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PubChem
| Name: | Mycophenolic Acid |
|---|---|
| PubChem Compound ID: | 4272 |
| Description: | An antibiotic substance derived from Penicillium stoloniferum, and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase. Mycophenolic acid is important because of its selective effects on the immune system. It prevents the proliferation of T-cells, lymphocytes, and the formation of antibodies from B-cells. It also may inhibit recruitment of leukocytes to inflammatory sites. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1301) |
| Molecular formula: | C17H20O6 |
| Molecular weight: | 320.337 g/mol |
| Synonyms: |
Spectrum4_000890; DivK1c_000146; Spectrum3_000797; Spectrum2_000892; KBio2_002535; KBio3_001754; KBio1_000146; KBio2_005103; Spectrum_001978; SPBio_000704.
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DrugBank
Identification
| Name: | Mycophenolic Acid |
|---|---|
| Name (isomeric): | DB01024 |
| Drug Type: | small molecule |
| Description: | An antibiotic substance derived from Penicillium stoloniferum, and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase. Mycophenolic acid is important because of its selective effects on the immune system. It prevents the proliferation of T-cells, lymphocytes, and the formation of antibodies from B-cells. It also may inhibit recruitment of leukocytes to inflammatory sites. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1301) |
| Synonyms: |
Mycophenoic acid
|
| Brand: | Myfortic, Melbex |
| Category: | Enzyme Inhibitors, Antibiotics, Antineoplastic |
| CAS number: | 24280-93-1 |
Pharmacology
| Indication: | For the prophylaxis of organ rejection in patients receiving allogeneic renal transplants, administered in combination with cyclosporine and corticosteroids. |
|---|---|
| Pharmacology: |
Mycophenolic acid is an antibiotic substance derived from Penicillium stoloniferum. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase. Mycophenolic acid is important because of its selective effects on the immune system. It prevents the proliferation of T-cells, lymphocytes, ...
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| Mechanism of Action: |
Mycophenolic acid is a potent, selective, uncompetitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation into DNA. Because T- and B-lymphocytes are critically dependent for their proliferation on de novo synthesis of purines, ...
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| Absorption: | Bioavailability following oral administration of Myfortic delayed-release tablet ranges from 70-95% |
| Protein binding: | >98% |
| Biotransformation: | Mycophenolic acid is metabolized mainly by glucuronyl transferase to glucuronidated metabolites, predominantly the phenolic glucuronide, mycophenolic acid glucuronide (MPAG). MPAG does not manifest pharmacological activity. The acyl glucuronide minor metabolite has pharmacological activity similar to mycophenolic acid. The AUC ratio of Mycophenolic acid:MPAG:acyl glucuronide is approximately 1:24:0.28 at steady state. |
| Half Life: | The mean elimination half-life for mycophenolic acid ranges from 8-16 hours, while that of the MPAG metabolite ranges from 13-17 hours. |
| Clearance: | 140 +/- 30 mL/min [Stable renal transplant patients] |
| Toxicity: | Oral (LD50): Acute: 352 mg/kg [Rat], 1000 mg/kg [Mouse], and >6000 mg/kg [Rabbit]. Possible signs and symptoms of acute overdose could include the following: hematological abnormalities such as leukopenia and neutropenia, and gastrointestinal symptoms such as abdominal pain, diarrhea, nausea and vomiting, and dyspepsia. |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
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