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Donepezil | CAS No: 120014-06-4 | GMP-certified suppliers
A medication that provides symptomatic support for cognitive and functional decline in Alzheimer's‑related dementia and is also used in other major dementia disorders.
Therapeutic categories
Primary indications
- Donepezil, administered orallyor via transdermal delivery system,is indicated for the treatment of dementia of the Alzheimer's type
- It is also available as an extended-release capsule in combination with [memantine] for the treatment of moderate-to-severe dementia of the Alzheimer's type in patients previously stabilized on 10mg of donepezil hydrochloride once daily
- Off-label uses include the management of vascular dementia, Parkinson's Disease-associated dementia, and Lewy body dementia, amongst others
Product Snapshot
- Donepezil is an oral small‑molecule API available in multiple tablet and solution forms, as well as a transdermal patch
- It is used for Alzheimer’s-type dementia and is also utilized for related cognitive disorders in broader neurodegenerative settings
- It is approved in the US and Canada
Clinical Overview
Its pharmacological activity is based on selective and reversible inhibition of acetylcholinesterase, increasing acetylcholine concentrations at cholinergic synapses and partially compensating for impaired central cholinergic transmission described in the cholinergic hypothesis of Alzheimer’s disease. Additional mechanistic observations include modulation of glutamatergic signaling via effects on NMDA receptor regulation, interactions with amyloid‑related pathways, and possible suppression of pro‑inflammatory signaling, though these secondary actions are not fully characterized.
Donepezil demonstrates good oral absorption with peak plasma concentrations typically within several hours. It is extensively metabolized in the liver, with CYP2D6 and CYP3A4 contributing to biotransformation. The drug and its metabolites are eliminated through renal and biliary pathways. Its relatively long elimination half‑life supports once‑daily dosing. Donepezil is a substrate of multiple CYP pathways and the BCRP/ABCG2 transporter, creating potential for clinically relevant drug interactions.
Safety considerations include risks of bradycardia, syncope, gastrointestinal intolerance, insomnia, and muscle cramps. Patients with cardiac conduction abnormalities or receiving other bradycardia‑inducing agents may require additional monitoring. Serious adverse reactions, while less common, may include gastrointestinal bleeding or seizures, particularly in predisposed individuals.
Notable usage contexts include branded formulations such as Aricept and the transdermal system Adlarity. For API procurement, suppliers should demonstrate control of stereochemical purity, residual solvent limits, and impurity profiles aligned with pharmacopeial or ICH guidelines, supported by validated analytical methods and stability data appropriate for global regulatory submissions.
Identification & chemistry
| Generic name | Donepezil |
|---|---|
| Molecule type | Small molecule |
| CAS | 120014-06-4 |
| UNII | 8SSC91326P |
| DrugBank ID | DB00843 |
Pharmacology
| Summary | Donepezil is a selective, reversible acetylcholinesterase inhibitor that increases central acetylcholine levels to support cholinergic signaling implicated in Alzheimer’s‑related cognitive decline. Additional reported actions include modulation of NMDA receptor activity, effects on amyloid‑related pathways, and interaction with inflammatory signaling networks, suggesting broader neuroprotective influences. Its pharmacodynamic profile reflects enhancement of cholinergic transmission that helps mitigate key cognitive and behavioral symptoms of dementia. |
|---|---|
| Mechanism of action | The commonly accepted cholinergic hypothesisproposes that a portion of the cognitive and behavioral decline associated with Alzheimer's are the result of decreased cholinergic transmission in the central nervous system. Donepezil selectively and reversibly inhibits the acetylcholinesterase enzyme, which normally breaks down acetylcholine. The main pharmacological actions of this drug are believed to occur as the result of this enzyme inhibition, enhancing cholinergic transmission, which relieves the symptoms of Alzheimer's dementia. In addition to the above, other mechanisms of action of donepezil are possible, including the opposition of glutamate-induced excitatory transmission via downregulation of NMDA receptors and the regulation of amyloid proteins, which have demonstrated significant effects on the disease process of Alzheimer's.Other possible targets for donepezil may also include the inhibition various inflammatory signaling pathways, exerting neuroprotective effects. |
| Pharmacodynamics | By inhibiting the acetylcholinesterase enzyme, donepezil improves the cognitive and behavioral signs and symptoms of Alzheimer's Disease, which may include apathy, aggression, confusion, and psychosis. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Acetylcholinesterase | Humans | inhibitor |
| 5-hydroxytryptamine receptor 2A | Humans | inducer |
| Cholinesterase | Humans | inducer |
ADME / PK
