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Iloperidone | CAS No: 133454-47-4 | GMP-certified suppliers
A medication that treats acute schizophrenia by addressing psychotic symptoms through antipsychotic effects with considerations for cardiac safety and metabolic monitoring.
Therapeutic categories
Primary indications
- Treatment of acute schizophrenia
Product Snapshot
- Iloperidone is an oral small molecule formulation available primarily as tablets and kits
- It is indicated for the treatment of acute schizophrenia
- The product is approved for use in the US market
Clinical Overview
Pharmacodynamically, iloperidone exhibits high affinity binding and receptor occupancy at dopamine D2 receptors localized primarily in the caudate nucleus and putamen, regions implicated in the pathophysiology of schizophrenia. The drug also demonstrates high affinity for serotonin 5-HT2A and dopamine D3 receptors, and significant binding to α-adrenergic receptors, which may contribute to its observed effects on cognition. Moderate affinity is observed at dopamine D4, serotonin 5-HT6, 5-HT7, and norepinephrine α1 receptors, while weak binding occurs at serotonin 5-HT1A, dopamine D1, and histamine H1 receptors.
Iloperidone’s mechanism of action primarily involves antagonism of dopamine D2 and serotonin 5-HT2A receptors, which underlies its neuroleptic properties and efficacy in symptom control. The compound belongs to the chemical class of alkyl-phenylketones, characterized by an aromatic ketone structure substituted with an alkyl and phenyl group.
Metabolically, iloperidone is a substrate of several cytochrome P450 enzymes including CYP2D6, CYP3A4, CYP3A5, and CYP2E1, which has implications for drug–drug interactions and variability in patient response. Key safety considerations include its classification among agents with a high risk of QTc interval prolongation, necessitating cardiac monitoring and caution in patients with known cardiac conduction abnormalities. Other observed adverse effects include potential for orthostatic hypotension due to α1-adrenergic antagonism, as well as metabolic effects such as hyperglycemia.
Notable brand names and usage contexts are primarily concentrated in the management of schizophrenia within adult populations in multiple global regions. Iloperidone’s role within second-generation antipsychotics contributes to its utilization in psychiatric practice focused on mitigating both positive and negative symptoms.
For API procurement, iloperidone demands stringent quality control to ensure purity, polymorphic consistency, and absence of contaminants, given its narrow therapeutic index and metabolic sensitivities. Suppliers should demonstrate compliance with current good manufacturing practices (cGMP) and provide comprehensive certificate of analysis data to support regulatory submissions and ensure batch-to-batch reproducibility.
Identification & chemistry
| Generic name | Iloperidone |
|---|---|
| Molecule type | Small molecule |
| CAS | 133454-47-4 |
| UNII | VPO7KJ050N |
| DrugBank ID | DB04946 |
Pharmacology
| Summary | Iloperidone is a neuroleptic agent primarily acting as an antagonist at dopamine D2 and serotonin 5-HT2A receptors, targeting dopaminergic and serotonergic pathways implicated in schizophrenia. It exhibits high affinity for dopamine D2 receptors in the striatum, as well as α-adrenergic receptors, contributing to its pharmacodynamic effects. Additional moderate to weak binding affinities include dopamine D3/D4, serotonin 5-HT6/7, and histamine H1 receptors. |
|---|---|
| Mechanism of action | Iloperidone is a dopamine D2 and 5-HT2A receptor antagonist and acts as a neuroleptic agent. |
| Pharmacodynamics | Iloperidone shows high affinity and maximal receptor occupancy for dopamine D2 receptors in the caudate nucleus and putamen of the brains of schizophrenic patients. The improvement in cognition is attributed to iloperidone's high affinity for α adrenergic receptors. Iloperidone also binds with high affinity to serotonin 5-HT2a and dopamine 3 receptors. Iloperidone binds with moderate affinity to dopamine D4, serotonin 5-HT6 and 5-HT7, and norepinephrine NEα1 receptors. Furthermore, iloperidone binds with weak affinity to serotonin 5-HT1A, dopamine D1, and histamine H1 receptors. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 2A | Humans | antagonist |
| Dopamine D2 receptor | Humans | antagonist |
| Dopamine D1 receptor | Humans | antagonist |
ADME / PK
| Absorption | Well absorbed from the GI tract and Cmax is reached within 2-4 hours. Steady-state concentration is achieved in 3-4 days post-administration of iloperidone. Relative bioavailability of the tablet formulation compared to oral solution is 96%. Accumulation occurs in a predictable fashion. |
|---|---|
| Half-life | The observed mean elimination half-lives for iloperidone, P88 and P95 in CYP2D6 extensive metabolizers (EM) are 18, 26 and 23 hours, respectively, and in poor metabolizers (PM) are 33, 37 and 31 hours, respectively. |
| Protein binding | 95% of iloperidone is bound to protein. Percent bound is not altered by renal or hepatic impairment or combination therapy with ketoconazole. |
| Metabolism | Iloperidone is hepatically metabolized by cytochrome enzymes which mediates O-dealkylation (CYP3A4), hydroxylation (CYP2D6), and decarboxylation/reduction processes. Metabolites formed are P89, P95, and P88. The minor metabolite is P89, whereas P95 and P88 are the major ones. The affinity of the iloperidone metabolite P88 is generally equal or less than that of the parent compound. In contrast, the metabolite P95 only shows affinity for 5-HT2A (Ki value of 3.91) and the NEα1A, NEα1B, NEα1D, and NEα2C receptors (Ki values of 4.7, 2.7, 8.8 and 4.7 nM respectively). |
| Route of elimination | Renal (in which <1% of iloperidone is excreted unchanged). |
| Volume of distribution | Apparent Vd = 1340-2800 L |
| Clearance | Apparent clearance (clearance/bioavilability) = 47-102 L/h. |
Formulation & handling
- Iloperidone is a small molecule API intended for oral administration, available mainly as tablets and kits.
