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General Description:

Tasonermin, identified by CAS number 94948-59-1, is a notable compound with significant therapeutic applications. Tasonermin is recombinant soluble form tumor necrosis factor α produced via _Escherichia coli_ cell culture. It was approved for use by the European Medicines Agency in April of 1999 for use as an adjunt to surgery for the subsequent removal of the tumor and in palliative care for irresectable soft tissue sarcoma of the limbs as the product Beromun. It is administered with via mild hyperthermic isolated limb perfusion.

Indications:

This drug is primarily indicated for: For use in adults as an adjunct to surgery for subsequent removal of the tumour so as to prevent or delay amputation, or in palliative care, for irresectable soft tissue sarcoma of the limbs . Used in combination with melphalan via mild hyperthermic isolated limb perfusion. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Tasonermin undergoes metabolic processing primarily in: No metabolism data is available. Tasonermin is assumed to be broken down similarly to other proteins in systemic circulation. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Tasonermin are crucial for its therapeutic efficacy: No absorption data is available. No enteral route formulation exists for tasonermin. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Tasonermin is an important consideration for its dosing schedule: Tasonermin has a terminal half life of 20-30 min at doses of 150 μg/m² . This value increases as dosage increases. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Tasonermin exhibits a strong affinity for binding with plasma proteins: No data is available on tasonermin binding to plasma proteins. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Tasonermin from the body primarily occurs through: No data is available on route of elimination. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Tasonermin is distributed throughout the body with a volume of distribution of: The estimated volume of distribution varies with the dose administered with intravenous doses of 35 μg/m² and 150 μg/m² producing values of 55 L and 17 L respectively . This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Tasonermin is a critical factor in determining its safe and effective dosage: Clearance was estimated to be 2 L/min and 0.5 L/min after intravenous doses of 35 μg/m² and 150 μg/m² respectively . This value decreases as dosage increases. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Tasonermin exerts its therapeutic effects through: Tasonermin is thought to contribute to the destruction of tumor tissue via several direct and indirect effects . Tasonermin directly inhibits cell proliferation in a variety of cancer cells. It also modifies endothelial cell morphology and reduces their proliferation in tumor microvasculature. Modification of the expression of cell adhesion proteins, proteins affecting coagulation, interleukins, and hematopoietic growth factors favors a procoagulant state resulting in microvascular thrombosis. These changes also increase infiltration of the tumor tissue by leukocytes. Monocytes, macrophages, and granulocytes are activated allowing better adherence to the endothelium and subjecting the tumor cells to phagocytosis and respiratory bursts as well as producing degranulation of immune cells to further enhance inflammatory activity. Active antigen presenting cells are able to activate and induce proliferation of T- and B-lymphocyte cells to allow the adaptive immune system to contribute to tumor cell damage. These changes lead to hemorraghic necrosis of the tumor. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Tasonermin functions by: Since tasonermin is recombinant TNF-α, it functions exactly as endogenous TNF-α does. The direct cytotoxic effect of TNF-α is mediated by TNF-α receptor 1 . The bound receptor activates the well-reviewed death receptor pathway involving the activation of initiator caspases 8 and 9 then ultimately ending in the activation of effector caspase 3 which begins the process of apoptosis. The effect on tumor vasculature is mediated by the inflammatory signalling pathway of TNF-α, the NFκB pathway . This pathway is also activated by TNFR1 when bound to TNFα. The NFκB transcription factor increases expression of proteins in vascular endothelial cells. These proteins include cell adhesion molecules, inflammatory mediators like prostaglandins and interleukins, and growth factors . TNF-&alpha also increases the expression of inducible nitric oxide synthase via this pathway which contributes to the generation of reactive nitrogen species . These species are able to damage cells in the tumor and microvasculature. The cytokines produced from NFκB activation and TNF-&aplha; itself serve to activate the cells of the immune system which further damage tumor cells with respiratory bursts, phagocytosis and subsequent breakdown of the cell, and release of cytotoxic enzymes. The antigen presenting cells which phagocytose the tumor cells are able to activate lymphocytes and allow the adaptive immune system to further damage the tumor tissue . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Tasonermin 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:

Tasonermin is categorized under the following therapeutic classes: Adjuvants, Immunologic, Antineoplastic and Immunomodulating Agents. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Tasonermin include:

• Isoelectric Point: 6.7
• Molecular Weight: 17724.0