| Absorption | Donepezil is slowly absorbed via the gastrointestinal tract after oral administration. Tmax is 3 to 4 hours with a bioavailability of 100% and steady-state concentrations are attained within 15 to 21 days of administration.The Tmax in one pharmacokinetic study determined a Tmax of 4.1 ± 1.5 hours.The Cmax of 5 mg donepezil tablets is estimated to be 8.34 ng/mL, according to the Canadian monograph.The AUC of 5 mg donepezil tablets has been determined to be 221.90-225.36 ng.hr/mL. |
|---|---|
| Half-life | The average elimination half-life of donepezil is about 70 hours according to the results of various studies and the FDA label for donepezil.. One pharmacokinetic study determined the average terminal half-life to be 81.5±22.0 h |
| Protein binding | Donepezil is 96% protein-bound, with approximately 75% binding to albumin and approximately 21% binding to alpha-1-glycoprotein. |
| Metabolism | Donepezil is metabolized by first pass metabolism in the liver, primarily by CYP3A4, in addition to CYP2D6. After this, O-dealkylation, hydroxylation, N-oxidation, hydrolysis, and O-glucuronidation occur, producing various metabolites with similar half-lives to the unchanged parent drug. A study of the pharmacokinetics of radiolabeled donepezil demonstrated that about 53% of plasma radioactivity appeared as donepezil in the unchanged form, and 11% was identified as the metabolite 6-O-desmethyl donepezil, which exerts similar potency inhibition of the acetylcholinesterase enzyme.This drug is heavily metabolized to four primary metabolites, two of which are considered pharmacologically active, as well as to multiple inactive and unidentified metabolites. |
| Route of elimination | In a study of radiolabeled administration donepezil in healthy adults, 57% of measured radioactivity was identified in the urine, and 5% was identified in the feces. |
| Volume of distribution | The volume of distribution of donepezil is 11.8 ± 1.7 L/kg for a 5-mg dose and 11.6 ± 1.91 L/kg for a 10-mg dose. It is largely distributed in the extravascular compartments. Donepezil crosses the blood-brain barrier and cerebrospinal fluid concentrations at the above doses have been measured at 15.7%.The volume of distribution at steady-state according to the FDA label for donepezil ranges from 12 - 16 L/kg. |
| Clearance | According to the FDA label, the average apparent plasma clearance of this drug is 0.13 – 0.19 L/hr/kg.A 5 mg dose of donepezil in healthy patients was shown to have a plasma clearance of 0.110±0.02 L/h/kg.In 10 patients diagnosed with alcoholic cirrhosis, showed a mean decrease in clearance by 20% when compared to the clearance in 10 healthy subjects. In 4 patients with severe renal impairment compared to 4 healthy subjects, no significant change in clearance was noted. |
Formulation & handling
- Low aqueous solubility and moderate lipophilicity support solid‑oral formulations, often requiring solubility‑enhancing excipients for consistent dissolution.
- Stable small‑molecule API suitable for oral and transdermal delivery; handling as a standard solid with no special sensitivity to food effects.
- Transdermal systems benefit from the API’s lipophilicity, enabling permeation but requiring control of adhesive matrix compatibility.
Regulatory status
| Lifecycle | The API’s core patents in the United States and Canada expired between 2010 and 2022, indicating that exclusivity has lapsed. With products marketed in both the US and Canada, the API is positioned in a mature market environment with established generic availability. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Donepezil’s supply landscape includes an originator and multiple established generic manufacturers, with a broad network of U.S.-based packagers supporting distribution. Branded and generic products are marketed in the United States and Canada, indicating mature global availability. Key patents have expired in both markets, supporting the presence of ongoing generic competition. |
|---|
Safety
| Toxicity | LD50 The rat oral LD50 of donepezil is 32.6 mg/kg. Overdose information Signs and symptoms of overdose with cholinesterase inhibitors such as donepezil can include severe nausea and vomiting, bradycardia, hypotension, perspiration, seizures, muscle weakness respiratory depression, and collapse. Significant muscle weakness may result in death if the respiratory muscles are affected by donepezil overdose. To manage an overdose, anticholinergics can be employed as antidotes. Atropine at intravenous doses of 1.0 - 2.0 mg can be administered and titrated according to the clinical response. Consult the local poison control center for the most updated guidelines on the management of a donepezil overdose. Whether donepezil can be removed from the body with dialysis is unknown at this time. |
|---|
- Rat oral LD50 is 32
- 6 mg/kg, indicating moderate acute toxicity by ingestion
- Overexposure may produce pronounced cholinergic effects, including bradycardia, hypotension, seizures, and respiratory muscle impairment
Good Manufacturing Practices
Active pharmaceutical ingredients are made in GMP-certified manufacturing facilities. GMP stands for Good Manufacturing Practices and is the main standard in the pharmaceutical industry. cGMP or Current GMP means that the company complies with the most recent requirements/version of GMP. The WHO has its own guideline for GMP, the World Health Organization or WHO GMP. The authority that has audited the company can also be from a country like China (Chinese GMP) or from the EU (EU GMP), every authority has different GMP requirements.
