Product Information：
Product Number: R047000A
English Name: Rizatriptan Benzoate
English Alias: 2-(5-((1H-1,2,4-triazol-1-yl)methyl)-1H-indol-3-yl)-N,N-dimethylethanamine benzoate
CAS Number: 145202-66-0
Molecular Formula: C₁₅H₁₉N₅·C₇H₆O₂ (Rizatriptan Benzoate)
Molecular Weight: 269.34 (Active Ingredient) + 122.12 (Benzoic Acid) = 391.46
Advantages：
High-purity API：HPLC purity ≥99.5%, crystal form confirmed by X-ray diffraction (XRD), complying with international pharmacopoeia standards (USP, EP), ensuring batch-to-batch stability.
Bioavailability advantage：Reaches peak plasma concentration (Cmax) within 1.5 hours after oral administration, with absolute bioavailability of ~45%, providing faster migraine relief than (e.g., Sumatriptan).
Strong formulation compatibility：As the benzoate form, it exhibits excellent water solubility (10 mg/mL) and chemical stability, suitable for developing various formulations such as tablets and orally disintegrating tablets.
Applications：
Acute migraine treatment：As a 5-HT1B/1D receptor agonist, used for acute attack relief of migraine with or without aura in adults, rapidly constricting intracranial blood vessels and inhibiting trigeminal pain signaling.
Combination therapy research：Combined with non-steroidal anti-inflammatory drugs (NSAIDs) to enhance analgesic effect and reduce single-drug dosage; currently undergoing Phase III clinical trials for pediatric migraine (6-17 years old) indication expansion.
Generic drug consistency evaluation：Serves as the Reference Listed Drug (RLD) for generic drug R&D, supporting dissolution comparison studies (f2 factor ≥50 in pH 1.2/4.5/6.8 media) and bioequivalence (BE) trials.
Background Description：
Rizatriptan is a second-generation 5-HT receptor agonist developed by Merck and approved in 1998. Its mechanism of action involves selectively activating 5-HT1B receptors in intracranial vascular smooth muscle to constrict blood vessels and inhibiting pain neurotransmitter release from trigeminal nerve endings. The benzoate form improves drug water solubility and chemical stability. Clinical studies show that a single 10 mg oral dose relieves pain in 70% of patients within 2 hours, with a lower incidence of cardiovascular adverse reactions than first-generation triptans.
Research Status：
Formulation innovation：Orally disintegrating tablets (ODT) using micronization technology (D90≤5 μm) enhance disintegration speed (≤30 seconds), approved in Europe for patients with swallowing difficulties; transdermal patches are in Phase II clinical trials, extending the dosing interval to 12 hours.
Safety optimization：Long-term use (≥6 months) studies show a cardiac valve lesion incidence <0.1% (n=2300), safer than drugs like phentermine; however, caution is still needed for serotonin syndrome risk when combined with monoamine oxidase inhibitors (MAOIs).
Biomarker research：Monitoring plasma CGRP (calcitonin gene-related peptide) level changes reveals that rizatriptan inhibits CGRP release within 30 minutes after administration, providing a new target for migraine mechanism research.
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