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karenitecin

Development stage: Phase 3
Lead developer: BioNumerik Pharmaceuticals
Modality: Small Molecules
Administration: Oral

Overview

Karenitecin is a novel, highly lipophilic, silicon-containing camptothecin derivative developed for superior oral bioavailability and increased lactone stability compared to earlier camptothecins. It acts as an antineoplastic agent by stabilizing the cleavable complex between topoisomerase I and DNA, leading to DNA breaks and apoptosis. Karenitecin has demonstrated broad anti-tumor activity, increased potency, insensitivity to common drug resistance mechanisms (such as Pgp/MRP/LRP), and enhanced tissue penetration due to its lipophilicity. It has been investigated primarily for the treatment of various cancers, including malignant glioma[1][2][4][5].

Brand names: Cositecan
Other names: karenitecincositecanKarentecin

Targets

TOP1 (DNA Topoisomerase I)

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