PharmaceuticalGabapentinoidAlpha-2-delta ligandAnalgesic

Mirogabalin

Also known as Tarlige · DS-5565

Written by enwyReviewed 5 Aug 20261 sources0 comments

Mirogabalin is a newer gabapentinoid approved in Japan and several Asian markets for peripheral neuropathic pain. It binds the same alpha-2-delta subunit as pregabalin but with reported selectivity for the alpha-2-delta-1 isoform, which its developer argues may separate analgesia from CNS side effects. It carries the class dependence and withdrawal considerations.

01 Overview

Mirogabalin (brand Tarlige) was approved in Japan in 2019 and later in South Korea, Taiwan and Thailand for diabetic peripheral neuropathic pain and postherpetic neuralgia. Phase III trials support efficacy, but the total human evidence base is smaller and more recent than gabapentin or pregabalin.

It has slower dissociation from alpha-2-delta-1 and faster dissociation from alpha-2-delta-2 than pregabalin, a profile proposed to reduce CNS side effects, though comparative data are limited. As a gabapentinoid it should be tapered rather than stopped abruptly.

02 Mechanism

Binds voltage-gated calcium channel alpha-2-delta subunits with reported preferential, slowly dissociating binding to the alpha-2-delta-1 isoform, reducing excitatory neurotransmitter release.

03 Dosing

Tier	Dose	Route	Notes
Neuropathic pain	10–30 mg/day	Oral	Usually 5 mg twice daily titrated to 15 mg twice daily; reduce in renal impairment.

04 Effects

Effect	Magnitude	Evidence
Neuropathic pain reliefReduced average daily pain in diabetic peripheral neuropathic pain and postherpetic neuralgia in phase III trials.	Moderate vs placebo	Clinical
Improved sleep interference from painSecondary endpoints showed reduced pain-related sleep disruption.	Moderate	Clinical

05 Side effects

Effect	Severity	Frequency	Evidence
Somnolence and dizzinessDrowsiness and dizziness, the most frequent trial adverse events.	Mild	Common	Clinical
Peripheral oedema and weight gainFluid retention and modest weight gain as seen across gabapentinoids.	Mild	Uncommon	Clinical
Withdrawal on abrupt cessationBy class analogy, abrupt stopping may provoke anxiety, insomnia and autonomic symptoms.	Moderate	Not well quantified	Unconfirmed

06 Legal status

United States

Not approved by the FDA

No US marketing authorisation; not routinely available. · as of Jan 2026

Approved prescription drug (Tarlige)

Approved for peripheral neuropathic pain since 2019. · as of Jan 2026

07 References

Mirogabalin for diabetic peripheral neuropathic pain: a randomized phase III studyDiabetes, Obesity and Metabolism, 2019

08 Discussion0 comments

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This page is reference information, not medical advice. Doses and protocols are documented as they appear in the clinical literature and in practice — describing them is not a recommendation to use them. Countermeasures listed here are not a substitute for a physician. Legal status varies by jurisdiction and changes.