Drug intelligence / Profile preview

namitecan

Development stage
Phase 1
Lead developer
Sigma Tau Pharmaceuticals
Modality
Peptides, Small Molecules
Administration
Intravenous
01

Overview

Namitecan is a novel, hydrophilic camptothecin analogue of the 7-oxyiminomethyl series and acts as a potent topoisomerase I inhibitor. It was developed to overcome limitations of earlier camptothecins such as water insolubility and lactone instability. Namitecan stabilizes the DNA-topoisomerase I cleavable complex, leading to persistent DNA damage and cell death in tumor cells. It demonstrates marked cytotoxic potency due to increased intracellular accumulation and favorable subcellular localization. Preclinical studies showed significant antitumor efficacy across various human tumor xenografts—including those resistant to topotecan and irinotecan—with particular activity in squamous cell carcinomas, bladder cancer, and endometrial carcinoma. The drug has an acceptable toxicity profile with neutropenia as the dose-limiting effect. Clinical development is ongoing for solid tumors[1][4][5][6][7].

Brand names
namitecan
Other names
372105-27-6Namitecan [INN]UNII-X34Z8N66T3UNII-X-34Z8N66T3UNII-X 34Z8N66T3
02

Targets

TOP1 (DNA Topoisomerase I)

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