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Almotriptan | CAS No: 154323-57-6 | GMP-certified suppliers
A medication that provides acute treatment for migraine headaches in adults by targeting serotonergic pathways to alleviate pain associated with migraine attacks.
Therapeutic categories
Primary indications
- For the treatment of acute migraine headache in adults
Product Snapshot
- Almotriptan is an oral small molecule formulated primarily as film-coated tablets
- It is indicated for the treatment of acute migraine headaches in adults
- Almotriptan is approved and marketed in the US and Canada, with some investigational statuses
Clinical Overview
Pharmacologically, Almotriptan acts as a high-affinity agonist at human 5-HT1B and 5-HT1D receptors. This selective agonism results in cranial vasoconstriction, which alleviates migraine headache pain. The drug has minimal affinity for other serotonin receptor subtypes such as 5-HT1A, 5-HT5A, and 5-HT7, and exhibits no significant interaction with receptors including 5-HT2, 5-HT3, 5-HT4, adrenergic, dopaminergic, muscarinic, or benzodiazepine receptors. Experimental evidence also suggests that Almotriptan activates 5-HT1 receptors on trigeminal nerve peripheral terminals innervating cranial blood vessels, contributing to its antimigraine effect.
Pharmacokinetics involve metabolism primarily through cytochrome P450 isoenzymes, including CYP2C19, CYP3A4, and CYP2D6. The compound is a substrate for multiple CYP enzymes and is mainly eliminated via renal excretion. These metabolic pathways necessitate consideration of potential drug-drug interactions, particularly with other CYP substrates or inhibitors.
Safety considerations include the risk of vasoconstriction-related adverse events and contraindications in patients with ischemic heart disease or uncontrolled hypertension. Almotriptan is structurally a fused-ring heterocyclic indole derivative with amine functionality, classifying it among serotonergic drugs with a potential for serotonin syndrome when combined with other serotonergic agents.
Notable brand names include Axert, among others, with widespread regulatory approvals for acute migraine treatment.
For API sourcing, quality control should emphasize chemical purity, batch consistency, and compliance with pharmacopeial standards. Given Almotriptan’s sensitivity to stereochemistry and functional groups critical for receptor binding, robust analytical characterization and adherence to GMP manufacturing are essential to ensure product efficacy and safety.
Identification & chemistry
| Generic name | Almotriptan |
|---|---|
| Molecule type | Small molecule |
| CAS | 154323-57-6 |
| UNII | 1O4XL5SN61 |
| DrugBank ID | DB00918 |
Pharmacology
| Summary | Almotriptan is a selective agonist of 5-HT1B and 5-HT1D receptors, primarily targeting cranial blood vessels to induce vasoconstriction. It also modulates 5-HT1 receptors on trigeminal nerve terminals, which may contribute to its effect on migraine relief. This pharmacological activity underlies its use in the acute treatment of migraine attacks in adults. |
|---|---|
| Mechanism of action | Almotriptan binds with high affinity to human 5-HT<sub>1B</sub> and 5-HT<sub>1D</sub> receptors leading to cranial blood vessel constriction. |
| Pharmacodynamics | Almotriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almotriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Almotriptan is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT<sub>1D</sub> family) having only a weak affinity for 5-HT<sub>1A</sub>, 5-HT<sub>5A</sub>, and 5-HT<sub>7</sub> receptors and no significant affinity or pharmacological activity at 5-HT<sub>2</sub>, 5-HT<sub>3</sub> or 5-HT<sub>4</sub> receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Almotriptan also activates 5-HT<sub>1</sub> receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Almotriptan in humans. |
Targets
| Target | Organism | Actions |
|---|---|---|
| 5-hydroxytryptamine receptor 1D | Humans | agonist |
| 5-hydroxytryptamine receptor 1B | Humans | agonist |
ADME / PK
| Half-life | 3-4 hours |
|---|---|
| Protein binding | 35% |
| Route of elimination | Almotriptan is eliminated primarily by renal excretion (about 75% of the oral dose), with approximately 40% of an administered dose excreted unchanged in urine. Approximately 13% of the administered dose is excreted via feces, both unchanged and metabolized. |
| Volume of distribution | * 180 to 200 L |
| Clearance | * 57 L/h [healthy] * 34.2 L/h [moderate renal impairment (creatinine clearance between 31 and 71 mL/min)] * 9.8 L/h [severe renal impairment (creatinine clearance between 10 and 30 mL/min)] |
Formulation & handling
- Almotriptan is a small molecule compound intended for oral administration as film-coated tablets.
- Its aqueous solubility is low (0.121 g/L), which may require consideration for formulation and bioavailability enhancement.
- The API's absorption is not significantly affected by food, simplifying dosing without food restrictions.
Regulatory status
| Lifecycle | The API's patent protection expired in Canada in July 2013 and in the United States in November 2015, indicating that the product is in the mature phase of its lifecycle in both markets. Generic competition may be present following patent expiry in these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Almotriptan is primarily manufactured and packaged by a limited number of originator companies within the Janssen Pharmaceuticals group, indicating a consolidated supply base. The branded products are predominantly present in the US and Canadian markets. Given that key patents expired in 2013 (Canada) and 2015 (US), the API is subject to existing generic competition in these regions. |
|---|
Almotriptan is a type of Selective Serotonin Reuptake Inhibitors (SSRIs)
Selective Serotonin Reuptake Inhibitors (SSRIs) are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used for the treatment of various mental health disorders, particularly depression and anxiety. SSRIs work by inhibiting the reuptake of serotonin, a neurotransmitter that plays a crucial role in regulating mood, emotions, and well-being.
These medications are designed to selectively target the serotonin transporter proteins in the brain, preventing the reabsorption of serotonin into the presynaptic neuron. By blocking the reuptake process, SSRIs increase the concentration of serotonin in the synaptic cleft, enhancing its availability for binding to postsynaptic receptors. This ultimately leads to an improved transmission of serotonin signals between neurons.
The mechanism of action of SSRIs helps to alleviate symptoms of depression and anxiety by stabilizing mood, reducing feelings of sadness, enhancing motivation, and promoting a sense of calmness. The exact therapeutic effects and onset of action may vary depending on the specific SSRIs used.
SSRIs have gained popularity due to their favorable safety profile and efficacy in treating a range of mental health conditions. Common SSRIs include fluoxetine, sertraline, citalopram, and escitalopram. These medications are typically available in oral dosage forms, such as tablets or capsules.
It's important to note that SSRIs should be prescribed and monitored by healthcare professionals, as they can have potential side effects and interactions with other medications. Individuals considering SSRIs should consult with their healthcare provider to determine the most appropriate treatment option for their specific needs.
Almotriptan API manufacturers & distributors
Compare qualified Almotriptan API suppliers worldwide. We currently have 4 companies offering Almotriptan 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 |
|---|---|---|---|---|---|
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| Mylan | Producer | India | India | CoA, GMP, USDMF, WC | 201 products |
| Ranke Quimica | Producer | Spain | Spain | CoA, GMP, USDMF | 3 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
When sending a request, specify which Almotriptan 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 Almotriptan 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.
