Geron announces initiation of clinical trial for its telomerase inhibitor drug in patients with solid tumor malignancies

05-Apr-2006

Geron Corporation announced that it has initiated clinical testing of its lead anti-cancer compound, GRN163L, in patients with solid tumor malignancies at The University of Chicago Cancer Research Center. This Phase I, dose-escalation trial of GRN163L is primarily designed to demonstrate the safety and tolerability of GRN163L administered intravenously (IV) on a weekly basis in patients with refractory or relapsed solid tumor malignancies. This study will also evaluate the tolerability of IV infusions of GRN163L at various rates of administration, and enable an assessment of the pharmacokinetic profile of GRN163L at escalating doses and at decreasing infusion durations. A secondary endpoint of the trial is the preliminary evaluation of anti-tumor activity of GRN163L in this patient population.

GRN163L is a potent inhibitor of telomerase. Inhibition of telomerase activity by GRN163L in cancer cells results in telomere shortening, and leads to cell cycle arrest or apoptosis. GRN163L is a 13-mer oligonucleotide N3¡¦"_ P5¡¦ thio-phosphoramidate (NPS oligonucleotide) that is covalently attached to a C16 (palmitoyl) lipid moiety. GRN163L binds directly with high affinity to the template region of the RNA component of human telomerase (hTR), which lies in the active or catalytic site of hTERT, the telomerase reverse transcriptase. GRN163L binding to hTR results in direct, competitive inhibition of telomerase enzymatic activity. The mechanism of action of the drug is not antisense mediated.

https://www.bionity.com/en/news/53688/geron-announces-initiation-of-clinical-trial-for-its-telomerase-inhibitor-drug-in-patients-with-solid-tumor-malignancies.html