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Brexpiprazole | CAS No: 913611-97-9 | GMP-certified suppliers
A medication that supports major depressive disorder treatment as adjunct therapy, manages schizophrenia, and addresses agitation in Alzheimer’s dementia for broad psychiatric and neurobehavioral care needs.
Therapeutic categories
Primary indications
- Brexpiprazole is indicated as adjunctive therapy to antidepressants for the treatment of major depressive disorder in adults
- It is also indicated for the treatment of schizophrenia in patients 13 years of age and older
- Brexpiprazole is also indicated for the treatment of agitation associated with dementia due to Alzheimer’s disease
Product Snapshot
- Brexpiprazole is an oral small‑molecule antipsychotic supplied as film‑coated tablets
- Its principal uses include adjunctive treatment of major depressive disorder, management of schizophrenia, and treatment of agitation associated with Alzheimer’s dementia
- It is approved in the US, Canada, and the EU, with some investigational programs ongoing
Clinical Overview
Clinically, brexpiprazole is indicated as adjunctive therapy to antidepressants for major depressive disorder in adults. It is also approved for the treatment of schizophrenia in patients 13 years and older. Additional approval covers the management of agitation associated with dementia due to Alzheimer’s disease, but it is not intended for as‑needed administration in this setting.
Brexpiprazole modulates neurotransmission through partial agonism at 5‑HT1A, D2, and D3 receptors and antagonism at 5‑HT2A, 5‑HT2B, 5‑HT7, and multiple alpha‑adrenergic receptors. It also shows affinity for histamine H1 and muscarinic M1 receptors. These combined actions influence dopaminergic and serotonergic pathways relevant to mood regulation, cognition, and psychosis. Subnanomolar affinity at key serotonergic and dopaminergic receptors supports its role in stabilizing neurotransmitter activity under varying endogenous dopamine levels.
Absorption, distribution, metabolism, and excretion characteristics include metabolism primarily via CYP3A4 and CYP2D6 pathways, consistent with its classification as a substrate of these enzymes. This underlines the relevance of drug‑drug interaction assessment, particularly with strong inhibitors or inducers of these pathways.
Safety considerations include dose‑dependent risks of akathisia, somnolence, metabolic changes, and orthostatic hypotension, reflecting its receptor interaction profile. Compared with aripiprazole, lower D2 intrinsic activity is associated with reduced likelihood of extrapyramidal symptoms, though susceptibility varies clinically.
Brexpiprazole is marketed in several regions under names such as Rexulti. For API procurement, quality considerations include confirmation of stereochemical integrity, control of related impurities, and verification of compliance with pharmacopeial or regional regulatory specifications.
Identification & chemistry
| Generic name | Brexpiprazole |
|---|---|
| Molecule type | Small molecule |
| CAS | 913611-97-9 |
| UNII | 2J3YBM1K8C |
| DrugBank ID | DB09128 |
Pharmacology
| Summary | Brexpiprazole is an atypical antipsychotic that modulates dopaminergic and serotonergic signaling through partial agonism at D2 and 5‑HT1A receptors and antagonism at 5‑HT2A receptors. Its activity across additional serotonin, dopamine, and adrenergic receptors contributes to effects on mood, cognition, and behavioral symptoms in psychiatric and neurocognitive disorders. The compound’s broad monoaminergic receptor profile underlies its role in conditions such as schizophrenia, major depressive disorder, and agitation associated with Alzheimer’s disease. |
|---|---|
| Mechanism of action | Although the exact mechanism of action of brexpiprazole in psychiatric disorders has not been fully elucidated, the efficacy of brexpiprazole may be attributed to combined partial agonist activity at 5-HT<sub>1A</sub> and dopamine D2 receptors, and antagonist activity at 5-HT<sub>2A</sub> receptors. Brexpiprazole binds to these receptors with subnanomolar affinities.These therapeutic targets have been implicated in psychiatric conditions such as schizophrenia and depression. Partial D2 receptor agonism allows the drug to stimulate D2 receptors under low dopamine conditions, while attenuating their activation when dopamine levels are high. Partial agonism at 5-HT<sub>1A</sub> receptors may be tied to improved memory function and cognitive performance. Antagonism at α-adrenergic receptors has also been implicated in schizophrenia and depression. |
| Pharmacodynamics | Brexpiprazole is an atypical antipsychotic agent used to ameliorate the symptoms of psychiatric conditions, such as cognitive deficits and affective symptoms.Brexpiprazole has affinity (expressed as Ki) for multiple monoaminergic receptors including serotonin 5-HT<sub>1A</sub> (0.12 nM), 5-HT<sub>2A</sub> (0.47 nM), 5-HT<sub>2B</sub> (1.9 nM), 5-HT<sub>7</sub> (3.7 nM), dopamine D2 (0.30 nM), D3 (1.1 nM), and noradrenergic α<sub>1A</sub> (3.8 nM), α<sub>1B</sub> (0.17 nM), α<sub>1D</sub> (2.6 nM), and α<sub>2C</sub> (0.59 nM) receptors. Brexpiprazole acts as a partial agonist at the 5-HT<sub>1A</sub>, D2, and D3 receptors and as an antagonist at 5-HT<sub>2A</sub>, 5-HT<sub>2B</sub>, 5-HT<sub>7</sub>, α<sub>1A</sub>, α<sub>1B</sub>, α<sub>1D</sub>, and α<sub>2C</sub> receptors. Brexpiprazole also exhibits affinity for histamine H1 receptor (19 nM) and for muscarinic M1 receptor (67% inhibition at 10 µM). |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 1A | Humans | partial agonist |
| Dopamine D2 receptor | Humans | partial agonist |
| Dopamine D3 receptor | Humans | partial agonist |
ADME / PK
| Absorption | After a single-dose administration, the T<sub>max</sub> was four hours and the absolute oral bioavailability was 95%. Brexpiprazole steady-state concentrations were attained within 10 to 12 days of dosing. After single and multiple once-daily dose administration, the C<sub>max</sub> and AUC increased dose-proportionally. A high-fat meal did not significantly affect the C<sub>max</sub> or AUC of brexpiprazole. |
