Omalizumab 是一种针对人免疫球蛋白 E (IgE) 的重组人源化单克隆抗体，KD 为 0.393 nM。
Omalizumab is a recombinant DNA-derived humanized IgG1k monoclonal antibody that specifically binds to free human immunoglobulin E (IgE) in the blood and interstitial fluid and to membrane-bound form of IgE (mIgE) on the surface of mIgE-expressing B lymphocytes. Omalizumab inhibits the binding of IgE to FcεRI on mast cells and basophils by binding to an antigenic epitope on IgE that overlaps with the site to which FcεRI binds. When IgE is bound to the receptor, the antigenic epitope on IgE to which omalizumab binds is sterically hindered by the receptor and is not accessible to omalizumab binding, thus averting the anaphylactic effects presumably unavoidable with an ordinary anti-IgE antibody . Furthermore, although the peptide elements on IgE involved in binding to low affinity IgE receptor (FcεRII) on many cell types are different from the peptide elements involved in binding to FcεRI, omalizumab, by steric hindrance, also prevents binding of IgE to FcεRII.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
|
Species |
Mouse |
Rat |
Rabbit |
Guinea pig |
Hamster |
Dog |
|
Weight (kg) |
0.02 |
0.15 |
1.8 |
0.4 |
0.08 |
10 |
|
Body Surface Area (m2) |
0.007 |
0.025 |
0.15 |
0.05 |
0.02 |
0.5 |
|
Km factor |
3 |
6 |
12 |
8 |
5 |
20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by?Animal B Km/Animal A Km
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
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