预约演示
更新于：2026-09-08
Dersimelagon
更新于：2026-09-08
概要
基本信息
非在研机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床1期 |
特殊审评快速通道 (美国)、孤儿药 (美国) |
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结构/序列
分子式C36H45F4N3O5 |
InChIKeyMUNWOYRHJPWQNE-GMFUQMJFSA-N |
CAS号1835256-48-8 |
关联
13
项与 Dersimelagon 相关的临床试验NCT06994286
A Phase 1, Randomized, Double-Blind, Placebo-Controlled Study to Investigate the Pharmacokinetics, Safety, Tolerability and Pharmacodynamics of Single and Multiple Doses of MT-7117 in Chinese Healthy Subjects
NCT06144840
A Phase 3, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate Efficacy, Safety, and Tolerability of MT-7117 in Adults and Adolescents With Erythropoietic Protoporphyria or X-Linked Protoporphyria
NCT05241535
A Phase 1, Randomized, Partial Double-Blind, Placebo- and Positive-Controlled, Three-way Crossover Study to Evaluate the Effect of MT-7117 on the QT/QTc Interval in Healthy Subjects
100 项与 Dersimelagon 相关的临床结果
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100 项与 Dersimelagon 相关的转化医学
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100 项与 Dersimelagon 相关的专利（医药）
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13
项与 Dersimelagon 相关的文献（医药）2026-03-04EXPERT OPINION ON PHARMACOTHERAPY
New and currently investigated pharmacotherapies for the erythropoietic protoporphyrias: spotlight on dersimelagon and bitopertin
Review
作者: Falchetto, Rocco ; Dechant, Cornelia ; Barman-Aksözen, Jasmin ; Wäscher, Sebastian ; Granata, Francesca
INTRODUCTION:
The erythropoietic protoporphyrias (EPP) are ultra-rare inborn errors of the heme biosynthesis characterized by painful and debilitating phototoxic reactions in the blood vessels upon exposure to visible light. Afamelanotide is the only approved treatment for EPP and effectively prevents pain and prolongs the time patients can spend in sunlight. However, afamelanotide does not address the underlying disease mechanism and is currently only approved for use in adult patients, leaving children and adolescents without a treatment option. The two investigational pharmacotherapies, dersimelagon and bitopertin, could offer benefits such as treatment options for children and prevention of some of the associated disease complications.
AREAS COVERED:
This narrative review (using Pubmed and trial databases) aims to provide an overview of the status of development of dersimelagon and bitopertin, with a focus on the prevention of phototoxicity.
EXPERT OPINION:
The currently available trial data on dersimelagon and bitopertin suggests treatment effects in EPP as compared to placebo control groups. However, safety and efficacy of dersimelagon and bitopertin need to be further characterized. Moreover, to ensure benefit for patients and access to therapy after regulatory approval, it also would be important to generate data on the relative safety and efficacy as compared to afamelanotide.
2025-02-01Pharmacology Research & Perspectives
Assessment of Potential Drug–Drug Interactions for Novel Oral Melanocortin‐1 Receptor Agonist Dersimelagon
Article
作者: Ogasawara, Akihito ; Inoue, Shinsuke ; Teng, Renli ; Ide, Ryosuke ; Tsuda, Minoru
ABSTRACT:
Dersimelagon is a novel investigational orally administered selective agonist of the melanocortin‐1 receptor. The drug–drug interaction (DDI) potential of dersimelagon was investigated in both nonclinical (in vitro) and clinical studies. The in vitro inhibition of CYP/UGT isoforms and efflux/uptake transporters by dersimelagon was assessed. The impact of 300‐mg dersimelagon on the pharmacokinetics (PK) of substrate drugs and the effect of co‐administering verapamil on 100‐mg dersimelagon PK (as substrate drug) were investigated in healthy participants in a Phase 1 study. DDIs were assessed based on ratios of Cmax and AUC0‐∞ of substrate drug administered alone and with dersimelagon (or verapamil). Relatively potent in vitro inhibition of CYP2C9, CYP3A, UGT1A1, BCRP, P‐gp, and OATPs by dersimelagon was observed. In the clinical study, exposures of atorvastatin (CYP3A, P‐gp, BCRP, OATP substrate) rosuvastatin (BCRP and OATP substrate), and β‐hydroxy simvastatin (metabolite of simvastatin) increased 2‐ to 3‐fold (atorvastatin: Cmax LS mean ratio = 198.0%; AUC0‐∞ ratio = 196.6%; rosuvastatin: Cmax ratio = 316.5%, AUC0‐∞ ratio = 206.0%) when co‐administered with dersimelagon. Midazolam (CYP3A substrate), digoxin (P‐gp), pravastatin (OATP), and simvastatin (CYP3A) did not show any clinically relevant DDI effects when co‐administered with dersimelagon. Dersimelagon exposure increased ~25% when co‐administered with verapamil, an effect not considered clinically relevant. Dersimelagon 300 mg did not elicit major DDIs involving CYP/UGT enzymes and drug transporters; however, dersimelagon may have potential for clinically relevant DDIs with drugs that are substrates for BCRP, such as atorvastatin and rosuvastatin, and caution should be exercised when co‐administering 300‐mg dersimelagon with these statin drugs.Trial Registration:ClinicalTrials.gov: NCT04793295, NCT04402489, NCT04440592, NCT02834442, NCT03520036, NCT03503266
2024-12-26JOURNAL OF MEDICINAL CHEMISTRY
Discovery of MT-7117 (Dersimelagon Phosphoric Acid): A Novel, Potent, Selective, and Nonpeptidic Orally Available Melanocortin 1 Receptor Agonist
Article
作者: Adachi, Takashi ; Andou, Junki ; Suzuki, Tsuyoshi ; Morokuma, Kenji ; Sato, Atsushi ; Ogasawara, Akihito ; Kawano, Yuko ; Kondo, Masahiro ; Miyashiro, Masahiko ; Yamamoto, Yasuo ; Ide, Mika
Activation of the melanocortin 1 receptor (MC1R) mediates melanogenesis in melanocytes, anti-inflammatory effects in inflammatory cells, and antifibrotic effects in fibroblasts. Thus, MC1R agonists are expected to be beneficial for treating skin, autoimmune, inflammatory, and fibrotic diseases. Afamelanotide, an α-melanocyte-stimulating hormone (α-MSH) analogue MC1R agonist, is used clinically for treating erythropoietic protoporphyria (EPP) as a subcutaneous implant formulation. We explored nonpeptidic small-molecule MC1R agonists with the aim of identifying more convenient oral drugs. By exploring the structure of previously reported compound 5, we discovered compound 11 (MT-7117: dersimelagon phosphoric acid). This compound exhibited strong MC1R agonistic activity, good pharmacokinetic properties, and excellent safety profiles. Furthermore, compound 11 was effective in animal pigmentation evaluation and skin fibrosis model studies. Compound 11 is currently in clinical trials for the treatment of EPP, X-linked protoporphyria (XLP), and systemic sclerosis (SSc). Proof of concept was obtained in phase 2 clinical studies on EPP and XLP.
