AIT-102 is a novel molecule that was selected from a series of analogues of the natural product mithramycin1. Mithramycin was originally isolated from the soil bacteria Streptomyces agrillaceus, and first approved as a pharmaceutical agent in 1970. Though it has been used for the treatment of various cancers, its use was limited due to liver toxicity2, and manufacture of mithramycin for pharmaceutical use was discontinued in 20003.
AIT-102 has been determined to have between 25-40x lower toxicity than mithramycin while demonstrating equal or greater anti-tumor activity against multiple tumor cell lines and tumor xenografts1,4.
1 Núñez, L. E., Nybo, S. E., González-Sabín, J., Pérez, M., Menéndez, N., Braña, A. F., ... & Méndez, C. (2012). A novel mithramycin analogue with high antitumor activity and less toxicity generated by combinatorial biosynthesis. Journal of medicinal chemistry, 55(12), 5813-5825.
2 Osada, N., Kosuge, Y., Ishige, K., & Ito, Y. (2013). Mithramycin, an agent for developing new therapeutic drugs for neurodegenerative diseases. Journal of pharmacological sciences, 122(4), 251-256.
3 NCATS Inxight Drugs: https://drugs.ncats.io/drug/NIJ123W41V
4 Méndez, C., González-Sabín, J., Morís, F., & Salas, J. A. (2015).Expanding the chemical diversity of the antitumoral compound mithramycin by combinatorial biosynthesis and biocatalysis: the quest for mithralogs with improved therapeutic window. Planta Medica, 81(15), 1326-1338.
