Monomethyl auristatin F explained

Monomethyl auristatin F (MMAF) is a synthetic antineoplastic agent.^[1] It is part of the approved drug belantamab mafodotin in multiple myeloma and some experimental anti-cancer antibody-drug conjugates such as vorsetuzumab mafodotin and SGN-CD19A. In International Nonproprietary Names for MMAF-antibody-conjugates, the name mafodotin refers to MMAF plus its attachment structure to the antibody.^[2]

Mechanism of action

Monomethyl auristatin F is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. It is linked to an antibody with high affinity to structures on cancer cells, causing MMAF to accumulate in such cells.^[3]

Chemistry

MMAF is actually desmethyl-auristatin F; that is, the N-terminal amino group has only one methyl substituent instead of two as in auristatin F itself.

See also

• Monomethyl auristatin E

Notes and References

1. 24569262. 2014. Tai. Y. T.. Novel afucosylated anti-B cell maturation antigen-monomethyl auristatin F antibody-drug conjugate (GSK2857916) induces potent and selective anti-multiple myeloma activity. Blood. Mayes. P. A.. Acharya. C. Zhong. M. Y.. Cea. M. Cagnetta. A. Craigen. J. Yates. J. Gliddon. L. Fieles. W. Hoang. B. Tunstead. J. Christie. A. L.. Kung. A. L.. Richardson. P. Munshi. N. C.. Anderson. K. C.. 10.1182/blood-2013-10-535088 . 123 . 20 . 3128–38. 4023420.
2. http://www.ama-assn.org/resources/doc/usan/mafodotin.pdf Statement on a nonproprietary name adopted by the USAN Council: Mafodotin
3. 10.3390/toxins3070848. 22069744. Immunotoxins and Anticancer Drug Conjugate Assemblies: The Role of the Linkage between Components. Toxins. 3. 12. 848–883. 2011. Dosio . F. . Brusa . P. . Cattel . L. . 3202854. free.