Raxibacumab

Thuốc trị ký sinh trùng, chống nhiễm khuẩn

Thuốc Gốc

Biotech

CAS: 565451-13-0

CTHH: C₆₃₂₀H₉₇₉₄N₁₇₀₂O₁₉₉₈S₄₂

PTK: 142844.5367 Daltons

Raxibacumab is a human IgG1λ monoclonal antibody that binds the protective antigen (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. FDA approved on December 14, 2012.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₆₃₂₀H₉₇₉₄N₁₇₀₂O₁₉₉₈S₄₂

Phân tử khối

142844.5367 Daltons

Điểm đẳng điện tích

9.0

Cơ Chế Tác Dụng : Raxibacumab is a human IgG1λ monoclonal antibody that binds the protective antigen (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. FDA approved on December 14, 2012. Raxibacumab 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.

Dược Động Học :

▧ Absorption :
Raxibacumab 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 Distribution :
Steady state volume of distribution exceeded plasma volume. This suggests that there is some distribution into the tissues.
▧ Half Life :
Mean terminal elimination half-lives of raxibacumab are as follows: IM dose = 15-19 days; IV dose = 16-19 days
▧ Clearance :
Clearance values were much smaller than the glomerular filtration rate indicating that there is virtually no renal clearance of raxibacumab.

Độc Tính : The most frequently reported adverse reactions were rash, pain in extremity, pruritus, and somnolence.

Chỉ Định : Raxibacumab 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.

Liều Lượng & Cách Dùng : Injection - Intravenous - 1700MG/34ML

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Human Genome Sciences Inc.

Sản phẩm biệt dược : Abthrax

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB08902

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D05706

Wikipedia

http://en.wikipedia.org/wiki/Raxibacumab

Drugs.com

http://www.drugs.com/raxibacumab.html

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