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Gabapentin | CAS No: 60142-96-3 | GMP-certified suppliers
A medication that supports management of partial-onset seizures and relieves peripheral neuropathic pain, including postherpetic and diabetic neuropathy, for broad clinical use.
Therapeutic categories
Acids, AcyclicAcids, CarbocyclicAminesAmino AcidsAmino Acids, Peptides, and ProteinsAminobutyrates
Generic name
Gabapentin
Molecule type
small molecule
CAS number
60142-96-3
DrugBank ID
DB00996
Approval status
Approved drug, Investigational drug
ATC code
N02BF01
Primary indications
- In the United States, gabapentin is officially indicated for the treatment of postherpetic neuralgia in adults and for the adjunctive treatment of partial-onset seizures, with or without secondary generalization, in patients 3 years of age and older
- In Europe, gabapentin is indicated for adjunctive therapy in the treatment of partial-onset seizures, with or without secondary generalization, in patients 6 years of age and older and as monotherapy in patients 12 years of age and older
- It is also used in adults for the treatment of various types of peripheral neuropathic pain, such as painful diabetic neuropathy
Product Snapshot
- Gabapentin is an oral small‑molecule API available mainly in solid oral forms with some topical presentations
- It is used for partial‑onset seizure management and for peripheral neuropathic pain conditions, including postherpetic neuralgia
- It is approved in the US and Canada, with additional investigational development noted in some markets
Clinical Overview
Gabapentin (CAS 60142-96-3) is a gamma‑amino acid derivative structurally related to GABA and classified among gabapentinoids. It was developed as an anti‑epileptic agent and is now used globally in seizure management and neuropathic pain conditions.
Gabapentin is indicated in the United States for postherpetic neuralgia in adults and as adjunctive therapy for partial‑onset seizures in patients 3 years and older. In Europe, it is approved as adjunctive treatment for partial‑onset seizures in children 6 years and older and as monotherapy in individuals 12 years and older. It is also used in adults for peripheral neuropathic pain, including painful diabetic neuropathy and postherpetic neuralgia.
Gabapentin exhibits anticonvulsant and analgesic activity by reducing excitatory neurotransmitter release. Although its mechanism of action is not fully defined, it binds to the α2δ‑1 auxiliary subunit of voltage‑gated calcium channels, reducing the trafficking of α1 subunits to presynaptic membranes and attenuating calcium‑dependent neurotransmitter release. Upregulation of α2δ subunits is associated with chronic pain states, and gabapentin’s inhibitory effect at this site is considered central to its therapeutic effects. Additional interactions with adenosine receptors and voltage‑gated potassium channels have been reported, though their clinical relevance remains uncertain.
Gabapentin is not effective for absence seizures and should be used cautiously in patients with mixed seizure disorders that include absence episodes. The compound has a wide therapeutic index and undergoes minimal metabolism, reducing the likelihood of pharmacokinetic drug interactions. Reported toxicities include somnolence, dizziness, and rare hypersensitivity reactions such as DRESS, which can be severe. Early symptoms including fever, rash, or lymphadenopathy warrant prompt evaluation.
Gabapentin is formulated in several regional brands and generics for oral administration. For API procurement, suppliers should provide evidence of compliance with pharmacopoeial specifications, validated impurity controls, and consistent particle‑size characteristics to support robust formulation development and regulatory submissions.
Gabapentin is indicated in the United States for postherpetic neuralgia in adults and as adjunctive therapy for partial‑onset seizures in patients 3 years and older. In Europe, it is approved as adjunctive treatment for partial‑onset seizures in children 6 years and older and as monotherapy in individuals 12 years and older. It is also used in adults for peripheral neuropathic pain, including painful diabetic neuropathy and postherpetic neuralgia.
Gabapentin exhibits anticonvulsant and analgesic activity by reducing excitatory neurotransmitter release. Although its mechanism of action is not fully defined, it binds to the α2δ‑1 auxiliary subunit of voltage‑gated calcium channels, reducing the trafficking of α1 subunits to presynaptic membranes and attenuating calcium‑dependent neurotransmitter release. Upregulation of α2δ subunits is associated with chronic pain states, and gabapentin’s inhibitory effect at this site is considered central to its therapeutic effects. Additional interactions with adenosine receptors and voltage‑gated potassium channels have been reported, though their clinical relevance remains uncertain.
