Primary information |
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ID | 16380 |
Therapeutic ID | Th1890 |
Protein Name | Bebtelovimab |
Sequence | >Th1890_Bebtelovimab
QITLKESGPTLVKPTQTLTLTCTFSGFSLSISGVGVGWLRQPPGKALEWLALIYWDDDKRYSPSLKSRLTISKDTSKNQVVLKMTNIDPVDTATYYCAHHSISTIFDHWGQGTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Molecular Weight | 144000.0 Da |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | Following a single intravenous dose of 175mg, the mean elimination half-life of bebtelovimab was 11.5 days |
Description | 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.1 This is in contrast to previously developed COVID-19 monoclonal antibody treatments - including bamlanivimab, etesevimab, casirivimab, and imdevimab - which have been found ineffective in the treatment of COVID-19 caused by the Omicron variant. |
Indication/Disease | The FDA has issued an emergency use authorization (EUA) for the use of bebtelovimab for the treatment of mild-to-moderate COVID-19 in adult and pediatric patients (≥12 years old and ≥40 kg) who are positive for SARS-CoV-2 infection, are at a high risk of progression to severe COVID-19, and for whom alternative treatment options are not accessible or clinically appropriate. |
Pharmacodynamics | Bebtelovimab binds the SARS-CoV-2 spike protein with a dissocation constant KD = 0.046 - 0.075 nM and blocks spike protein attachment to the human ACE2 receptor with an IC50 value of 0.39 nM. |
Mechanism of Action | Bebtelovimab is a neutralizing human IgG1κ monoclonal antibody targeted against the spike (S) protein of SARS-CoV-2,2 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. |
Toxicity | Single doses of up to 1750mg of bebtelovimab (10 times the authorized dose) have been administered in clinical trials without evidence of dose-limited toxicity. Treatment of bebtelovimab overdose should consist of general supportive measures. |
Metabolism | As with other therapeutic proteins, bebtelovimab is likely degraded via catabolic processes into smaller peptides and amino acids. |
Absorption | Following a single intravenous dose of 175mg, the mean Cmax and AUCinf of bebtelovimab were 59.8 mcg/mL and 522 mcg.day/mL, respectively. |
| At steady-state, the volume of distribution of bebtelovimab is 4.61 L. |
Clearance | Following a single intravenous dose of 175mg, the mean clearance of bebtelovimab was 0.335 L/day. |
Categories | Amino Acids, Peptides, and Proteins,Antibodies,Approved Treatments for COVID-19,Blood Proteins,Globulins,Immunoglobulins,Immunoproteins,Proteins,Serum Globulins |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | Spike glycoprotein |
Brand Name | Bebtelovimab |
Company | Eli Lilly and Company |
Brand Description | Eli Lilly and Company |
Prescribed For | Injection, solution |
Chemical Name | 87.5 mg/1mL |
Formulation | NA |
Physical Appearance | fever difficulty breathing low oxygen level in your blood chills tiredness fast or slow heart rate chest discomfort or pain weakness confusion nausea headache shortness of breath low or high blood pressure wheezing swelling of your lips, face, or throat rash including hives itching muscle aches dizziness feeling faint, and sweating. |
Route of Administration | Bebtelovimab has not undergone the same type of review as an FDA-approved product. In issuing an EUA under the COVID-19 public health emergency, the FDA has determined, among other things, that based on the total amount of scientific evidence available, including data from adequate and well-controlled clinical trials, it is reasonable to believe that the product may be effective for diagnosing, treating, or preventing COVID-19, or a serious or life-threatening disease or condition caused by COVID-19; that the known and potential benefits of the product, when used to diagnose, treat, or prevent such disease or condition, outweigh the known and potential risks of such product; and that there are no adequate, approved and available alternatives. |
Recommended Dosage | Bebtelovimab is an investigational medicine used under Emergency Use Authorization (EUA) for the treatment of mild-to-moderate coronavirus disease 2019 (COVID-19) in adults and children (12 years of age and older weighing at least 88 pounds [40 kg]) |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | Link |
Remarks | NA |