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Metyrosine | CAS No: 672-87-7 | GMP-certified suppliers
A medication that manages pheochromocytoma by reducing catecholamine production, aiding preoperative preparation, and treating patients when surgery is contraindicated or for chronic malignant cases.
Therapeutic categories
Primary indications
- 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
Product Snapshot
- Metyrosine is an oral small molecule available in capsule formulation
- It is primarily indicated for the management and preoperative preparation of patients with pheochromocytoma, including cases where surgery is contraindicated
- The product is approved for use in the US market
Clinical Overview
Pharmacologically, metyrosine acts by inhibiting the enzyme tyrosine 3-monooxygenase (tyrosine hydroxylase), which catalyzes the rate-limiting initial step in catecholamine biosynthesis—the conversion of tyrosine to dihydroxyphenylalanine (DOPA). By blocking this enzymatic step, metyrosine effectively reduces the endogenous synthesis of dopamine, norepinephrine, and epinephrine. Clinical administration of metyrosine at doses ranging from one to four grams per day has demonstrated reductions in total catecholamine production by 35 to 80 percent, evidenced by decreased urinary excretion of catecholamines and their metabolites such as metanephrine and vanillylmandelic acid. The maximum biochemical effect is typically observed within two to three days following treatment initiation, with a reversal of effects noted within three to four days after cessation of therapy.
Clinically, this biochemical suppression translates to a reduction in the frequency and severity of hypertensive crises commonly seen in pheochromocytoma patients, accompanied by symptomatic relief of headache, nausea, sweating, and tachycardia. Blood pressure decreases progressively during the initial days of treatment and returns towards baseline after withdrawal of the drug.
From a safety perspective, careful titration and monitoring are necessary due to the potential for hypotension and related adverse effects associated with catecholamine depletion. Metyrosine is classified under enzyme inhibitors and antihypertensive agents, and is an established pharmaceutical intervention approved in relevant therapeutic contexts.
For API procurement and formulation development, high purity standards must be adhered to, considering the drug’s enzymatic target and its narrow therapeutic index. Suppliers should provide detailed certificates of analysis confirming identity, potency, and absence of impurities or degradation products that could compromise efficacy or safety. Stability profiles and compliance with pharmacopeial monographs relevant to metyrosine should also be verified to ensure consistent clinical performance.
Identification & chemistry
| Generic name | Metyrosine |
|---|---|
| Molecule type | Small molecule |
| CAS | 672-87-7 |
| UNII | DOQ0J0TPF7 |
| DrugBank ID | DB00765 |
Pharmacology
| Summary | Metyrosine acts as an inhibitor of tyrosine hydroxylase (tyrosine 3-monooxygenase), the rate-limiting enzyme in catecholamine biosynthesis, reducing the conversion of tyrosine to dihydroxyphenylalanine (DOPA). This inhibition leads to decreased synthesis and endogenous levels of catecholamines, including dopamine, norepinephrine, and epinephrine. The drug is primarily used to manage catecholamine excess in pheochromocytoma by lowering catecholamine biosynthesis and associated hemodynamic effects. |
|---|---|
| Mechanism of action | 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. |
| Pharmacodynamics | 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. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Tyrosine 3-monooxygenase | Humans | binder |
ADME / PK
| Absorption | Well absorbed from the gastrointestinal tract. |
|---|---|
| Half-life | 3.4 to 3.7 hours |
| Metabolism | Little biotransformation, with catechol metabolites accounting for less than 1% of the administered dose. |
| Route of elimination | Because the first step is also the rate-limiting step, blockade of tyrosine hydroxylase activity results in decreased endogenous levels of catecholamines, usually measured as decreased urinary excretion of catecholamines and their metabolites. |
Formulation & handling
- Metyrosine is administered orally in capsule form and is classified as a small molecule with phenylpropanoic acid structure.
- It exhibits moderate water solubility (2.48 g/L) and a low logP (-1.1), indicating hydrophilic properties suitable for oral formulations.
- Avoid co-administration with alcohol due to increased sedative and CNS depressant effects; no peptide or biologic stability concerns reported.
Regulatory status
| Lifecycle | The API is currently marketed in the US with patent protection active until , after which generic competition is expected to increase, indicating a transition toward market maturity. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Metyrosine is manufactured primarily by a single originator company, Aton Pharma Inc., with packaging support from multiple entities including Aton Pharma Inc., Draxis Specialty Pharmaceuticals Inc., and Merck & Co. The branded products are available mainly in the US market. Given the current limited manufacturer base and market presence, patent expiry status would need to be confirmed to assess potential for generic competition. |
|---|
Safety
| Toxicity | Signs of metyrosine overdosage include those central nervous system effects observed in some patients even at low dosages. At doses exceeding 2000 mg/day, some degree of sedation or feeling of fatigue may persist. Doses of 2000-4000 mg/day can result in anxiety or agitated depression, neuromuscular effects (including fine tremor of the hands, gross tremor of the trunk, tightening of the jaw with trismus), diarrhea, and decreased salivation with dry mouth. The acute toxicity of metyrosine was 442 mg/kg and 752 mg/kg in the female mouse and rat respectively. |
|---|
- Exposure to metyrosine may induce central nervous system effects such as sedation, fatigue, anxiety, or agitation at elevated doses
- Neuromuscular symptoms including fine hand tremors, trunk tremors, and jaw tightness with trismus have been observed with doses above 2000 mg/day
- Acute toxicity values are reported at 442 mg/kg (mouse) and 752 mg/kg (rat), indicating species-specific sensitivity considerations
Metyrosine is a type of Adrenergic agents
Adrenergic agents are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that target the adrenergic system in the body. This system is responsible for regulating various physiological responses, including heart rate, blood pressure, and smooth muscle contraction.
Adrenergic agents can be further divided into two main groups: adrenergic agonists and adrenergic antagonists. Adrenergic agonists stimulate the adrenergic receptors, leading to an increase in sympathetic nervous system activity. This can result in effects such as vasoconstriction, bronchodilation, and increased heart rate. Adrenergic agonists are commonly used in the treatment of conditions such as asthma, hypotension, and cardiac arrest.
On the other hand, adrenergic antagonists block the adrenergic receptors, thereby inhibiting the effects of sympathetic nervous system activation. These agents are often employed to lower blood pressure, treat certain heart conditions, and manage symptoms associated with conditions like benign prostatic hyperplasia. Adrenergic antagonists can be further classified into alpha-adrenergic antagonists and beta-adrenergic antagonists, based on their selectivity for different adrenergic receptor subtypes.
Pharmaceutical companies extensively utilize adrenergic agents as key components in the development of various medications. Adrenergic APIs offer targeted effects on the adrenergic system, allowing for precise modulation of physiological responses. The understanding of adrenergic agents and their mechanisms of action is vital for the design and optimization of drugs used in the treatment of numerous medical conditions. Researchers and scientists continue to explore and innovate within this subcategory to develop new adrenergic agents with enhanced efficacy and fewer side effects, ultimately improving patient outcomes.
Metyrosine (Adrenergic agents), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Metyrosine API manufacturers & distributors
Compare qualified Metyrosine API suppliers worldwide. We currently have 3 companies offering Metyrosine API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Biophore India | Producer | India | India | CoA, USDMF | 46 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Patheon | Producer | Austria | Austria | CoA, USDMF | 6 products |
When sending a request, specify which Metyrosine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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