Mertansine
Encyclopedia
Mertansine is a cytotoxic agent also known as DM1. It is a maytansinoid
(that is, a derivative of maytansine
).
Its patent rights are owned by ImmunoGen Inc.
s combining monoclonal antibodies
with mertansine as the cytotoxic component. Mertansine is linked via 4-mercaptovaleric acid.
Mertansine can also be linked via a more complicated structure – 4-(3-mercapto-2,5-dioxo-1-pyrrolidinylmethyl)-cylohexanecarboxylic acid or MCC –, in which case the International Nonproprietary Name
of the conjugate is formed with emtansine:
Maytansinoid
A maytansinoid is a chemical derivative of maytansine.Some are being investigated as the cytotoxic component of antibody-drug conjugates.Examples:*Ansamitocin*Mertansine...
(that is, a derivative of maytansine
Maytansine
Maytansine is a cytotoxic agent. It inhibits the assembly of microtubules by binding to tubulin at the rhizoxin binding site.It is a macrolide of the ansamycin type and can be isolated from plants of the genus Maytenus....
).
Its patent rights are owned by ImmunoGen Inc.
Uses
The following drugs are antibody-drug conjugateAntibody-drug conjugate
Antibody-drug conjugates are a new type of targeted therapy, used for example for cancer. They consist of an antibody linked to a payload drug . Hence, they are a type of immunoconjugate and often an immunotoxin.The antibody causes the ADC to bind to the target cancer cells...
s combining monoclonal antibodies
Monoclonal antibodies
Monoclonal antibodies are monospecific antibodies that are the same because they are made by identical immune cells that are all clones of a unique parent cell....
with mertansine as the cytotoxic component. Mertansine is linked via 4-mercaptovaleric acid.
- Bivatuzumab mertansineBivatuzumab mertansineBivatuzumab mertansine is a combination of bivatuzumab, a humanized monoclonal antibody, and mertansine, a cytotoxic agent. It is designed for the treatment of squamous cell carcinoma....
- Cantuzumab mertansineCantuzumab mertansineCantuzumab mertansine is a humanized monoclonal antibody used to treat colorectal cancer and other types of cancer. It is linked to a cytotoxic agent, mertansine.Three phase I clinical studies had reported results by 2003....
- Lorvotuzumab mertansineLorvotuzumab mertansineLorvotuzumab mertansine is an antibody-drug conjugate of lorvotuzumab linked to mertansine intended for CD56 positive cancers .It has been granted Orphan drug status for Merkel cell carcinoma....
(IMGN901) for CD56 positive cancers, for example multiple myelomaMultiple myelomaMultiple myeloma , also known as plasma cell myeloma or Kahler's disease , is a cancer of plasma cells, a type of white blood cell normally responsible for the production of antibodies...
Mertansine can also be linked via a more complicated structure – 4-(3-mercapto-2,5-dioxo-1-pyrrolidinylmethyl)-cylohexanecarboxylic acid or MCC –, in which case the International Nonproprietary Name
International Nonproprietary Name
An International Nonproprietary Name is the official nonproprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization...
of the conjugate is formed with emtansine:
- Trastuzumab emtansineTrastuzumab emtansineTrastuzumab emtansine is an antibody-drug conjugate consisting of the antibody trastuzumab linked to the cytotoxin mertansine ....
(T-DM1), an anti-HER2/neuHER2/neuHER-2 also known as proto-oncogene Neu, receptor tyrosine-protein kinase erbB-2, CD340 or p185 is an enzyme that in humans is encoded by the ERBB2 gene. Over expression of this gene is correlated with higher aggressiveness in breast cancers...
antibody-drug conjugate