Donepezil is a type of Cholinesterase inhibitors
Cholinesterase inhibitors are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the treatment of various medical conditions. These compounds work by inhibiting the activity of the enzyme cholinesterase, which breaks down the neurotransmitter acetylcholine in the body.
Acetylcholine is involved in many important processes in the central and peripheral nervous systems, including muscle contractions, memory, and cognitive functions. By inhibiting cholinesterase, these APIs help to increase the levels of acetylcholine in the brain and enhance cholinergic neurotransmission.
Cholinesterase inhibitors have proven to be highly effective in the management of Alzheimer's disease, a progressive neurodegenerative disorder characterized by cognitive decline and memory loss. These APIs, such as donepezil, rivastigmine, and galantamine, are commonly used as symptomatic treatments to alleviate cognitive impairment and enhance patients' overall quality of life.
Furthermore, cholinesterase inhibitors find applications beyond Alzheimer's disease. They are also utilized in the treatment of other conditions, including Parkinson's disease, glaucoma, myasthenia gravis, and certain types of dementia.
The development and utilization of cholinesterase inhibitors have revolutionized the treatment options for patients suffering from these debilitating disorders. As research in neuroscience and pharmacology advances, the continuous refinement of cholinesterase inhibitors and the discovery of novel compounds within this subcategory hold promise for future therapeutic breakthroughs.
Donepezil (Cholinesterase inhibitors), 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.
Donepezil API manufacturers & distributors
Compare qualified Donepezil API suppliers worldwide. We currently have 28 companies offering Donepezil API, with manufacturing taking place in 6 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 |
|---|---|---|---|---|---|
| Chongqing Zein | Producer | China | China | CoA, WC | 2 products |
| Cipla | Producer | India | India | CoA, GMP, USDMF, WC | 164 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, KDMF, MSDS, USDMF, WC | 170 products |
| Finetech Pharma | Producer | Israel | Israel | CoA, USDMF | 4 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 98 products |
| Hikal | Producer | India | India | CoA, GMP, WC | 26 products |
| Ind-Swift Labs. | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 27 products |
| Kolon Life Science | Producer | South Korea | South Korea | CoA | 32 products |
| LGM Pharma | Distributor | United States | World | - | 441 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Piramal Healthcare | Producer | United Kingdom | India | CoA, GMP, WC | 31 products |
| Piramal Pharma Solutions | Producer | India | India | CoA, USDMF, WC | 44 products |
| PLIVA | Producer | Czech Republic | Czech Republic | CoA, JDMF | 31 products |
| Shandong Chenghui Shuangd... | Producer | China | China | CEP, CoA, GMP, ISO9001 | 98 products |
| Sichuan Benepure | Producer | China | China | CoA | 23 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, MSDS, USDMF | 757 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
| Torrent Pharma | Producer | India | India | CoA, USDMF | 34 products |
| Unichem Labs. | Producer | India | India | CoA, USDMF | 62 products |
| Unnati Pharmaceuticals Pv... | Distributor | India | India | CoA | 70 products |
| USV | Producer | India | India | CoA, GMP, USDMF, WC | 35 products |
| Vasudha Pharma Chem Ltd. | Producer | India | India | CoA, GMP, JDMF, MSDS, USDMF, WC | 37 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 133 products |
| Zhejiang East Asia Pharma... | Producer | China | China | CoA, JDMF | 4 products |
| Zhejiang East-Asia Pharma | Producer | China | China | CoA, JDMF | 7 products |
| Zhejiang Hisun Pharma | Producer | China | China | CoA, USDMF | 69 products |
When sending a request, specify which Donepezil 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 Donepezil 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.
Frequently asked questions about Donepezil API
Sourcing
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Technical
What is Donepezil (CAS 120014-06-4) used for?
Which therapeutic class does Donepezil fall into?
What conditions is Donepezil mainly prescribed for?
How does Donepezil work?
What should someone know about the safety or toxicity profile of Donepezil?
What are important formulation and handling considerations for Donepezil as an API?
Is Donepezil a small molecule?
Are there special stability concerns for oral Donepezil?
Regulatory
Where is Donepezil approved or in use globally?
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Pharmaoffer
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