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General Description:

Bebtelovimab, identified by CAS number 2578319-11-4, is a notable compound with significant therapeutic applications. Bebtelovimab (LY-COV1404, LY-3853113) is a human monoclonal antibody approved for emergency use in the treatment of COVID-19. It binds to a portion of the SARS-CoV-2 spike (S) protein's receptor-binding domain, thereby preventing spike protein interaction with ACE2 and subsequent viral entry into host cells. Bebtelovimab is notable in that the epitope to which it binds appears infrequently mutated, making it a viable candidate for use in resistant SARS-CoV-2 strains (i.e. variants of concern, VOCs), including the B.1.617.2 (Delta) and B.1.1.529 (Omicron) variants. This is in contrast to previously developed COVID-19 monoclonal antibody treatments - including , , , and - which have been found ineffective in the treatment of COVID-19 caused by the Omicron variant. Bebtelovimab was issued an emergency use authorization (EUA) by the FDA on February 11, 2022, for the treatment of mild-to-moderate COVID-19 in select patients. In November 2022, the FDA updated the Health Care Provider Fact Sheet for bebtelovimab to inform of its expected reduced activity against certain emerging Omicron subvariants of SARS-CoV-2. On November 30, 2022, the EUA for bebtelovimab was officially withdrawn due to a lack of efficacy against Omicron subvariants, therefore bebtelovimab is no longer authorized for emergency use in the US.

Indications:

This drug is primarily indicated for: Bebtelovimab currently has no approved indications. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Bebtelovimab undergoes metabolic processing primarily in: As with other therapeutic proteins, bebtelovimab is likely degraded via catabolic processes into smaller peptides and amino acids. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Bebtelovimab are crucial for its therapeutic efficacy: Following a single intravenous dose of 175mg, the mean C_max and AUC_inf of bebtelovimab were 59.8 mcg/mL and 522 mcg.day/mL, respectively. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Bebtelovimab is an important consideration for its dosing schedule: Following a single intravenous dose of 175mg, the mean elimination half-life of bebtelovimab was 11.5 days. This determines the duration of action and helps in formulating effective dosing regimens.

Volume of Distribution:

Bebtelovimab is distributed throughout the body with a volume of distribution of: At steady-state, the volume of distribution of bebtelovimab is 4.61 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Bebtelovimab is a critical factor in determining its safe and effective dosage: Following a single intravenous dose of 175mg, the mean clearance of bebtelovimab was 0.335 L/day. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Bebtelovimab exerts its therapeutic effects through: Bebtelovimab binds the SARS-CoV-2 spike protein with a dissocation constant K_D = 0.046 - 0.075 nM and blocks spike protein attachment to the human ACE2 receptor with an IC₅₀ value of 0.39 nM. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Bebtelovimab functions by: Bebtelovimab is a neutralizing human IgG1κ monoclonal antibody targeted against the spike (S) protein of SARS-CoV-2, which is responsible for facilitating viral entry into host cells. More specifically, bebtelovimab binds to an epitope of the S protein receptor-binding domain (RBD) which overlaps the ACE2-interacting site, effectively inhibiting the interaction between ACE2 and the S protein required for viral entry. Of note, the epitope to which bebtelovimab binds is infrequently mutated, making it theoretically less susceptible to viral resistance. _In vitro_ studies using a number of variants of concern (VOCs) demonstrated retained activity across all variants tested, including the newer and highly infectious B.1.1.529 (Omicron) variant. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Bebtelovimab 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:

Bebtelovimab is categorized under the following therapeutic classes: Amino Acids, Peptides, and Proteins, Antibodies, Approved Treatments for COVID-19, Blood Proteins, Globulins, Immunoglobulins, Immunoproteins, 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 Bebtelovimab include:

• Molecular Weight: 144000.0