Auristatin E-d 8 is the deuterium labeled Auristatin E. Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10, is linear peptides comprised of four amino acids [1] [2] [3].
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. MADDON Paul J, et al. PSMA ANTIBODIES AND PROTEIN MULTIMER. 2002 October 23. WO 03/034903 A2
[2]. Peter D. Senter, et al. PENTAPEPTIDE COMPOUNDS AND USES RELATED THERETO. 2005 Jan. 13. US 2005/0009751 A l.
[3]. LAW, Che-Leung, et al. TREATMENT OF IMMUNOLOGICAL DISORDERS 5 USING ANTI-CD30 ANTIBODIES. 2002 November 20. WO 03/043583 A2.
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. MADDON Paul J, et al. PSMA ANTIBODIES AND PROTEIN MULTIMER. 2002 October 23. WO 03/034903 A2
[2]. Peter D. Senter, et al. PENTAPEPTIDE COMPOUNDS AND USES RELATED THERETO. 2005 Jan. 13. US 2005/0009751 A l.
[3]. LAW, Che-Leung, et al. TREATMENT OF IMMUNOLOGICAL DISORDERS 5 USING ANTI-CD30 ANTIBODIES. 2002 November 20. WO 03/043583 A2.