Gabapentin is not effective for absence seizures and should be used cautiously in patients with mixed seizure disorders that include absence episodes. The compound has a wide therapeutic index and undergoes minimal metabolism, reducing the likelihood of pharmacokinetic drug interactions. Reported toxicities include somnolence, dizziness, and rare hypersensitivity reactions such as DRESS, which can be severe. Early symptoms including fever, rash, or lymphadenopathy warrant prompt evaluation.
Gabapentin is formulated in several regional brands and generics for oral administration. For API procurement, suppliers should provide evidence of compliance with pharmacopoeial specifications, validated impurity controls, and consistent particle‑size characteristics to support robust formulation development and regulatory submissions.
Identification & chemistry
| Generic name | Gabapentin |
|---|---|
| Molecule type | Small molecule |
| CAS | 60142-96-3 |
| UNII | 6CW7F3G59X |
| DrugBank ID | DB00996 |
Pharmacology
| Summary | Gabapentin modulates neuronal excitability primarily by binding to the α2δ‑1 subunit of voltage‑gated calcium channels, reducing presynaptic calcium channel density and subsequent release of excitatory neurotransmitters. This activity underlies its therapeutic use in neuropathic pain and partial‑onset seizure disorders. Secondary interactions with adenosine receptors and potassium channels have been observed, but their clinical relevance is uncertain. |
|---|---|
| Mechanism of action | The precise mechanism through which gabapentin exerts its therapeutic effects is unclear.The primary mode of action appears to be at the auxillary α2δ-1 subunit of voltage-gated calcium channels (though a low affinity for the α2δ-2 subunit has also been reported).The major function of these subunits is to facilitate the movement of pore-forming α1 subunits of calcium channels from the endoplasmic reticulum to the cell membrane of pre-synaptic neurons.There is evidence that chronic pain states can cause an increase in the expression of α2δ subunits and that these changes correlate with hyperalgesia.Gabapentin appears to inhibit the action of α2δ-1 subunits, thus decreasing the density of pre-synaptic voltage-gated calcium channels and subsequent release of excitatory neurotransmitters.It is likely that this inhibition is also responsible for the anti-epileptic action of gabapentin. There is some evidence that gabapentin also acts on adenosine receptorsand voltage-gated potassium channels,though the clinical relevance of its action at these sites is unclear. |
| Pharmacodynamics | Gabapentin is an anti-convulsant medication that inhibits the release of excitatory neurotransmitters, allowing for its use against pathologic neurotransmission such as that seen in neuropathic pain and seizure disorders.It has a wide therapeutic index, with doses in excess of 8000 mg/kg failing to cause a fatal reaction in rats. Gabapentin is ineffective in absence seizures and should be used in caution in patients with mixed seizure disorders involving absence seizures. Gabapentin has been associated with drug reaction with eosinophilia and systemic symptoms (DRESS), otherwise known as multi-organ hypersensitivity. This reaction can prove fatal and early symptoms such as fever, lymphadenopathy, and rash should be promptly investigated. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-dependent calcium channel subunit alpha-2/delta-1 | Humans | inhibitor |
| Voltage-dependent calcium channel subunit alpha-2/delta-2 | Humans | inhibitor |
| Voltage-dependent N-type calcium channel | Humans | inhibitor |
ADME / PK
| Absorption | Absorption of gabapentin is thought to occur solely via facilitated transport by the LAT1 transporter within the intestines.As this process is saturable, the oral bioavailability of gabapentin is inversely proportional to the administered dose - the oral bioavailability of a 900mg/day regimen is approximately 60%, whereas a 4800mg/day regimen results in only 27% bioavailability.The T<sub>max</sub> of gabapentin has been estimated to be 2-3 hours.Food has no appreciable effect on gabapentin absorption. |
|---|---|
| Half-life | The elimination t<sub>1/2</sub> of gabapentin in patients with normal renal function is 5-7 hours.In patients with reduced renal function, the elimination t<sub>1/2</sub> may be prolonged - in patients with a creatinine clearance of <30 mL/min, the reported half-life of gabapentin was approximately 52 hours. |
| Protein binding | Less than 3% of an orally administered dose of gabapentin is bound to plasma proteins. |
| Metabolism | Gabapentin is not appreciably metabolized in humans- in humans, metabolites account for less than 1% of an administered dose, with the remainder being excreted as unchanged parent drug in the urine. |
| Route of elimination | Gabapentin is eliminated solely in the urine as unchanged drug.Cimetidine, an inhibitor of renal tubular secretion, reduces clearance by approximately 12%, suggesting that some degree of tubular secretion is involved in the renal elimination of gabapentin. |
| Volume of distribution | The apparent volume of distribution of gabapentin after IV administration is 58±6 L.The drug is found in the CSF in concentrations approximately 9-20% of the corresponding plasma concentrations and is secreted into breast milk in concentrations similar to that seen in plasma. |
| Clearance | Both the plasma clearance and renal clearance of gabapentin are directly proportional to the patient's creatinine clearance due to its primarily renal elimination. |
Formulation & handling
- Oral small‑molecule API with high aqueous solubility, enabling conventional tablet, capsule, and liquid formulations without complex solubilization strategies.
