Ubrogepant is a selective calcitonin gene-related peptide receptor antagonist produced as an active pharmaceutical ingredient for oral solid dosage formulations targeting acute migraine therapy. Manufactured under controlled synthetic routes, the molecule features defined stereochemical configuration and consistent polymorphic properties. Each batch is supplied with comprehensive analytical validation packages to support global regulatory submissions, precise impurity profiling, and scale-up manufacturing from clinical evaluation to commercial production.
Technical Specifications
|
Parameter |
Specification |
|
Product Name |
Ubrogepant |
|
CAS Number |
953762-84-8 |
|
Synonyms |
MK-1602 |
|
Structural Class |
Small-molecule CGRP receptor antagonist |
|
Physical Description |
White to off-white crystalline powder |
|
Assay (Purity) |
≥ 99.0% (anhydrous basis) |
|
Chiral Purity |
≥ 99.5% Enantiomeric Excess |
|
Storage Conditions |
Protected from light and moisture at 2°C to 8°C |
Quality & Analytical Standards
|
Identification |
Retention time and spectra match reference standards via HPLC and FTIR. |
|
Impurity Profile |
Individual specified impurities ≤ 0.10%; total impurities ≤ 0.50%. |
|
Water Content |
≤ 0.5% determined by volumetric Karl Fischer titration. |
|
Residue on Ignition |
≤ 0.1% via gravimetric analysis. |
|
Heavy Metals |
≤ 10 ppm measured by ICP-MS. |
|
Residual Solvents |
Complies with strict international harmonization limits for ethanol, ethyl acetate, and heptane. |
|
Particle Size Distribution |
D(0.5): 15 µm - 35 µm; d(0.9): < 75 µm verified by laser diffraction. |
Manufacturing Standards
Synthetic Route: Multi-step convergent synthesis utilizing advanced chiral resolution to secure absolute stereochemical integrity.
Reaction Control: Low-temperature amide coupling and catalytic hydrogenation executed under closed-system inert gas protection.
Purification: Multi-stage crystallization protocols designed to isolate target compounds and eliminate reaction byproducts.
Cleanroom Operations: Isolation, micronization, and packaging performed within ISO Class 8 cleanroom facilities equipped with high-efficiency particulate air filtration.
Production Scale: Scalable manufacturing capacity ranging from research quantities to commercial production blocks exceeding 100 kilograms per campaign.
Regulatory Documentation
Provided for every manufactured batch detailing complete physical and chemical test results against validated release criteria.
Open and closed part documentation prepared in structured formats to facilitate regulatory filings across international jurisdictions.
Complete method validation packages covering accuracy, precision, linearity, specificity, and robustness.
Accelerated and long-term stability data available to support verified shelf-life determinations.
Packaging & Storage
Primary Packaging
Double-layer medical-grade low-density polyethylene bags heat-sealed under nitrogen purge to eliminate residual oxygen and moisture.
Secondary Packaging
Rigid high-density polyethylene fiber drums or UN-certified aluminum barrier foil drums providing mechanical protection and light shielding.
Desiccant Integration
Food-grade silica gel packets positioned between containment layers to maintain stable internal micro-environments.
Pharmaceutical Applications
Utilized as the active pharmaceutical ingredient in the manufacture of immediate-release oral tablets and capsules.
Acts directly on calcitonin gene-related peptide receptors within the trigeminal cerebrovascular system to block nociceptive transmission.
Engineered particle size distribution optimizes direct compression and wet granulation manufacturing workflows, ensuring consistent dissolution profiles and high bioavailability.
FAQ
Q: What is the standard batch size available for initial evaluation?
A: Evaluation samples are supplied in quantities starting from 100 grams to 1 kilogram, accompanied by a complete batch-specific Certificate of Analysis.
Q: Is a Drug Master File available for regulatory review?
A: Yes, a comprehensive file structured according to established regulatory guidelines is maintained and available for cross-referencing upon receipt of confidentiality agreements and regulatory notices.
Q: How is stereochemical purity verified during routine production?
A: Chiral purity is quantified using validated high-performance liquid chromatography methods capable of detecting trace enantiomeric variations down to 0.05%.
Q: Can particle size distribution be adjusted for custom formulations?
A: Secondary processing parameters such as controlled jet milling can be adapted to meet specific particle size targets required for specialized tableting workflows.
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