant human granulocyte-colony stimulating factor (rhG-CSF). Like endogenous G-CSF, eflapegrastim binds to G-CSF receptors on myeloid progenitor cells and neutrophils - this triggers signaling pathways that result in neutrophil differentiation, proliferation, migration, and survival. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Eflapegrastim belongs to the None, classified under the direct parent group Peptides. This compound is a part of the Organic Compounds, falling under the Organic Acids superclass, and categorized within the Carboxylic Acids and Derivatives class, specifically within the Amino Acids, Peptides, and Analogues subclass.

Categories:

Eflapegrastim is categorized under the following therapeutic classes: Amino Acids, Peptides, and Proteins, Biological Factors, Blood Proteins, Colony-Stimulating Factors, Cytokines, Globulins, Glycoproteins, Granulocyte Colony-Stimulating Factors, Hematopoietic Cell Growth Factors, Immunoglobulin Constant Regions, Immunoglobulin Fragments, Immunoglobulins, Immunoproteins, Intercellular Signaling Peptides and Proteins, Peptide Fragments, Peptides, Proteins, Serum Globulins. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Eflapegrastim include:

• Molecular Weight: 72000.0