Repositioning Candidate Details
| Candidate ID: | R0271 |
| Source ID: | DB00765 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Metyrosine |
| Synonyms: | (-)-alpha-Methyl-L-tyrosine; (–)-α-methyl-L-tyrosine; (S)-alpha-Methyltyrosine; Methyltyrosine; Metirosine; Metyrosine; α-methyl-L-p-tyrosine; α-methyl-p-tyrosine; α-methyl-para-tyrosine; α-MPT |
| Molecular Formula: | C10H13NO3 |
| SMILES: | C[C@](N)(CC1=CC=C(O)C=C1)C(O)=O |
| Structure: |
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| DrugBank Description: | An inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with pheochromocytoma. (Martindale, The Extra Pharmacopoeia, 30th ed) |
| CAS Number: | 672-87-7 |
| Molecular Weight: | 195.2151 |
| DrugBank Indication: | For use in the treatment of patients with pheochromocytoma, for preoperative preparation of patients for surgery, management of patients when surgery is contraindicated, and chronic treatment of patients with malignant pheochromocytoma. |
| DrugBank Pharmacology: | In patients with pheochromocytoma, who produce excessive amounts of norepinephrine and epinephrine, administration of one to four grams of metyrosine per day has reduced catecholamine biosynthesis from about 35 to 80 percent as measured by the total excretion of catecholamines and their metabolites (metanephrine and vanillylmandelic acid). The maximum biochemical effect usually occurs within two to three days, and the urinary concentration of catecholamines and their metabolites usually returns to pretreatment levels within three to four days after metyrosine is discontinued. Most patients with pheochromocytoma treated with metyrosine experience decreased frequency and severity of hypertensive attacks with their associated headache, nausea, sweating, and tachycardia. In patients who respond, blood pressure decreases progressively during the first two days of therapy with metyrosine; after withdrawal, blood pressure usually increases gradually to pretreatment values within two to three days. |
| DrugBank MoA: | Metyrosine inhibits tyrosine hydroxylase, which catalyzes the first transformation in catecholamine biosynthesis, i.e., the conversion of tyrosine to dihydroxyphenylalanine (DOPA). Because the first step is also the rate-limiting step, blockade of tyrosine hydroxylase activity results in decreased endogenous levels of catecholamines and their synthesis. This consequently, depletes the levels of the catecholamines dopamine, adrenaline and noradrenaline in the body,usually measured as decreased urinary excretion of catecholamines and their metabolites. One main end result of the catecholamine depletion is a decrease in blood presure. |
| Targets: | Tyrosine 3-monooxygenase binder |
| Inclusion Criteria: | Therapeutic strategy associated |
