he linker payload, mc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) was conjugated to the A1 anti-5T4 monoclonal antibody through a cysteine residue at a ratio of approximately 4 compound moieties per antibody molecule.
 |
Source | Ther Adv Respir Dis (2018). Figure 3. MMAD |
| Method | Influence of inhalation duration on lung deposition | |
| Cell Lines | mice | |
| Concentrations | 1.5, 3.0, 4.5 μM | |
| Incubation Time | - | |
| Results | Other studies also suggest that particles with an MMAD in the range 1.5–4.5 μm can achieve good lung deposition, consistent with these findings. |
| Molecular Weight | 771.06 |
| Formula | C41H66N6O6S |
| CAS Number | 203849-91-6 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
[1] Paul Zarogoulidis, et al. Modification Tadalafil and Macitentan tablets to aerosol
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