Last reviewed · How we verify
Maxalt (RIZATRIPTAN)
Maxalt works by binding to serotonin receptors in the brain to relieve migraine pain.
Maxalt (Rizatriptan) is a serotonin-1b and serotonin-1d receptor agonist, a small molecule developed by Merck and currently owned by Gensco. It targets the 5-hydroxytryptamine receptor 1D to treat migraine, with FDA approval in 1998. Maxalt is available as a generic medication, with 16 generic manufacturers. Key safety considerations include its short half-life of 2.2 hours and moderate bioavailability of 45%. The commercial status of Maxalt is generic, as it is no longer patented.
At a glance
| Generic name | RIZATRIPTAN |
|---|---|
| Sponsor | Gensco |
| Drug class | Serotonin-1b and Serotonin-1d Receptor Agonist |
| Target | 5-hydroxytryptamine receptor 1D |
| Modality | Small molecule |
| Therapeutic area | Neuroscience |
| Phase | FDA-approved |
| First approval | 1998 |
Mechanism of action
Mechanism of Action. Rizatriptan binds with high affinity to human cloned 5-HT1B and 5-HT1D receptors. Rizatriptan has weak affinity for other 5-HT1 receptor subtypes (5-HT1A, 5-HT1E, 5-HT1F) and the 5-HT7 receptor, but has no significant activity at 5-HT2, 5-HT3, alpha- and beta-adrenergic, dopaminergic, histaminergic, muscarinic or benzodiazepine receptors. Current theories on the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of vasoactive and pro-inflammatory peptides from sensory nerve endings in an activated trigeminal system. The therapeutic activity of rizatriptan in migraine can most likely be attributed to agonist effects at 5-HT1B/1D receptors on the extracerebral, intracranial blood vessels that become dilated during migraine attack and on nerve terminals in the trigeminal system. Activation of these receptors results in cranial vessel constriction, inhibition of neuropeptide release and reduced transmission
Approved indications
- Migraine
Common side effects
- Dizziness
- Somnolence
- Asthenia/Fatigue
- Nausea
- Pain and other Pressure Sensations
- Dry Mouth
- Pain, location unspecified
- Diarrhea
- Vomiting
- Dyspepsia
- Tongue edema
- Abdominal distention
Drug interactions
- sertraline
- sibutramine
- tapentadol
- tranylcypromine
- venlafaxine
Key clinical trials
- Initiating Early Control of Migraine Pain and Associated Symptoms (PHASE3)
- Open-Label Study of AXS-07 for the Acute Treatment of Migraine in Adults With a Prior Inadequate Response to an Oral CGRP Inhibitor (EMERGE) (PHASE3)
- A Comparison of Nurtec ODT to Maxalt MLT-ODT in Adult ED Patients With Migraine Headache (PHASE4)
- Quality Improvement and Practice Based Research in Neurology Using the EMR (PHASE4)
- Efficacy and Safety of Rizatriptan-Naproxen (10/550 Mg) in the Acute Treatment of Migraine (PHASE3)
- Treatments of Migraine with Triptans in Individuals with Elevated Cardiovascular Risk and in Pregnant Women
- Study to Test an Approved Product in the Early Treatment of Migraine (0462-065) (PHASE3)
- Study to Test a Marketed Drug in the Treatment of Menstrual Migraine (0462-071) (PHASE3)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Maxalt CI brief — competitive landscape report
- Maxalt updates RSS · CI watch RSS
- Gensco portfolio CI