- Stable solid suitable for standard handling; hygroscopicity is modest but solutions and suspensions require typical aqueous‑system microbial and pH control.
- Food has minimal impact on absorption, allowing flexible administration timing in formulation design.
Regulatory status
| Lifecycle | Key U.S. and Canadian patents for the API expired between 2016 and 2022, indicating that exclusivity has lapsed in both markets. With products marketed in Canada and the United States, the API is in a mature stage of its lifecycle with established generic availability expected. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Gabapentin’s supply landscape is dominated by numerous generic manufacturers and repackagers, with the original product introduced by Pfizer and its legacy entities before broad generic entry. The molecule is widely available in major markets such as the US and Canada, with multiple branded generic presentations. Key US and Canadian patents have expired, indicating that generic competition is well established. |
|---|
Safety
| Toxicity | The oral TDLo of gabapentin in humans is 2.86 mg/kg and the LD<sub>50</sub> in rats has been found to be >8000 mg/kg.Symptoms of overdose are consistent with the drug's adverse effect profile and involve CNS depression (e.g. dizziness, drowsiness, slurred speech, lethargy, loss of consciousness) and gastrointestinal symptoms such as diarrhea.Management of overdose should involve symptomatic and supportive treatment. Gabapentin can be removed by hemodialysis - this may be of benefit in some patients, such as those with impaired renal function. Multi-drug overdoses involving gabapentin, particularly in combination with other CNS depressants such as opioids, can result in coma and death - this possibility should be considered when managing overdosage. |
|---|
High Level Warnings:
- Human oral TDLo is 2
- 86 mg/kg and rat LD50 exceeds 8000 mg/kg
- Acute exposure may produce CNS depression and gastrointestinal disturbances consistent with the compound’s known adverse effect profile
Gabapentin is a type of Anticonvulsants
Anticonvulsants are a vital category of pharmaceutical Active Pharmaceutical Ingredients (APIs) used for the treatment of seizures and epilepsy. These APIs play a crucial role in managing and preventing convulsions, which are characterized by abnormal electrical activity in the brain. With a significant demand for effective anticonvulsant medications, these APIs hold immense importance in the pharmaceutical industry.
Anticonvulsant APIs work by stabilizing the excessive electrical activity in the brain, preventing or reducing seizures. They achieve this by targeting specific receptors or channels involved in the regulation of neuronal excitability. Some commonly used anticonvulsant APIs include phenytoin, valproic acid, carbamazepine, and lamotrigine.
Pharmaceutical companies utilize these APIs to formulate various dosage forms, such as tablets, capsules, and oral suspensions, ensuring convenient administration for patients. Additionally, anticonvulsant APIs may also be employed in the development of extended-release formulations, providing sustained and controlled drug release.
The market for anticonvulsant APIs continues to grow due to the rising prevalence of epilepsy and other seizure disorders. Moreover, ongoing research and development efforts aim to enhance the efficacy, safety, and tolerability of these APIs, ensuring better treatment outcomes for patients.
In conclusion, anticonvulsant APIs are a crucial pharmaceutical category used to manage seizures and epilepsy. With their ability to stabilize brain activity, these APIs play a pivotal role in improving the quality of life for individuals living with these conditions. The pharmaceutical industry's continued focus on research and development in this area ensures the availability of advanced and effective anticonvulsant medications for patients in need.
