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isovalerylspiramycin I
- Development stage
- Preclinical
- Lead developer
- Shen Yang Fuyang Medicine Technology
- Modality
- RNA-Targeting Small Molecules → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Isovalerylspiramycin I is a semi-synthetic macrolide antibiotic and a principal active component of carrimycin, derived by acylating the 4'-OH group of spiramycin with an isovaleryl side chain. It features a 16-membered lactone ring structure and exhibits both antibacterial and anticancer properties. Mechanistically, it acts as an inhibitor of topoisomerase 1 (TOP1), directly binding to this enzyme, thereby inhibiting DNA replication in cancer cells. Additionally, it suppresses the ATR/CHEK1 DNA damage repair pathway, leading to increased DNA damage and apoptosis in tumor cells. Isovalerylspiramycin I has demonstrated efficacy against various solid tumors (including osteosarcoma) and shows potential antiviral activity against enterovirus, herpes virus, influenza virus, and HIV[2][3][5][10].
- Other names
- ISP-I
02
Targets
TOP1 (DNA Topoisomerase I)
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