100 项与 Dersimelagon 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 红细胞生成性卟啉病 | 临床3期 | 美国 | 2021-08-10 | |
| 红细胞生成性卟啉病 | 临床3期 | 日本 | 2021-08-10 | |
| 红细胞生成性卟啉病 | 临床3期 | 澳大利亚 | 2021-08-10 | |
| 红细胞生成性卟啉病 | 临床3期 | 保加利亚 | 2021-08-10 | |
| 红细胞生成性卟啉病 | 临床3期 | 加拿大 | 2021-08-10 | |
| 红细胞生成性卟啉病 | 临床3期 | 捷克 | 2021-08-10 | |
| 红细胞生成性卟啉病 | 临床3期 | 法国 | 2021-08-10 | |
| 红细胞生成性卟啉病 | 临床3期 | 德国 | 2021-08-10 | |
| 红细胞生成性卟啉病 | 临床3期 | 意大利 | 2021-08-10 | |
| 红细胞生成性卟啉病 | 临床3期 | 荷兰 | 2021-08-10 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 76 | (MT-7117) | 繭獵醖製積壓醖壓淵築(簾簾鏇構製鏇淵選觸製) = 顧鹹築網選衊鹹顧構淵 淵廠憲淵壓繭淵築壓鏇 (壓艱顧構艱遞衊鏇淵鏇, 鑰窪襯簾遞襯顧淵鹹襯 ~ 積壓醖鑰糧襯艱網顧淵) 更多 | - | 2025-11-03 | ||
Placebo (Placebo) | 繭獵醖製積壓醖壓淵築(簾簾鏇構製鏇淵選觸製) = 餘鏇獵膚淵糧築齋願糧 淵廠憲淵壓繭淵築壓鏇 (壓艱顧構艱遞衊鏇淵鏇, 願構壓壓顧襯夢淵構構 ~ 簾衊顧膚鹽糧蓋簾憲選) 更多 | ||||||
临床3期 | 184 | placebo (DBT ITT1 Placebo) | 蓋獵淵網繭選積遞遞夢(廠鏇獵鏇獵繭鹹窪蓋鏇) = 鹹窪醖網壓窪遞淵簾遞 構鑰艱鑰鏇蓋糧餘鑰窪 (觸鏇夢蓋顧糧觸夢壓鹽, 10.29) 更多 | - | 2025-03-21 | ||
(DBT ITT1 MT- 7117 Low Dose) | 蓋獵淵網繭選積遞遞夢(廠鏇獵鏇獵繭鹹窪蓋鏇) = 壓顧淵觸廠願鑰衊鏇鏇 構鑰艱鑰鏇蓋糧餘鑰窪 (觸鏇夢蓋顧糧觸夢壓鹽, 10.04) 更多 | ||||||
临床1期 | - | 144 | 衊艱淵餘築壓膚壓構膚(製壓鬱艱顧齋衊獵膚鹽) = 鏇鹹艱鹹衊積膚廠積醖 糧齋願窪簾觸艱築積鑰 (齋廠餘窪餘壓憲廠鹽憲 ) 更多 | - | 2023-04-15 | ||
Placebo | 衊艱淵餘築壓膚壓構膚(製壓鬱艱顧齋衊獵膚鹽) = 鏇顧積糧觸淵繭壓願簾 糧齋願窪簾觸艱築積鑰 (齋廠餘窪餘壓憲廠鹽憲 ) | ||||||
临床2期 | 102 | (MT-7117 Low Dose) | 糧憲鑰繭遞顧鑰構積鹽(願餘顧顧製窪獵願積憲) = 襯選繭願簾餘簾簾網簾 鏇糧顧網築夢憲鹹醖鬱 (築獵鹽憲選築選夢觸淵, 76.8) 更多 | - | 2023-01-20 | ||
(MT-7117 High Dose) | 糧憲鑰繭遞顧鑰構積鹽(願餘顧顧製窪獵願積憲) = 夢遞膚顧齋製築夢鏇襯 鏇糧顧網築夢憲鹹醖鬱 (築獵鹽憲選築選夢觸淵, 100) 更多 |
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