==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

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Primary information
ThPP IDTh1138
Therapeutic Peptide/Protein NameRaxibacumab
SequenceN.A. view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight142844.5367
Chemical FormulaC6320H9794N1702O1998S42
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeElimnation half life-IM dose- 15-19 days; IV dose-16-19 days
DescriptionRecombinant (murine cell line derived), human IgG1 monoclonal antibody that binds the protective antigen (PA) component of B. anthracis toxin. FDA approved on December 14, 2012.
Indication/DiseaseRaxibacumab is indicated for the treatment of adult and pediatric patients with inhalational anthrax due to Bacillus anthracis in combination with appropriate antibacterial drugs, and for prophylaxis of inhalational anthrax when alternative therapies are not available or are not appropriate.
PharmacodynamicsN.A.
Mechanism of ActionRaxibacumab is a monoclonal antibody that binds free PA with an affinity equilibrium dissociation constant (Kd) of 2.78 ± 0.9 nM. Raxibacumab inhibits the binding of PA to its cellular receptors, preventing the intracellular entry of the anthrax lethal factor and edema factor, the enzymatic toxin components responsible for the pathogenic effects of anthrax toxin. It does not have direct antibacterial activity.
ToxicityThe most frequently reported adverse reactions were rash, pain in extremity, pruritus, and somnolence.
MetabolismN.A.
AbsorptionRaxibacumab does not cross the blood-brain-barrier. When a single IV dose of 40 mg/kg was administered to healthy, male and female human subjects, the pharmacokinetic parameters are as follows: Cmax = 1020.3 ± 140.6 mcg/mL; AUCinf = 15845.8 ± 4333.5 mcg·day/mL.; Bioavailability is also dependent on site of injection. When administered to the vastus lateralis, the bioavailability is 71-85%. When administered to the gluteus maximus, the bioavailability is 50-54%.
Volume of DistributionSteady state volume of distribution exceeded plasma volume. This suggests that there is some distribution into the tissues.
ClearanceClearance values were much smaller than the glomerular filtration rate indicating that there is virtually no renal clearance of raxibacumab.
CategoriesAnti-Infective Agents and Monoclonal antibodies
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetProtective antigen
Information of corresponding available drug in the market
Brand NameRAXIBACUMAB
CompanyGSK
Brand DiscriptionRaxibacumab is a human IgG1λ monoclonal antibody that binds the PA component of B. anthracis toxin. Raxibacumab has a molecular weight of approximately 146 kilodaltons. Raxibacumab is produced by recombinant DNA technology in a murine cell expression system.
Prescribed forRaxibacumab is indicated for the treatment of adult and pediatric patients with inhalational anthrax due to Bacillus anthracis in combination with appropriate antibacterial drugs, and for prophylaxis of inhalational anthrax when alternative therapies are not available or are not appropriate
Chemical NameN.A.
FormulationSingle-use vial contains 1700 mg/34 mL (50 mg/mL) raxibacumab solution.
Physcial AppearnceRaxibacumab is supplied as a sterile, liquid formulation in single-dose vials for Intravenous infusion. Each vial contains 50 mg/mL raxibacumab in citric acid (0.13 mg/mL), glycine (18 mg/mL), polysorbate 80 [0.2 mg/mL (w/v)], sodium citrate (2.8 mg/mL), and sucrose (10 mg/mL), with a pH of 6.5. Eac
Route of AdministrationN.A.
Recommended DosagePremedicate with diphenhydramine. Dilute and administer as an Intravenous infusion over 2 hours and 15 minutes. Adults: 40 mg/kg raxibacumab. Pediatrics greater than 50 kg: 40 mg/kg raxibacumab. Pediatrics greater than 15 kg to 50 kg: 60 mg/kg raxibacumab. Pediatrics 15 kg or less: 80 mg/kg raxibacumab.
ContraindicationThere have been no studies of raxibacumab in the pediatric population. Dosing in pediatric patients was derived using a population PK approach. Raxibacumab does not cross the blood-brain barrier and does not prevent or treat meningitis. Raxibacumab should be used in combination with appropriate antibacterial drugs. Nursing Mothers: Caution should be exercised when administered to a nursing woman. Pediatric Use: Safety and effectiveness in children <16 years of age not studied.
Side EffectsInfusion reactions may occur. Premedicate with diphenhydramine. Slow or interrupt infusion and administer treatment based on severity of the reaction. Common adverse reactions in healthy adult subjects (≥1.5%) were: rash, pain in extremity, pruritus, and somnolence.
Useful Linkhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2012/125349s000lbl.pdf, http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm332341.htm,
PubMed ID25487792, 24812521, 23545582, 23344456, 20068396
3-D StructureN.A.