Rubitecan (Orathecin)

Target Profile to be Developed

A second-generation oral Camptothecin

The second asset in our scientific pipeline is Rubitecan (Orathecin), a second-generation oral Camptothecin. The oral-based Camptothecin treatment was acquired by Vivacitas after having been given to over 900 patients, and showing promising results as a second line of defense therapy. The next stages in clinical development are currently being evaluated.

AR-67 has the potential to deliver the efficacy of Camptothecins with significantly less gastrointestinal and hematological toxicity than Irinotecan. That could be a game changer for patients with gastrointestinal cancers.
Dr. Gerard Blobe, MD, PhD.Duke University School of Medicine.
AR–67 is a next generation camptothecin optimized for fewer side effects and blood-brain-barrier penetration. In glioblastoma patients treated with AR-67 on a clinical trial at our center, we saw encouraging outcomes and tumor shrinkage. AR-67 was extremely well tolerated. I believe AR-67 represents a novel approach in treating this devastating disease.
Dr. Jai Grewal, MD.NSPC Brain and Spine Surgery, NY

References

1. Novel silatecan displays high lipophilicity, improved blood stability and potent
anticancer activity. Bom D, et al J Med Chem 2000; 43:3970-3980

2. Silatecan DB-67 is a novel DNA Topo-1 targeted radiation sensitizer: Chen AY. Mol
Cancer Ther 2005; 4(2): 317-24.

3. Phase I study publication: Arnold SM, et al. Clin Cancer Res. 2010;6:673-680

4. Phase II study publication (abstract): Kumthekar P, et al. SNO 2019. Poster ACTR-40,
published in Neuro-Oncology(https://academic.oup.com/neuro-oncology)

5. Ubiquitin-dependent Destruction of Topoisomerase I Is
Stimulated by the Antitumor Drug Camptothecin*, Desai et al. The Journal of Biological Chemistry, Vol. 272, No. 39, Issue of September 26, pp. 24159–24164, 1997.  https://www.jbc.org

6. Metabolic Pathways of the Camptothecin Analog AR-67, Horn et al. Drug Metabolism and Disposition, Vol. 39, No. 4, 37390/3672838, 2011. https://dmd.aspetjournals.org