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Zolmitriptan | CAS No: 139264-17-8 | GMP-certified suppliers
A medication that provides acute treatment for migraines with or without aura in adults, supporting reliable development of products for neurological pain management needs.
Therapeutic categories
Primary indications
- Zolmitriptan is indicated for the acute treatment of migraine with or without auras in patients aged 18 and over
Product Snapshot
- Zolmitriptan is a small‑molecule API supplied for oral solid dosage forms and intranasal spray formulations
- It is used for acute migraine management, including cases with or without aura
- It holds regulatory approvals in the US and Canada, with some investigational statuses noted in certain markets
Clinical Overview
Zolmitriptan is a selective serotonin 5‑HT1B/1D/1F receptor agonist. Activation of 5‑HT1B/1D receptors within the trigeminocervical complex is proposed to reduce nociceptive signaling associated with migraine. Additional actions include inhibition of calcitonin gene‑related peptide release through 5‑HT1D receptor activation and cranial vasoconstriction via 5‑HT1B receptor engagement. Activity at 5‑HT1F receptors is known but its clinical significance remains incompletely characterized.
The therapeutic effect aligns with current understanding of migraine pathophysiology, which involves trigeminovascular activation, release of vasoactive neuropeptides, and cortical spreading depression in cases with aura. Zolmitriptan provides relief in the headache phase but is not intended for prophylaxis.
Zolmitriptan is rapidly absorbed, with oral bioavailability influenced by first‑pass metabolism. It is hepatically metabolized, including via CYP1A2, to an active metabolite that contributes to clinical effect. Elimination occurs through both renal and fecal pathways. The onset and systemic exposure vary by formulation, with nasal delivery generally providing faster absorption.
Safety considerations include the risk of vasoconstriction‑related events such as myocardial ischemia, arrhythmias, stroke, and peripheral vasospasm. Serotonin syndrome is possible, particularly with concurrent serotonergic drugs. Medication overuse headache has been reported with frequent use. Patients with phenylketonuria require caution with formulations containing phenylalanine.
For API procurement, suppliers should provide evidence of impurity control consistent with ICH guidelines, validated analytical methods, and documentation supporting consistent polymorphic form and stability to ensure suitability for regulated pharmaceutical manufacturing.
Identification & chemistry
| Generic name | Zolmitriptan |
|---|---|
| Molecule type | Small molecule |
| CAS | 139264-17-8 |
| UNII | 2FS66TH3YW |
| DrugBank ID | DB00315 |
Pharmacology
| Summary | Zolmitriptan is a serotonin receptor agonist that primarily targets 5‑HT1B and 5‑HT1D receptors within trigeminovascular pathways to modulate nociceptive signaling during acute migraine attacks. Activation of these receptors suppresses release of vasoactive peptides such as CGRP and produces cranial vasoconstriction, reducing migraine‑associated neurovascular activation. The drug also interacts with 5‑HT1F and additional serotonin receptor subtypes, reflecting broader involvement in migraine‑related neuronal circuits. |
|---|---|
| Mechanism of action | Migraines are complex physiological events characterized by unilateral throbbing headaches combined with photophobia and other aversions to sensory input. Migraine attacks are generally divided into phases: the premonitory phase, which typically involves irritability, fatigue, yawning, and stiff neck; the headache phase, which lasts for between four and 72 hours; and the postdrome phase, which lasts for up to a day following resolution of pain and whose symptoms are similar to those of the premonitory phase. In addition, neurological deficits, collectively termed migraine aura, may precede the headache phase. The underlying pathophysiology of migraines is a matter of active research but involves both neurological and vascular components. The head pain associated with migraine is thought to be a consequence of activation of the nociceptive nerves comprising the trigeminocervical complex (TCC).Terminals of nociceptive nerves that innervate the dura matter release vasoactive peptides, such as calcitonin gene-related peptide (CGRP), resulting in cranial vasodilation. Finally, when present, migraine aura appears to correlate with a transient wave(s) of cortical depolarization, termed cortical spreading depression (CSD). Triptans, including zolmitriptan, are proposed to act in three ways. The main