Taxane Drugs and Un-natural Amino Acids
John Thottathil
Independent Consultant, Pharma Biotech Drug Development
Taxanes are a class of anticancer drugs widely used for various types of cancers and tumors.
Popular taxanes include Paclitaxel (Taxol), Abraxane (albumin bound taxol), Docetaxel (Taxotere), Cabazitaxel (Jevtana), Ortataxel (in development), Tesetaxel (in development).
They are used to treat patients with: lung, ovarian, breast, and prostate cancers and advanced forms of kaposis sarcoma and prevention of restenosis. Both Tesetaxel and Ortataxel are being developed (company websites) as oral drugs for the treatment of above causes and additional indications (gastric cancer, Solid tumors, and tumors resistant to paclitaxel)
All the taxanes have the baccatin (or modified baccatin, 10-DAB III for example) core structure and the 13-hydroxyl attached side chains. All the side chains are complex ?-hydroxy ?-amino acids. While baccatin core by itself is considered pharmacologically inactive, attachment of these side chains give the molecules the needed pharmacological effect as valuable drugs.
The presentation will give a brief summary of various general methods for the development and manufacturing of these unusual amino acids and their efficient coupling to baccatin core.
John is a pharma-life sciences product development and manufacturing leader; currently providing independent consulting services to the industry.
John is also currently the Chief Scientific Officer at LAT Pharma. Previously he served as Acting Head of Technical Development and Manufacturing at Genta Pharmaceuticals. John has held various senior management roles at New River Pharmaceuticals, Abbot in Immunodiagnostics Division, and at Bristol Myers Squibb. During his extensive career in drug product development he was involved in several major product launches including Taxol, Fosinopril and Entecavir.
John has 74 patents and pending patent applications, 44 publications in peer reviewed journals, and has chaired or presented at 25 conferences.