Mycophenolic acid (mycophenolate) is an immunosuppressant agent used to prevent rejection in organ transplantation. Mycophenolic acid (mycophenolate) is derived from the fungus Penicillium stoloniferum. Mycophenolate mofetil is metabolised in the liver to the active moiety mycophenolic acid. Mycophenolic acid (mycophenolate) inhibits inosine monophosphate dehydrogenase, the enzyme that controls the rate of synthesis of guanine monophosphate in the de novo pathway of purine synthesis used in the proliferation of B and T lymphocytes. Mycophenolic acid (mycophenolate) is potent and can be used in place of the older anti-proliferative azathioprine. Mycophenolic acid (mycophenolate) is usually used as part of a three-compound regimen of immunosuppressants, also including a calcineurin inhibitor (ciclosporin or tacrolimus) and prednisolone.
| Molecular Weight | 320.34 |
| Formula | C17H20O6 |
| CAS Number | 24280-93-1 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| 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.
[3] Agnieszka Siebert, et al. New Analogues of Mycophenolic Acid
[4] A Dasgupta. Therapeutic Drug Monitoring of Mycophenolic Acid
[5] Sarah J Strathie Page, et al. Mycophenolic acid in dermatology a century after its discovery
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