mechanism is through modulation of nociceptive nerve signalling in the central nervous system through 5-HT<sub>1B/1D</sub> receptors throughout the TCC and associated areas of the brain. In addition, triptans can enhance vasoconstriction, both through direct 5-HT<sub>1B</sub>-mediated dilation of cranial blood vessels,as well as through 5-HT<sub>1D</sub>-mediated suppression of CGRP release. Although triptans are classically described solely in terms of their effects on 5-HT<sub>1B/1D</sub> receptors, they also act as 5-HT<sub>1F</sub> agonists as well. This 5-HT subtype is also found throughout the TCC, but is not present appreciably in cerebral vasculature; the significance of triptan-mediated 5-HT<sub>1F</sub> activation is currently not well described.Additionally, CSD that initiates in the ipsilateral parietal region may exert its effects in a manner that relies on 5-HT<sub>1B/1D</sub> receptor activation, suggesting that triptans may have some effect on CSD-mediated symptoms. |
| Pharmacodynamics | Zolmitriptan, like other triptans, is a serotonin (5-hydroxytryptamine; 5-HT) receptor agonist, with enhanced specificity for the 5-HT<sub>1B</sub> and 5-HT<sub>1D</sub> receptor subtypes. It is through the downstream effects of 5-HT<sub>1B/1D</sub> activation that triptans are proposed to provide acute relief of migraines.Zolmitriptan is also a vasoconstrictor,leading to possible adverse cardiovascular effects such as myocardial ischemia/infarction, arrhythmias, cerebral and subarachnoid hemorrhage, stroke, gastrointestinal ischemia, and peripheral vasospastic reactions. In addition, chest/throat/neck/jaw pain, tightness, and/or pressure has been reported, along with the possibility of medication overuse headaches and serotonin syndrome. Patients with phenylketonuria should be advised that ZOMIG-ZMT contains phenylalanine. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 1B | Humans | agonist |
| 5-hydroxytryptamine receptor 1D | Humans | agonist |
| 5-hydroxytryptamine receptor 1F | Humans | agonist |
ADME / PK
| Absorption | Zolmitriptan tablets have a mean absolute oral bioavailability of approximately 40%, with food having no effect on the rate or extent of absorption.The dosing kinetics are linear over a range of 2.5 to 50 mg with 75% of the eventual C<sub>max</sub> being attained within 1 hour of dosing. The median T<sub>max</sub> for the tablet form is 1.5 hours, while for the orally disintegrating tablet form, it is 3 hours.The AUC across studies was in the range of 84.4-173.8 ng/mL*h while the C<sub>max</sub> was between 16 and 25.2 ng/mL. Zolmitriptan administered as a nasal spray is detected in the plasma within 2-5 minutes, compared to 10-15 minutes for the tablet form; the faster kinetics likely reflect fast absorption across the nasal mucosa.The bioavailability compared to the tablet is 102%, and plasma zolmitriptan concentration is maintained for 4-6 hours after intranasal delivery. The active N-desmethyl metabolite of zolmitriptan has a mean plasma concentration that is roughly two-thirds of zolmitriptan, regardless of dosage route or concentration. |
|---|---|
| Half-life | Zolmitriptan has a mean elimination half-life of approximately three hours following oral or nasal administration. Its active N-desmethyl metabolite has a slightly longer (approximately 3.5 hours) half-life. |
| Protein binding | Zolmitriptan and its active N-desmethyl metabolite remain approximately 25% bound to plasma proteins over a concentration range of 10-1000 ng/mL. |
| Metabolism | Zolmitriptan is metabolized in the liver, and studies using cytochrome P450 inhibitors like [cimetidine] suggest that it is likely metabolized by CYP1A2, as well as by monoamine oxidase (MAO).Zolmitriptan metabolism results in three major metabolites: an active N-desmethyl metabolite (183C91) as well as inactive N-oxide (1652W92) and indole acetic acid (2161W92) metabolites. |
| Route of elimination | Zolmitriptan is primarily excreted in urine (approximately 65%) and feces (approximately 30%). Within urine, the most common form is the indole acetic acid metabolite (31%), followed by the N-oxide (7%), and N-desmethyl (4%) metabolites; the majority of zolmitriptan recovered in feces remains unchanged. |
| Volume of distribution | Zolmitriptan has a volume of distribution between 7 and 8.4 L/kg. |
| Clearance | Zolmitriptan has a clearance of 31.5 mL/min/kg for oral tablets and 25.9 mL/min/kg for nasal administration; one-sixth of the clearance is renal. |
Formulation & handling
- Oral tablets and ODTs require attention to the API’s low aqueous solubility, often necessitating disintegration optimization or solubility‑enhancing excipients.