Gabapentin API manufacturers & distributors
Compare qualified Gabapentin API suppliers worldwide. We currently have 25 companies offering Gabapentin API, with manufacturing taking place in 9 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 |
|---|---|---|---|---|---|
| ACE Japan | Producer | Japan | Japan | CoA | 76 products |
| Anjan Drugs | Producer | India | India | CEP, CoA, FDA, GMP, USDMF | 4 products |
| Divis Labs. | Producer | India | India | CEP, CoA, FDA, GMP, ISO9001, Other, JDMF, KDMF, USDMF, WC | 47 products |
| Duchefa Farma B.V. | Distributor | Netherlands | India | CoA, GMP, ISO9001, MSDS | 170 products |
| Erregierre | Producer | Italy | Italy | CEP, CoA, FDA, GMP, USDMF | 44 products |
| G.C. Chemie Pharmie Ltd | Producer | India | India | CoA | 21 products |
| Hetero Drugs | Producer | India | Unknown | CEP, CoA, FDA, GMP, KDMF, USDMF, WC | 98 products |
| Hikal | Producer | India | India | CEP, CoA, FDA, GMP, JDMF, KDMF, USDMF, WC | 26 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Malladi Drugs & Pharma | Producer | India | India | CoA, GMP, WC | 14 products |
| Medichem | Producer | Spain | Unknown | CEP, CoA, FDA, GMP | 39 products |
| Menadiona, S.L. | Producer | Spain | Spain | BSE/TSE, CoA, GMP, ISO9001, KDMF, MSDS, USDMF, WHO-GMP | 15 products |
| Metapharmaceutical Indust... | Producer | Spain | India | BSE/TSE, CoA, GDP, GMP, ISO14001, MSDS, WC, WHO-GMP | 21 products |
| Mylan | Producer | India | India | CEP, CoA, FDA, GMP, KDMF, USDMF, WC | 201 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, USDMF | 144 products |
| Saraca Labs. | Producer | India | India | CEP, CoA, FDA, USDMF | 2 products |
| Sicor | Producer | Italy | Italy | CoA, GMP | 47 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, USDMF | 757 products |
| Strides Pharma Science | Producer | India | Unknown | CEP, CoA, GMP, KDMF | 14 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
| Tresinde Biotech | Producer | India | India | CoA, GMP | 50 products |
| Unnati Pharmaceuticals Pv... | Distributor | India | India | CoA | 70 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 134 products |
| Zhejiang Chiral M.C. | Producer | China | China | CEP, CoA, FDA, KDMF, USDMF | 4 products |
| Zhejiang Excel Pharma | Producer | China | China | CoA, USDMF | 2 products |
When sending a request, specify which Gabapentin 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 Gabapentin 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 Gabapentin API
Sourcing
What matters most when sourcing GMP-grade Gabapentin?
When sourcing GMP‑grade Gabapentin in the US or Canada, confirm that the manufacturer complies with current GMP requirements and can provide complete regulatory documentation such as DMFs or equivalent quality files. Supplier qualification should include verification of audit history, change‑control practices, and batch-to-batch consistency. Given the broad generic market, it is also important to confirm clear traceability through repackagers to the original API manufacturer.
Which documents are typically required when sourcing Gabapentin API?
Request the core API documentation set: CoA (25 companies), GMP (17 companies), USDMF (14 companies), CEP (13 companies), FDA (9 companies). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Gabapentin API?
Known or reported manufacturers for Gabapentin: Duchefa Farma B.V., Xi'an Tian Guangyuan Biotech Co.,Ltd, Tresinde Biotech, Sinoway industrial Co.,Ltd, Veeprho Group, LGM Pharma, Rochem International, Inc.. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Gabapentin API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Gabapentin manufacturers?
Audit reports may be requested for Gabapentin: 9 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Gabapentin API on Pharmaoffer?
Reported supplier count for Gabapentin: 25 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Gabapentin API?
Production countries reported for Gabapentin: India (11 producers), China (4 producers), Italy (2 producers). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Gabapentin usually hold?
Common certifications for Gabapentin suppliers: CoA (25 companies), GMP (17 companies), USDMF (14 companies), CEP (13 companies), FDA (9 companies). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Gabapentin (CAS 60142-96-3) used for?
