Discovery of MT-7117 (dersimelagon phosphoric acid) as a MC1R Agonist
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- Yamamoto Yasuo
- Discovery Technology Laboratories, Research Division, Mitsubishi Tanabe Pharma Corporation
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- Sato Atsushi
- Oncology & Immunology Unit, Research Division, Mitsubishi Tanabe Pharma Corporation
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- Morokuma Kenji
- Neuroscience Unit, Research Division, Mitsubishi Tanabe Pharma Corporation
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- Miyashiro Masahiko
- Mitsubishi Tanabe Pharma Corporation
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- Suzuki Tsuyoshi
- Oncology & Immunology Unit, Research Division, Mitsubishi Tanabe Pharma Corporation
Bibliographic Information
- Other Title
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- MC1R作動薬MT-7117（dersimelagon phosphoric acid）の創製
Abstract
Melanocortin 1 receptor (MC1R) agonists are expected as promising therapeutic agents for skin and autoimmune diseases by promoting melanogenesis and inhibiting inflammation and fibrosis. In fact, the peptide analog afamelanotide is approved for the treatment of erythropoietic protoporphyria (EPP), however it is used as a subcutaneous implant formulation. Thus, aiming at an oral drug that would greatly improve convenience for patients, we challenged the optimization of chemical structures to meet potent MC1R agonistic activity, excellent pharmacokinetic and safety profiles. In the course of our trials and errors, we successfully discovered MT-7117 (dersimelagon phosphoric acid) by “introduction of a carboxylic acid”, “introduction of a fluorine atom on pyrrolidine ring” and “conversion of imidazole-amide to tertiary amide”. As of February 2024, global phase 3 clinical studies of MT-7117 for EPP and X-linked protoporphyria (XLP) and phase 2 studies for systemic sclerosis (SSc) are ongoing.
Journal
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- MEDCHEM NEWS
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MEDCHEM NEWS 34 (2), 74-79, 2024-05-01
The Pharmaceutical Society of Japan
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Keywords
Details 詳細情報について
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- CRID
- 1390581468909751168
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- ISSN
- 24328626
- 24328618
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- Text Lang
- ja
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- Data Source
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- JaLC
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- Abstract License Flag
- Disallowed