- Nasal spray formulations benefit from the small‑molecule, moderately lipophilic profile, supporting rapid mucosal absorption but requiring control of solution clarity and chemical stability.
- Food has minimal impact on oral bioavailability, so no special formulation adjustments for food effects are typically needed.
Regulatory status
| Lifecycle | Most core U.S. and Canadian patents for this API expired between 2011 and 2021, indicating that market exclusivity has largely ended. With products marketed in both the United States and Canada, the API is in a mature stage with established generic availability expected. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Zolmitriptan was originally developed and supplied by a small group of originator manufacturers, with additional packagers supporting distribution in the US and Canada. Branded and authorized generic products are widely available in both markets, indicating established global presence beyond the originator brands. With key US and Canadian patents having expired between 2011 and 2021, the molecule is already subject to mature generic competition. |
|---|
Safety
| Toxicity | Toxicity information regarding zolmitriptan is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as cardiovascular symptoms due to excessive vasoconstriction and activation of serotonergic receptors. Patients receiving a single 50 mg oral dose of zolmitriptan often experienced sedation. Symptomatic and supportive measures are recommended. |
|---|
- Excessive exposure may intensify serotonergic and vasoconstrictive activity, posing risk for cardiovascular adverse effects
- High oral doses (e
- G
Zolmitriptan is a type of Selective 5HT1-agonists
Selective 5HT1-agonists are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the treatment of various neurological and psychiatric disorders. These compounds specifically target and activate the 5HT1 receptor subtype, which belongs to the serotonin (5-hydroxytryptamine) receptor family. The 5HT1 receptor is primarily found in the central nervous system and is involved in regulating neurotransmitter release, mood, pain perception, and vasoconstriction.
Selective 5HT1-agonists have demonstrated therapeutic potential in the management of several conditions, including migraines, cluster headaches, and depression. By binding to and activating the 5HT1 receptor, these APIs can modulate serotonin levels in the brain, leading to a cascade of neurochemical events that alleviate symptoms associated with these disorders.
One of the key advantages of selective 5HT1-agonists is their targeted action, focusing specifically on the 5HT1 receptor without significant interactions with other receptor subtypes. This selectivity reduces the risk of adverse effects and improves the overall safety profile of these APIs.
Moreover, selective 5HT1-agonists often exhibit high affinity for the 5HT1 receptor, enhancing their efficacy and therapeutic potential. Through their agonistic activity, these compounds can regulate the release of neurotransmitters and modulate pain pathways, offering relief to patients suffering from debilitating migraines or cluster headaches.
In summary, selective 5HT1-agonists are a valuable subcategory of pharmaceutical APIs that provide targeted and effective treatment options for various neurological and psychiatric disorders. Their ability to selectively activate the 5HT1 receptor offers therapeutic benefits with reduced side effects, making them an essential component in the management of conditions such as migraines, cluster headaches, and depression.
Zolmitriptan (Selective 5HT1-agonists), 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.
Zolmitriptan API manufacturers & distributors
Compare qualified Zolmitriptan API suppliers worldwide. We currently have 12 companies offering Zolmitriptan API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Emcure Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 80 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Hetero Drugs | Producer | India | India | CoA, USDMF | 98 products |
| Jubilant Pharmova | Producer | India | India | BSE/TSE, CEP, CoA, GMP, ISO9001, JDMF, MSDS, USDMF | 52 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Mylan | Producer | India | India | CoA, GMP, USDMF, WC | 201 products |
| Natco Pharma | Producer | India | India | CoA, FDA, GMP, USDMF, WC | 40 products |
| PLIVA | Producer | Czech Republic | Croatia | CoA, GMP | 31 products |
| SEDANAH | Distributor | Jordan | World | CoA, GMP | 70 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
| Syn-tech Chem | Producer | Taiwan | Taiwan | CoA, JDMF, USDMF | 22 products |
| Unichem Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 62 products |
When sending a request, specify which Zolmitriptan 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 Zolmitriptan 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 Zolmitriptan API
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Regulatory
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