- 【Updated on May 12, 2025】 Integration of CiNii Dissertations and CiNii Books into CiNii Research
- Trial version of CiNii Research Knowledge Graph Search feature is available on CiNii Labs
- 【Updated on June 30, 2025】Suspension and deletion of data provided by Nikkei BP
- Regarding the recording of “Research Data” and “Evidence Data”
Pharmacological, pharmacodynamics, and clinical profile of mirogabalin besylate (Tarlige<sup>®</sup> tablets 2.5 mg∙5 mg∙10 mg∙15 mg)
-
- Kitano Yutaka
- Specialty Medicine Research Laboratories I, Daiichi Sankyo Co., Ltd.
-
- Kai Kiyonori
- Medicinal Safety Research Laboratories, Daiichi Sankyo Co., Ltd.
-
- Yamamura Naotoshi
- Drug Metabolism & Pharmacokinetics Research Laboratories, Daiichi Sankyo Co., Ltd.
-
- Yoshiba Satoshi
- Clinical Pharmacology Department, Daiichi Sankyo Co., Ltd.
-
- Kuroha Masanori
- Clinical Development Department, Daiichi Sankyo Co., Ltd.
Bibliographic Information
- Other Title
-
- ミロガバリンベシル酸塩(タリージェ<sup>®</sup>錠2.5 mg・5 mg・10 mg・15 mg)の薬理学的および薬物動態学的特性と臨床試験成績
- 新薬紹介総説 ミロガバリンベシル酸塩(タリージェ錠2.5 mg・5 mg・10 mg・15 mg)の薬理学的および薬物動態学的特性と臨床試験成績
- シンヤク ショウカイ ソウセツ ミロガバリンベシル サンエン(タリージェジョウ 2.5 mg ・ 5 mg ・ 10 mg ・ 15 mg)ノ ヤクリガクテキ オヨビ ヤクブツ ドウタイガクテキ トクセイ ト リンショウ シケン セイセキ
Search this article
Description
<p>Mirogabalin, a novel ligand for the α2δ subunit of voltage-gated calcium channels, has been approved for the treatment of peripheral neuropathic pain including painful diabetic peripheral neuropathy (DPNP) and postherpetic neuralgia (PHN) in Japan. Mirogabalin showed potent and selective binding affinities for the α2δ subunits, and slower dissociation rates for the α2δ-1 subunit than for the α2δ-2 subunit. It also showed potent and long-lasting analgesic effects in rat models of neuropathic pain, and wider safety margins for the central nervous system side effects. A pharmacological study using mutant mice demonstrated that the analgesic effects of mirogabalin were mediated by binding of the drug to the α2δ-1 subunit, not the α2δ-2 subunit. The pharmacological properties of mirogabalin can be associated with its unique binding characteristics. The bioavailability of mirogabalin is high and its plasma exposure increases dose-proportionally. Mirogabalin is mainly excreted via the kidneys in an unchanged form, thus, mirogabalin has a low possibility of undergoing drug–drug interaction, while dose adjustment based on the creatinine clearance level is specified in patients with renal impairment. In double-blind, placebo-controlled phase 3 studies in Asian patients with DPNP and PHN, mirogabalin showed significant and dose-dependent pain relief, and all tested doses of mirogabalin were well tolerated. In summary, mirogabalin has a balanced efficacy versus safety profile, and can provide an alternative therapeutic option for the treatment of peripheral neuropathic pain.</p>
Journal
-
- Folia Pharmacologica Japonica
-
Folia Pharmacologica Japonica 154 (6), 352-361, 2019
The Japanese Pharmacological Society
- Tweet
Details 詳細情報について
-
- CRID
- 1390845702329636736
-
- NII Article ID
- 130007754352
-
- NII Book ID
- AN00198335
-
- ISSN
- 13478397
- 00155691
-
- NDL BIB ID
- 030106400
-
- PubMed
- 31787689
-
- Text Lang
- ja
-
- Article Type
- journal article
-
- Data Source
-
- JaLC
- NDL Search
- Crossref
- PubMed
- CiNii Articles
- OpenAIRE
-
- Abstract License Flag
- Disallowed