|---|---|
| Half-life | After multiple once-daily administrations, the terminal elimination half-lives of brexpiprazole and its major metabolite, DM-3411, were 91 hours and 86 hours, respectively. |
| Protein binding | _In vitro_, brexpiprazole was 99% bound to plasma proteins, mainly serum albumin and α1-acid glycoprotein. |
| Metabolism | According to _in vitro_ studies, brexpiprazole is mainly metabolized by CYP3A4 and CYP2D6. Brexpiprazole and its major metabolite, DM-3411, were the predominant drug moieties in the systemic circulation following single and multiple dose administration. At steady-state, DM-3411 represented 23% to 48% of brexpiprazole exposure (AUC) in plasma. DM-3411 is considered not to be pharmacologically active. |
| Route of elimination | Following a single oral dose of radiolabeled brexpiprazole, approximately 25% and 46% of radioactivity was recovered in the urine and feces, respectively. Less than 1% of unchanged brexpiprazole was excreted in the urine, and approximately 14% of the oral dose was recovered unchanged in the feces. |
| Volume of distribution | The volume of distribution of brexpiprazole following intravenous administration is 1.56 ± 0.42 L/kg, indicating extravascular distribution. |
| Clearance | Apparent oral clearance of brexpiprazole after once-daily administration is 19.8 (±11.4) mL/h/kg. |
Formulation & handling
- Oral small‑molecule API with very low aqueous solubility, often requiring solubility‑enhancing approaches for tablet development.
- High lipophilicity (LogP ~4.6) may influence excipient choice for dissolution performance and uniformity in solid oral dosage forms.
- Food has minimal impact on exposure, allowing flexible administration, but avoid coformulation with strong CYP3A inducers such as St. John’s wort extracts.
Regulatory status
| Lifecycle | Most U.S. patents for the API expire between 2026 and 2027, with one later‑expiring patent extending protection to 2032, indicating a staggered loss of exclusivity. Across the US, Canada, and the EU, the market is moving toward mid‑cycle maturity with potential for increased generic entry as early patents expire. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Brexpiprazole appears to be supplied primarily by a single originator, with branded products marketed in the US, Canada, and the EU, indicating a broad commercial footprint across major regulated markets. Most listed US patents expire between 2026 and 2027, but one extends to 2032, suggesting that full generic entry may be staggered and limited until the later‑expiring protection lapses. This creates a landscape of established originator supply with only early indications of future generic competition. |
|---|
Safety
| Toxicity | There is limited information regarding acute toxicity and human overdosage with brexpiprazole. Management of overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and management of symptoms. Close medical supervision and monitoring should continue until the patient recovers. Oral activated charcoal and sorbitol (50 g/240 mL), administered one hour after ingesting oral brexpiprazole, decreased brexpiprazole C<sub>max</sub> and area under the curve (AUC) by approximately 5% to 23% and 31% to 39% respectively; however, there is insufficient information available on the therapeutic potential of activated charcoal in treating an overdose with brexpiprazole. There is no information on the effect of hemodialysis in treating an overdose with brexpiprazole; hemodialysis is unlikely to be useful because brexpiprazole is highly bound to plasma proteins. |
|---|
- Limited acute toxicity data
- High plasma‑protein binding suggests low dialyzability and minimal benefit from hemodialysis in overdose scenarios
- Charcoal co‑administration can reduce exposure (Cmax and AUC), though its therapeutic relevance in overdose remains unconfirmed
Brexpiprazole 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.
Brexpiprazole (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.
Brexpiprazole API manufacturers & distributors
Compare qualified Brexpiprazole API suppliers worldwide. We currently have 17 companies offering Brexpiprazole API, with manufacturing taking place in 7 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, GMP, USDMF | 229 products |
| Cambrex | Producer | Italy | United States | CoA, GMP | 104 products |
| Chongqing Jooe Co., Ltd. | Producer | China | China | CoA, FDA, GMP, MSDS | 10 products |
| Dr. Sahu's Laboratories | Producer | India | India | CoA, GMP | 70 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Honour Lab | Producer | India | India | CoA, USDMF | 30 products |
| Jubilant Pharmova | Producer | India | India | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF | 52 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Morepen Laboratories Ltd. | Producer | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 22 products |
| MSN Life Sciences | Producer | India | India | CoA, USDMF | 46 products |
| PLIVA | Producer | Czech Republic | Croatia | CoA, GMP | 31 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, MSDS, USDMF | 64 products |
| Quimica Sintetica | Producer | Spain | Spain | CoA, GMP | 51 products |
| Raks Pharma | Producer | India | India | CoA, USDMF | 58 products |
| Senova Technology Co., Lt... | Producer | China | China | BSE/TSE, CoA, ISO9001, MSDS | 157 products |
| Sichuan Qingmu Pharmaceut... | Producer | China | China | CoA | 31 products |
| Tianjin Pharmacn Medical ... | Producer | China | China | CoA, GMP | 66 products |
When sending a request, specify which Brexpiprazole 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.).
Use the list above to find high-quality Brexpiprazole API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
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