G3.5-betaAla-SN38

G3.5-betaAla-SN38 is a research-stage dendrimer-drug conjugate designed to enhance the delivery and efficacy of SN38, the active metabolite of the topoisomerase I inhibitor irinotecan. The compound consists of a generation 3.5 carboxyl-terminated poly(amidoamine) (PAMAM) dendrimer covalently linked to SN38 via a β-alanine spacer. This architecture is intended to overcome the poor water solubility of SN38 and improve its oral bioavailability while potentially mitigating gastrointestinal toxicity. Preclinical studies in colorectal cancer cell lines, such as HCT-116 and HT-29, have demonstrated that the conjugate effectively inhibits cell proliferation, induces G2/M phase cell cycle arrest, and promotes nuclear fragmentation. The conjugate shows stability at physiological pH and is being explored for the treatment of colorectal carcinoma and its associated hepatic metastases.

Other names

G3.5-beta-alanine-SN38G-3.5-beta-alanine-SN38G 3.5-beta-alanine-SN38G3.5 PAMAM dendrimer-SN38 conjugate with beta-alanine spacerG-3.5 PAMAM dendrimer-SN38 conjugate with beta-alanine spacerG 3.5 PAMAM dendrimer-SN38 conjugate with beta-alanine spacer