- It exhibits low water solubility (0.03 g/L) and moderate lipophilicity (LogP 3.22), factors to consider in formulation design.
- Food intake, especially high-fat meals, may delay Tmax of iloperidone without affecting overall exposure (Cmax or AUC).
Regulatory status
| Lifecycle | The API is currently marketed in the United States with initial patents expired as of 2016 and several patents remaining active through 2031. This indicates ongoing market exclusivity with potential generic entry limited until the latest patent expirations. |
|---|
| Markets | US |
|---|
Supply Chain
| Supply chain summary | Iloperidone is primarily marketed in the US with multiple branded presentations under a single originator company. Several patents related to the drug remain active through 2031, indicating ongoing intellectual property protection and limited generic competition in the near term. The supply landscape is therefore characterized by a dominant originator presence and restricted generic entry based on current patent status. |
|---|
Safety
| Toxicity | Commonly observed adverse reactions (incidence ≥5% and two-fold greater than placebo) were: dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, and weight increased. |
|---|
- May cause central nervous system effects including dizziness, somnolence, and fatigue
- Associated with autonomic adverse reactions such as dry mouth, nasal congestion, orthostatic hypotension, and tachycardia
- Potential for weight increase observed
Iloperidone is a type of Atypical antipsychotics
Atypical antipsychotics belong to the subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various mental disorders, particularly schizophrenia and bipolar disorder. These medications are designed to alleviate the symptoms of psychosis by targeting specific neuroreceptors in the brain.
Unlike traditional antipsychotics, atypical antipsychotics exhibit a different pharmacological profile, providing a more favorable side effect profile and improved efficacy. These medications primarily act on dopamine and serotonin receptors, regulating the neurotransmitter levels in the brain to restore the chemical balance.
The mechanism of action of atypical antipsychotics involves blocking dopamine receptors, particularly D2 receptors, as well as modulating serotonin receptors, notably 5-HT2A receptors. By inhibiting excessive dopamine transmission and enhancing serotonin activity, atypical antipsychotics help reduce hallucinations, delusions, and other psychotic symptoms.
Some commonly used atypical antipsychotics include risperidone, olanzapine, quetiapine, and aripiprazole. These APIs are typically formulated into oral tablets or capsules for convenient administration.
Despite their effectiveness, atypical antipsychotics may have potential side effects such as weight gain, metabolic abnormalities, sedation, and extrapyramidal symptoms. Therefore, close monitoring and individualized treatment plans are essential to ensure optimal therapeutic outcomes.
In conclusion, atypical antipsychotics are a crucial subcategory of APIs used in the treatment of mental disorders. Their distinct pharmacological profile and mechanism of action make them valuable in managing psychosis while minimizing adverse effects.
Iloperidone (Atypical antipsychotics), classified under Antipsychotics
Antipsychotics belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category used to treat psychiatric disorders such as schizophrenia, bipolar disorder, and other related conditions. These medications play a crucial role in managing symptoms associated with psychosis, including hallucinations, delusions, and disorganized thinking.
Antipsychotics work by modulating the levels of neurotransmitters in the brain, particularly dopamine and serotonin. They can be categorized into two classes: first-generation (typical) antipsychotics and second-generation (atypical) antipsychotics. Typical antipsychotics primarily target dopamine receptors, while atypical antipsychotics also affect serotonin receptors.
The pharmaceutical API category of antipsychotics includes various well-known drugs, such as haloperidol, chlorpromazine, risperidone, quetiapine, and olanzapine. These APIs are often formulated into different dosage forms, including tablets, capsules, injections, and oral suspensions, to provide flexibility in administration and patient-specific needs.
Antipsychotics offer relief from psychotic symptoms by stabilizing the imbalanced neurotransmitter activity in the brain. However, they may also have certain side effects, such as sedation, weight gain, extrapyramidal symptoms, and metabolic disturbances. It is essential for healthcare professionals to carefully monitor patients receiving antipsychotic treatment to optimize therapeutic benefits while minimizing adverse effects.
In summary, antipsychotics are a vital category of pharmaceutical APIs used to manage psychiatric disorders by modulating neurotransmitter activity in the brain. Their effectiveness in treating psychosis has made them a cornerstone of mental health treatment, providing much-needed relief to individuals suffering from these conditions.
Iloperidone API manufacturers & distributors
Compare qualified Iloperidone API suppliers worldwide. We currently have 6 companies offering Iloperidone API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Formosa Labs | Producer | Taiwan | Taiwan | CoA, USDMF | 36 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| MSN Organics | Producer | India | India | CoA, USDMF | 21 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Procos | Producer | Italy | Italy | CoA, GMP, USDMF | 22 products |
| Symed Labs | Producer | India | India | CoA, USDMF | 28 products |
When sending a request, specify which Iloperidone 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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