Mirogabalin CAS No. 1138245-13-2

Product Description

Mirogabalin is a next-generation gabapentinoid developed by Daiichi Sankyo that targets neuropathic pain by acting as a selective ligand for the α2δ-1 and α2δ-2 subunits of voltage-gated calcium channels (VGCCs). Unlike its predecessors, pregabalin and gabapentin, mirogabalin exhibits higher affinity for α2δ-1 (linked to analgesic effects) and lower affinity for α2δ-2 (associated with CNS side effects), potentially offering superior efficacy with reduced side effects such as dizziness and somnolence. Approved in Japan (2019) for diabetic peripheral neuropathy (DPN) and postherpetic neuralgia (PHN), it is also under investigation for fibromyalgia and lumbar spinal stenosis (LSS). Clinical trials, including the MiroTAS study, demonstrate its effectiveness as an add-on to NSAIDs, significantly reducing leg pain (VAS) and improving quality of life (EQ-5D-5L, PGIC) in LSS patients. With once- or twice-daily dosing and renal-adjusted titration, mirogabalin provides a promising alternative for patients who fail to respond or tolerate traditional gabapentinoids.

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Product Use & Characteristics

Chemical & Physical Properties

• Molecular Formula (MF): C₁₂H₁₉NO₂
• Molecular Weight (MW): 209.28 g/mol

Mechanism of Action

• Selective binding to α2δ-1 (analgesic) and α2δ-2 (CNS side-effect) subunits of VGCC

• Slower dissociation from α2δ-1 (t½ = 11.1 h) vs α2δ-2 (t½ = 2.4 h) → prolonged analgesia, lower dizziness/somnolence than pregabalin/gabapentin

• Reduces presynaptic Ca²⁺ influx → ↓ glutamate, substance P & CGRP release → diminished neuropathic pain signalling

Pharmacokinetics

Parameter	Value
Bioavailability	~90 % (oral)
Peak plasma (T_max)	0.5–1 h
Half-life (t½)	2.9–4.5 h (single); 3.6–4.9 h (multiple)
Metabolism	<20 % hepatic (UGT); 61–72 % renal unchanged
Dose Adjustment	Moderate renal impairment: 50 % dose; Severe: 75 % dose; No adjustment for mild hepatic impairment

Uses (Approved & Investigational)

1. Peripheral Neuropathic Pain
   • Diabetic Peripheral Neuropathic Pain (DPNP) – approved Japan, China, Taiwan, Korea
   • Post-herpetic Neuralgia (PHN) – approved Japan, Taiwan

2. Central Neuropathic Pain
   • Spinal-cord-injury (SCI) related pain – Phase III (Ushida 2023) – Class I evidence

3. Fibromyalgia – Phase III discontinued (USA/EU)

4. Chemotherapy-Induced Peripheral Neuropathy (CIPN) – Phase III (MiroCIP study) – significant pain/tingling relief

5. Orthopedic/Post-surgical neuropathic pain – Add-on to NSAIDs in lumbar spinal stenosis (MiroTAS study)

Recommended Dosing

Renal Function	Starting → Target
Normal (CrCl ≥60 mL/min)	5 mg BID → 10 mg BID → 15 mg BID
Moderate (30–59 mL/min)	2.5 mg BID → 5 mg BID → 7.5 mg BID
Severe (15–29 mL/min)	2.5 mg BID → 5 mg BID → 5 mg QD

Safety & Tolerability

• Common TEAEs: somnolence, dizziness, peripheral edema, weight gain, nasopharyngitis, constipation

• Discontinuation rate: ≤10 % (mostly mild–moderate)

• Drug interactions: probenecid/cimetidine modestly ↑ exposure; additive CNS depression with alcohol, lorazepam

• Switching: pregabalin → mirogabalin well-tolerated; improved AE profile (↓ dizziness, somnolence)

Cost-Effectiveness & Real-World Data

• ICER vs placebo: US$8,766–15,658 per QALY (Taiwan/China) – below WTP thresholds

• Real-world switching studies: >70 % patients successfully titrated; lower AE incidence vs pregabalin

Why us!

Qingdao Sigma Chemical Co., Ltd., established in January 2017 and headquartered in Qingdao, China, is a reliable chemical supplier. Specializing in pharmaceuticals, biochemical intermediates, and research chemicals, the company offers a diverse product portfolio, including peptides (e.g., Tirzepatide, Semaglutide), nootropics, veterinary products, and APIs, often marketed with ≥99% purity and COA certification. We provides R&D, custom synthesis, and contract manufacturing services at various scales, while claiming a global export presence across 100+ countries. With international warehouses in the USA, Europe, Australia, and Canada, Qingdao Sigma Chemical also facilitates drop-shipping and reshipments, positioning itself as a key supplier for laboratory and research applications.