Gabapentin is used as adjunctive therapy for partial‑onset seizures and for the management of neuropathic pain conditions. In the United States, it is indicated for postherpetic neuralgia in adults and for partial‑onset seizures in patients 3 years and older. In Europe, it is approved for partial‑onset seizures in children 6 years and older, as monotherapy from 12 years, and for peripheral neuropathic pain in adults, including painful diabetic neuropathy and postherpetic neuralgia.
Which therapeutic class does Gabapentin fall into?
Gabapentin belongs to the following therapeutic categories: Acids, Acyclic, Acids, Carbocyclic, Amines, Amino Acids, Amino Acids, Peptides, and Proteins. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Gabapentin mainly prescribed for?
The primary indications for Gabapentin: In the United States, Gabapentin is officially indicated for the treatment of postherpetic neuralgia in adults and for the adjunctive treatment of partial-onset seizures, with or without secondary generalization, in patients 3 years of age and older, In Europe, Gabapentin is indicated for adjunctive therapy in the treatment of partial-onset seizures, with or without secondary generalization, in patients 6 years of age and older and as monotherapy in patients 12 years of age and older, It is also used in adults for the treatment of various types of peripheral neuropathic pain, such as painful diabetic neuropathy. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Gabapentin work?
The precise mechanism through which Gabapentin exerts its therapeutic effects is unclear.The primary mode of action appears to be at the auxillary α2δ-1 subunit of voltage-gated calcium channels (though a low affinity for the α2δ-2 subunit has also been reported).The major function of these subunits is to facilitate the movement of pore-forming α1 subunits of calcium channels from the endoplasmic reticulum to the cell membrane of pre-synaptic neurons.There is evidence that chronic pain states can cause an increase in the expression of α2δ subunits and that these changes correlate with hyperalgesia.Gabapentin appears to inhibit the action of α2δ-1 subunits, thus decreasing the density of pre-synaptic voltage-gated calcium channels and subsequent release of excitatory neurotransmitters.It is likely that this inhibition is also responsible for the anti-epileptic action of Gabapentin.
There is some evidence that Gabapentin also acts on adenosine receptorsand voltage-gated potassium channels,though the clinical relevance of its action at these sites is unclear.
What should someone know about the safety or toxicity profile of Gabapentin?
Gabapentin has a wide therapeutic index, with a human oral TDLo of 2.86 mg/kg and a rat LD50 exceeding 8000 mg/kg. Acute overexposure may lead to CNS depression and gastrointestinal disturbances, consistent with its known adverse effects. Common toxicities include somnolence and dizziness, and rare hypersensitivity reactions such as DRESS can occur; early signs like fever, rash, or lymphadenopathy require prompt evaluation. It should be used cautiously in individuals with mixed seizure disorders that include absence episodes.
What are important formulation and handling considerations for Gabapentin as an API?
Gabapentin’s high aqueous solubility supports conventional tablet, capsule, and liquid formulations without specialized solubilization approaches. The solid API is generally stable, though modest hygroscopicity warrants standard moisture control during handling and manufacturing. Aqueous solutions or suspensions require routine pH and microbial management. Food has minimal impact on absorption, so timing of administration does not impose specific formulation constraints.
Is Gabapentin a small molecule?
Gabapentin is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Gabapentin?
Gabapentin is a stable solid with only modest hygroscopicity, so typical protection from moisture during manufacturing and storage is sufficient. In aqueous oral solutions or suspensions, standard microbial preservation and pH control are required. No special stability concerns beyond routine measures for aqueous systems are noted.
Regulatory
Where is Gabapentin approved or in use globally?
Gabapentin is reported as approved in the following major regions: Canada, US. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
What’s the regulatory and patent landscape for Gabapentin right now?
Gabapentin is approved in both the United States and Canada, where it is available as a generic drug. Key patents on the original formulations have expired, allowing multiple manufacturers to market approved generics. Current regulatory oversight focuses on maintaining compliance with quality, labeling, and post‑market safety requirements.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Gabapentin procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Gabapentin. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Gabapentin included in the PRO Data Insights coverage?
PRO Data Insights coverage for Gabapentin: 4762 verified transactions across 937 suppliers and 500 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Gabapentin?
Market report availability for Gabapentin: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
